List of editors
Edited by Mizaton Hazizul Hasan, Kalavathy Ramasamy, Lim Siong Meng, Aisyah Hasyila
Jahidin, Gurmeet Kaur Surindar Singh, Kamran Ashraf, Nor Hayati Abu Samah, Neoh Chin
Fen and Fazlin Mohd Fauzi
Sponsorship
Publication charges for this supplement were funded by the conference.
Numbering format
I - Introduction
KN – Keynote Lecture
PL – Plenary Lecture
IL – Invited Lecture
OPT – Oral Presenter Pharmaceutics
OPP – Oral Presenter Pharmacology
OPL– Oral Presenter Life Sciences
OPC – Oral Presenter Chemistry
PPT – Poster Presenter Pharmaceutics
PPP – Poster Presenter Pharmacology
PPL– Poster Presenter Life Sciences
PPC – Poster Presenter Chemistry
PPR – Poster Presenter Pharmacy Practice
INTRODUCTION
Asian Conference on Pharmaceutical Sciences (Asia Pharm) is an international conference
dedicated to promoting advances in pharmaceutical sciences. Asia Pharm was first held
in Vietnam, from July 10-12 2016, with the theme of “Advances in Pharmaceutical and
Biosciences”. Asia Pharm I was co-organised by Ton Duc Thang University, Vietnam and
Seoul National University, South Korea. Following the success of Asia Pharm I, Asia
Pharm II was hosted from July 20-22 2017 at Seoul National University with the theme
of “Education and Science in Pharmacy”. The Asia Pharm network was further expanded
with the organisation of the third series of Asia Pharm where it was organised by
Bandung Institute of Technology, Indonesia. Asia Pharm III was held from July 2-4
2018 in Bali with the theme of “Expecting the role of pharmaceutical sciences in discovering
future medicines”. This year, the Faculty of Pharmacy, Universiti Teknologi MARA will
play host for the fourth series of Asia Pharm. Asia Pharm IV took place from August
28-29 2019 with the theme of “Advancing Health Care through Collaborative Innovation”
Asia Pharm has consistently becoming an important annual international scientific
conference that serves as a platform to discuss and present challenges, ideas and
innovation in the field of pharmaceutical sciences that includes diverse areas such
as Drug Design and Discovery, Formulation Design and Pharmaceutical Technology, Natural
Products, Translational Research and Individualized Medicines, Pharmacokinetics or
Pharmacodynamics and Systems Biology, Regulatory Science, Analytical Sciences and
Quality, and Biotechnology. This year, Asia Pharm IV aims to not only continue the
exchange of ideas, but stimulate a culture of collaborative innovation, promoting
open forms of collaboration where access to different but complementary capabilities
and knowledge among participants would enable the acceleration of innovation. Furthermore,
by promoting a culture of collaborative innovation, significant progress can be made
from the conception, to the use and application of medicines. This would be beneficial
in improving the health of the population and also the health care system, on a national
and global level.
KEYNOTE ADDRESS
KN1 A pharmaceutically scientific approach to treating Aβ amyloid as the cause of
Alzheimer’s disease
Colin L Masters
The Florey Institute, The University of Melbourne, Kenneth Myer Building, 30 Royal
Parade, Parkville, Victoria 3010, Australia
Correspondence: Colin L Masters (c.masters@unimelb.edu.au)
The etiology of Alzheimer’s disease (AD) is best understood through the deposition
of Aβ-amyloid (Aβ). There are two basic forms of AD. The common (>95%) form is sporadic
and is caused by the failure to clear Aβ (mean age at onset 80 years). The rare (<
5%) autosomal dominant familial form is caused by the over-production of Aβ42, also
on a background of failure to clear (mean age at onset 45 years). In both forms, the
kinetics of Aβ accumulation are similar, taking about 30 years to accumulate a total
of approximately 7mg of Aβ. Thus, we estimate that sporadic AD starts about the age
of 50 years and the autosomal dominant form starts about 15 years of age. The advent
of validated biomarkers (PET/CSF Aβ and tau) now provides us with unprecedented opportunities
for preclinical diagnosis, enabling the development of primary and secondary prevention
strategies. Predictive algorithms utilizing age, biomarkers, polygenic and vascular
risk scores are now being developed from longitudinal cohort studies to estimate times
of onset and rates of cognitive decline. Applications of biomarker screens (blood,
CSF, PET) to subjects who are about to cross the lower cut point threshold will define
a population who may be suitable for primary prevention clinical trials.
Therapeutic targeting the Aβ pathway remains the principal strategy for delaying onset
of AD. There are many molecular targets in this pathway, and no single one is likely
to prove efficacious on its own. Therefore, a combination of strategies needs to be
developed and applied.
PLENARY LECTURE
PL1 Potential therapeutic targets for the treatment of tamoxifen-resistant breast
cancer
Keon Wook Kang
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National
University, Seoul 08826, Korea
Correspondence: Keon Wook Kang (kwkang@snu.ac.kr)
Breast cancer is the most common malignancy in Western women and grows under hormone-dependent
control. Hence, the ability to reduce breast tumor growth through the administration
of anti-estrogens has played a key role in the endocrine therapy of breast cancer.
The non-steroidal anti-estrogen, tamoxifen (TAM), is the most widely used anti-estrogen
in estrogen receptor-positive breast cancer patients. Although most patients are initially
responsive, resistance to TAM is a critical problem for anti-estrogen therapy. To
mimic this condition, we established an MCF-7 derived TAM-resistant cell line (TAMR-MCF-7
cells) by long-term culture of MCF-7 cells with 4-hydroxytamoxifen in 2007. RNA sequencing
analysis using MCF-7 and TAMR-MCF-7 cells showed that many coding and non-coding RNAs
regulating both estrogen signaling and epithelial mesenchymal transition were differentially
expressed in both the cell types. In this presentation, I will briefly summarize our
previous studies identifying potential targets to overcome TAM resistance and the
related pharmacological approaches.
Keyword: breast cancer, EMT, tamoxifen-resistance, therapeutic targets
PL2 Vietnamese ginseng – from an ethno-medicine to a national product of Vietnam
Minh Duc Nguyen1, Jeong Hill Park2
1Faculty of Pharmacy, Ton Duc Thang University, Ho Chi Minh City, Vietnam; 2College
of Pharmacy, Seoul National University, Seoul 08826, Korea
Correspondence: Minh Duc Nguyen (nguyenminhduc@tdtu.edu.vn)
Panax species occur in the northern hemisphere from Central Himalaya to North America
through China, Korea and Japan. This genus includes the well-known medicinal plant
Panax ginseng C.A. Meyer (Korean or Asian ginseng) and its two congeners, P. notoginseng
(Burk.) F. H. Chen (Sanchi ginseng), and P. quinquefolium L. (American ginseng), which
have been widely used in many countries of the world and are important plants in terms
of therapeutic uses and economic values.
In 1973, a wild Panax species was discovered at the elevation of 1,800 m above sea
level of Ngoc Linh Mount in Middle Vietnam. The plant used to be a secrete tonic and
body-strengthening ethno-medicine of the Sedang ethnic group living in high mountains
of the Truong Son Range. In 1985, it was defined as a new Panax species with the scientific
name Panax vietnamensis Ha et Grushv, Araliace family, and is now commonly known as
Vietnamese ginseng (VG) which is used for many indications similar to those of Panax
ginseng (PG), such as enhancement for physical strength, tonic, lowering blood cholesterol,
preventing cardiovascular diseases etc.
Since then, scientific studies of VG on botany, cultivation, chemistry, bio-activities,
etc., have been done. The result showed that VG contains a characteristic saponin
composition, which includes not only known dammarane saponins found in PG such as
ginsenoside-Rb1, -Rb3, -Rg1, -Rd, -Re, etc., but also ocotillol saponins in high yield,
especially majonoside-R2 (more than 5%). Twenty-five (25) new dammarane saponins named
vina-ginesnnosides-R1-R25 from the underground part and 8 named vina-ginsenosides-L1-L8
from the leaves were also isolated and identified. The underground part of VG contains
up to 15-20% saponins, which is the highest content compared with that of PG (4-6%)
and other Panax spp. As for pharmacological activities, VG showed similar effects
with those of PG, including tonic, dose-dependent stimulation/depression on CNS, physical
strength enhancement, analeptic, antifatigue, adaptogenic, androgenic, anti-tumorigenic
etc. VG also showed remarkable physical and psychological anti-stress activities.
Results of scientific studies have proven that VC is a trustful herbal medicine. It
has therefore become an important medicinal plant of Vietnam in terms of theuraputic
uses and economic value. Recently, the Vietnam government defined VG as an important
national product. A national program was set up to protect the wild plant and the
biodiversity of its native areas, and to develop the large-scale cultivation of VG.
An updated review on VG will be reported to show how the used-to-be ethno-herb VG
becomes an national profduct and its impact to the contemporary Vietnam medicine.
Keywords: Vietnamese ginseng, Panax vietnamensis, ethno-medicine, Vietnam national
product
PL3 Gene-Chemical Interplay in Alzheimer’s Disease
Abu Bakar Abdul Majeed
Brain Research Laboratory, Faculty of Pharmacy, Universiti Teknologi MARA Selangor,
42300 Puncak Alam, Malaysia
Correspondence: Abu Bakar Abdul Majeed (abubakar@uitm.edu.my)
Alzheimer’s disease (AD) is a neurodegenerative disease that debilitates numerous
human psycho-behavioural functions, notably memory processing. In the developed world
AD is considered as one of the major causes of death. In the developing world, the
number of people living with AD (PLWAD) is expected to rise significantly in the coming
decades. Though AD is more prevalent among the elderlies over 65 years old, cases
of early onset AD are also widely known. Both types of AD are linked to genes. Much
research is ongoing to elucidate the exact pathophysiology of AD, hence leading to
its ultimate cure. Chemicals whether working in synchrony or otherwise, are known
to be responsible for the preservation or destruction of the brain function, respectively.
Firstly, putative neurotransmitters in normal brain physiology related to AD include acetylcholine,
dopamine, serotonin, noradrenaline, aspartate and GABA. Secondly, chemicals that precede
the pathology of AD. Among them are the pro inflammatory mediators, the levels of
which are constantly checked by anti-inflammatory mediators. Thirdly, the group of
chemicals found to play an important role in AD is the pathological proteins. Among
them are beta-amyloid, hyperphosphorylated tau and alpha-synuclein. The formation
of these proteins leads to the neuronal dysfunction that contributes to the psycho-physical
disability of PLWAD. At the heart of the chemical homeostasis or imbalance are the
genes. Six genes identified in a Malaysian cohort of PLWAD will be highlighted. The
over- or under-expression of these genes tilts the chemical homeostasis, which ultimately
promotes the manifestation of symptoms of AD.
INVITED LECTURE
IL1 Developing proposed national competency framework for pharmacists in Vietnam
Dinh Thi Thanh Hai
Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hoan kiem, Hanoi, Vietnam
Correspondence: Dinh Thi Thanh Hai (haidtt@hup.edu.vn)
Background
In recent years, the number of pharmaceutical human resource training institutions
has been increasing (28 establishments) including public and non-public establishments.
However, the training program, facilities, quality of teaching staff, quality of students'
inputs and especially the way of implementing training programs, training organization
capacity of each institution is different, so the quality of output products, quality
of practice is also different. Therefore, it is necessary to have basic competency
standards for pharmacists in Vietnam. On the other hand, in the face of extensive
regional and international integration needs, managers and employers need to have
a set of tools to control, evaluate and standardize the quality of human resources.
Recognizing that reality, the Ministry of Health has directed the construction of
the Basic Competence Standard for Pharmacists in Vietnam with the participation of
all stakeholders including experts in the field of training, employers, Employers,
managers, professionals, social organizations. In the process of construction, the
Drafting Board has consulted the standard of competencies of pharmacists in the region
and the world to adjust to suit the situation in Vietnam.
Therefore, this study was carried out to develop a basic competency framework for
pharmacist in Vietnam.
Method
The study was conducted by a method of retrospective and cross-sectional descriptions,
combining qualitative research (method of in-depth interview; group discussion) and
quantitative research based on FIP and Thailand pharmacist competency standards. The
data is processed on SPSS software.
Results
A basic competency framework was developed for pharmacist in Vietnam. 98 competencies
required for pharmacist, organised into 24 standards, 7 domains: professional and
ethical practice, communication and collaboration, organisation and management, quality
assurance of pharmaceutical, prepare pharmaceutical products, supply of medicines,
safe and rational use of medicines.
Conclusion
The proposed competency framework of pharmacist in Vietnam provides a solid foundation
for both pharmacy training and curriculum development and is based on several rounds
of scientific research. The proposed competency framework may help understand the
pharmacist role and how to best prepare for the Practice of Pharmacy and many added
values for stakeholders.
IL2 Vietnam pharmaceutical industry: Actual status and perspectives for decade 2020-2030
Le Van Truyen
Faculty of Pharmacy, Hanoi Business and Technology University, House no.29A, Gate
124, Vinh Tuy Street, Vinh Tuy Ward, Hai Ba Trung Dist, Hanoi, Vietnam
Correspondence: Le Van Truyen (levantruyen@gmail.com)
The presentation described an overall outlook on the actual status of Vietnam pharmaceutical
industry, which is considered as one of the fastest developing sectors among the emerging
countries in pharma-industries. The Vietnam general and healthcare indicators were
presented and analysed. The presentation also gave a SWOT analysis of the Vietnam
pharmaceutical industry. The perspectives of Vietnam pharmaceutical industry for decade
2020-2030 were analysed, based on the policies and strategies determined relevant
to the resolutions of the Government of Vietnam especially in New Drug Law 2016. The
factors impacting into the process of modernization of Vietnam pharmaceutical industry
were discussed and suggested for realization of the objectives of the Vietnam pharmaceutical
industry development in the context of deeper participation of the nation in the process
of economic globalization in ASEAN and the world.
IL3 Phytochemicals: a new insight into regenerative medicine
Rajesh Ramasamy, Ramesh Renggasamy, Hamza Lawal and Johnson Stanslas
Immunology Unit, Department of Pathology, Faculty of Medicine and Health Sciences,
Universiti Putra Malaysia, 43400 UPM Serdang, Selangor, Malaysia
Correspondence: Rajesh Ramasamy (rajesh@upm.edu.my)
Targetting the impairment of stem cells in disease models and conditions become a
primary target of the modern therapeutic approaches. Stem cells sit at the top of
the cellular hierarchy, maintain the structure and homeostasis of an organ by uninterrupted
tissue-specific cells’ supply. Besides, the ageing and diseases processes affect stem
cells, many chronic diseases such as cancers, diabetes and other organ-related diseases
are consequent of functional impairment of stem cells. Phytochemicals, whose therapeutic
activities are not only limited to the somatic cells but showcasing a profound impact
on stem cells too. To date, not much research data are available regarding the effect
of phytochemicals on stem cells. Amongst, Moringa oleifera, a local plant, has exhibited
a profound impact on adult mesenchymal stem cells (MSCs). Mesenchymal stem cells are
found mainly in the bone marrow, which promote haematopoiesis, alleviate inflammation
and mediate tissue repair. In line with this, the ethanol extract of Moringa oleifera
(MOEE) boosted the proliferation of human MSCs. The enhanced proliferation activity
of MSCs was due to an intensification of the cell cycle with reduced apoptosis. The
treatment of MOEE altered the cytokine secretory profile of MSCs depicting anti-inflammation
with enhanced expression of growth factors that mediate tissue repair. Similarly,
various administrations of MOEE in a rat model of immunosuppression showed reconstitution
of immune cells by preserving the bone marrow-derived haematopoietic stem cells (HSCs)
and MSCs. The phytochemicals from MOEE showed a promising way of recovering immune
cells and immunity in degenerative diseases. However, the identification and isolating
specific compound/s to accelerate the desired therapeutical properties and challenges
of diversified actions in a multiorgan system need to be addressed prior to clinical
applications.
IL5 Role of Microbial-Catalysed Biotransformation In Sustainable Medicinal Chemistry
Sadia Sultan1,2
1Department of Pharmaceutical Pharmacology and Chemistry, Faculty of Pharmacy, Universiti
Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, 42300 Selangor, Malaysia;
2Atta-ur-Rahman Institute for Natural Product Discovery (AuRins), Universiti Teknologi
MARA, Puncak Alam Campus, Bandar Puncak Alam, 42300 Selangor, Malaysia.
Correspondence: Sadia Sultan (drsadia@uitm.edu.my), (sadiasultan301@yahoo.com)
Background
Over the past few years there has been an upsurge interest from medicinal chemistry
groups in embracing the philosophy and tools of green chemistry. This philosophy is
in part a driver to move towards more sustainable practices, but there is also an
interest in using emerging new technologies to speed up the drug discovery process
and to discover new and diverse structures as scaffolds and lead compounds. Microbial-catalysed
biotransformation plays an important role in the production of commercially valuable
steroids and terpenes for therapeutic use by the pharmaceutical industry with the
advantage of high stereo- and region-selectivity, which additionally fulfils green
chemistry principles.
Methods
Different bioactive natural products have been exposed to the microbial bio-catalysis
as an attempt to find further lively and fewer toxic products. Initially screening
of selected steroids and terpenes were performed with different fungi. Preparative
scale started upon detection of biotransformed products. Resulted metabolites were
isolated and elucidated using HPLC, LC-MS, ID and 2D NMR spectroscopic techniques.
Resulted metabolites were screened for bioassays including anti-inflammatory, α-glucosidase
inhibitory, tyrosinase inhibitory, acetylcholinesterase inhibitory and antiproliferative
assays, respectively. The binding interactions of compounds were studied by molecular
docking studies.
Results
Novel products were obtained during biotransformation of multifunctional steroid and
terpenoid drugs with growing cultures of fungi from different biotopes. Some of the
products showed more than or comparable activities to the standard inhibitors.
Conclusions
Hence, the identification of these novel compounds opens the possibility of producing
more promising pharmaceutical agents with potential bioactivities with lesser side
effects than the existing drugs.
Keywords: Biotransformation, Steroids, Terpenes
IL6 Preclinical studies of Carica papaya against DEN-2 dengue infection
Mohd Ridzuan1, Adlin Afzan1, Noor Rain Abdullah1, Ami Fazlin Syed Mohamed1
1Herbal Medicine Research Center, Institute for Medical Research, Level 5, Block C6, National
Institutes of Health Complex, No 1, Jalan Setia Murni U13/52, Section U13, 40170 Setia
Alam, Selangor, Malaysia
Correspondence: Ami Fazlin Syed Mohamed (ami@imr.gov.my)
Background
Dengue is still a major problem in Malaysia and causing high mortality. There is no
specific treatment for dengue and one of the strategy is to study the effect of herbal
medication on dengue. The aim is to review the results of the series of preclinical
studies that has been conducted for Carica papaya in treating dengue fever.
Methods
Several preclinical studies were conducted namely the phytochemical, efficacy and
toxicity studies. Phytochemistry studies were conducted on water extract of C.papaya
with chromatography and spectrometry analysis. The in vitro plaque assay and the in
vivo studies on AG129 mice were conducted with non-mouse adapted Malaysian dengue
virus type 2 (DEN-2) infection. The mouse model of DENV-infection that closely mimicked
the human disease was established and used to study the immunomodulatory activity
involving specific cytokines, the endothelial cell biology in dengue infection and
the effect of dosing on the day of infection. The genotoxicity and general toxicology
studies were also conducted.
Results
The phytochemistry studies allowed confirmation of the herb identity and consistency
of the chemical composition for efficacy and toxicity studies. Plaque assay and the
in vivo studies have confirmed that the extract of C. papaya do not kill the dengue
virus. The extract affected the immunomodulatory system and the endothelial cells
of the blood vessels. These provide clues to the control of the cytokine ‘storm’ and
the vascular leakage that is the characteristic of dengue haemorrhagic fever. A previous
study has confirmed that C. papaya juice increases the platelet by inducing the platelet
production in the bone marrow. The results of the toxicity studies were also favourable.
Conclusions
The preclinical studies has provided evidence that C. papaya extract worked on different
pathogenesis of dengue fever and can be further studied in a clinical trial.
Keywords: preclinical, herbal, Carica papaya, dengue
ORAL PRESENTATION
OPT1 The study on ORF239342, a protein isolated from the mushroom
Agaricus bisporus as a potent pharmaceutical biomolecule
Heni Rachmawati1, Diana Diana1, Najwa Nabila1, Sophi Damayanti1, Olivia M. Tandrasasmita2,
Raymond R. Tjandrawinata2, Wangsa T. Ismaya2
1School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung 40132, Indonesia;
2Dexa Laboratories of Biomolecular Science, Industri Selatan V PP-7, Jababeka II Industrial
Estate, Cikarang 17550, Indonesia
Correspondence: Heni Rachmawati (h_rachmawati@fa.itb.ac.id)
Background
Drug absorption becomes constrained when the permeability is low leading to limited
bioavailability. The use of lectin for glycotargeting is an approach to overcome problems
in the delivery of compounds with low permeability. Interaction between lectin with
several types of oligosaccharides present in cells on the surface of gastrointestinal
wall could facilitate the lectin to be absorbed. Vast glycosylated areas within gastrointestinal
tracts can be targeted for this purpose. LSMT (light chain subunit in the tetramer
complex of tyrosinase enzyme Agaricus bisporus) has the ability to recognize a specific
group of sugar moieties, non-toxic, and nonimmunogenic. Formation of LSMT-drug bioconjugate
was explored in this study to assess the ability of LSMT as a drug carrier using captopril
as a drug model.
Methods
Prior to permeability study, solvent accessibility of cysteine residue (functional
target candidate for bioconjugation) using ASAView and NetSurfP programs was conducted.
In vitro accessibility of cystein was performed to determine free sulfhydryl using
DTNB reagent. Conjugation was performed using different conditions of reaction, then
characterized.
Results
Lysine is chosen as an active side of the reaction. Conjugate is formed with SMPT
as a linker utilizing a reduced disulphide bond to release the drug. Optimum conditions
currently found for conjugate formation was at 4°C for 24 hours for protein activation
stage with SMPT and 48 hours for captopril binding stage with ratio of protein:SMPT
= 1:10 and activated protein:captopril = 1:100. Conjugate substitution obtained under
these conditions was between 1-2 mol of captopril per mole of LSMT. Conjugate formed
was stable in simulated gastric and intestinal solutions. Furthermore, preliminary
in vitro permeability study using Caco2 cells and ex vivo with non-everted gut sac
method showed intact ability of LSMT to penetrate gastrointestinal wall.
Conclusions
LSMT is a promising biomolecule for a drug carrier to improve per oral boavailability.
Keywords: Light subunit mushroom tyrosinase, recombinant protein, Agaricus bisporus,
drug delivery
OPT2 Formulation design and characterization of self nano emulsifying drug delivery
system (SNEDDS) roxitromycin using capryol–90, polysorbat–80 and PEG–400
Mardiyanto Mardiyanto, Najma Annuria Fithri, Duha Inda Misdwima
1 Department of Pharmacy Faculty of Science Sriwijaya University, Kampus UNSRI Indralaya
JL Raya Palembang-Prabumulih KM32 South Sumatra, 30162, Indonesia
Correspondence: Mardiyanto Mardiyanto (mardiyantoUNSRI@gmail.com)
Background
Roxithromycin is a macrolide antibiotic included in the biopharmaceutics classification
system (BCS) class II with poor water solubility (0.0189 mg/mL) resulting poor solubility
of roxithromycin in gastrointestinal track and decreases bioavailability. Technology
development of self nano emulsifying drug delivery system (SNEDDS) to reduce particle
size has known effectively for increasing drug solubility.
Methods
An optimum formulation of this reseach were determined by simplex lattice design method
in Design Expert®10. Investigated factors were solubility of roxithromycin in capryol-90
and in mixture of polysorbat-80 and PEG-400 also the ternary phase of capryol-90:polysorbat-80:PEG-400.
The emulsification system was performed by ultrasonication. The characters of SNEDS
were determined by dynamic light scattering and transmission electron microscopy.
The thermodynamic stability test was performed by heating-cooling cycle.
Results
Capryol–90 could dissolve roxithromycin properly (2.355±0.040 mg/mL). Polysorbate–80,
and PEG–400 also could increase the solubility of roxithromycin in water. Determination
of ternary phase diagram to obtain combination proportions formed a spontaneous range
of 10 - 60% capryol–90, 20 - 50% polysorbate–80, and 10 - 70% PEG–400. Proportion
of optimum roxithromycin SNEDDS formula obtained from simplex lattice® design was
resulted 20.00% capryol–90, 60.00% polysorbate–80, and 20.00% PEG–400. Characterization
of optimum formula resulted percent of transmittance (80.60 ± 0.35)%, emulsification
time (71.70 ± 0.99) second, viscosity (3.76 ± 0.02) cP, pH (7.84 ± 0.07), and robustness
to dilution in aquadest, SGF, and SIF (99.16 ± 0.67)%, (93.23 ± 0.14)%, and (98.34
± 0.34)%. Dissolution test showed that SNEDDS could improve dissolution of roxithromycin
in SIF pH 7.4 compared to pure and generic tablet.
Conclusions
Proportion of optimum roxithromycin SNEDDS was resulted 20.00% capryol–90, 60.00%
polysorbate–80, and 20.00% PEG–400. Dissolution profile showed that SNEDDS could improve
dissolution of roxithromycin in SIF pH 7.4 compared to pure and generic tablet.
Keywords: Formulation-design, roxithromycin, characterization, SNEDDS
OPT3 Hyaluronic Acid Coated Chitosan-Latanoprost-Link Nanoparticle for Prolonged Ocular
Drug Delivery
Ana Marie L. Rubenicia1, Agnes L. Castillo2, Dr. Oliver B. Villaflores2
1 Graduate School, University of Santo Tomas, Espańa, Manila, 1008 and School of Pharmacy,
Centro Escolar University, Mendiola, Manila, 1008, Philippines; 2 Faculty of Pharmacy,
Research Center for Natural and Applied Sciences, University of Santo Tomas, Espańa,
Manila, 1008, Philippines
Correspondence: Ana Marie L. Rubenicia (arubenicia@ceu.edu.ph)
Background
The major problem with conventional eye drops is the assurance of optimum drug concentration
to the target site, due to pre-corneal and nasal drug elimination, as well as barriers
of the eye impeding drug access. The use of nanomeric drug delivery systems with mucoadhesive
properties may enhance drug residence time to the active site, thus providing better
ocular availability, as well as improved tolerability of the formulation. In this
study, latanoprost molecules was linked to mucoadhesive nanocarrier, chitosan (CS)
and hyaluronic acid (HA) that can control the drug release and prolong residence time
in ocular tissues.
Methods
The methods that was used for physical and chemical characterizations were: (1) electron
microscopy (2) the dynamic light-scattering method (DLS); (3) Cup and Bob viscometry
(4) infrared spectroscopy and (5) high performance liquid chromatography. Draize test
was performed to determine the safety of the polymeric nanoparticle.
Results
The optimum CS: TPP ratio had the lowest particle size of 198 nm, with PDI of 0.274,
ZP of +27.7mV and an entrapment efficiency (EE) of 62%. It was further coated with
HA, where the optimum HA: CS ratio had the lowest particle size of 314 nm, with a
PDI of 0.424, ZP of +29.87 mV and an EE of 72%. In the in vitro drug release study,
the optimum HA coated CS-latanoprost link nanoparticle formulation has 0% drug release
in 30 minutes, 29% in 2 hours and 87% in 8 hours as compared with the conventional
latanoprost solution that released 28% of the drug in 30 minutes, and 100% in 2 hours.
Release mechanism of the drug from the polymeric nanoparticles matrix led to a zero
order kinetic with a correlation coefficient of 0.9848. Drug release could also be
expressed by Higuchi’s equation as the plot showed linearity at 0.9492, where the
value of diffusion exponent obtained from the Korsemeyer-Peppas model is 1.13. Addition
of mucin to the positively charged nanoparticles reduced the ZP to an average of -4.30
mV. The draize test on albino rabbits showed the polymeric nanoparticle were safe
for ophthalmic use.
Conclusion
The results of this study could serve as a basis that mucoadhesive HA coated CS-latanoprost-link
nanoparticles could provide a prolonged ocular delivery system of latanoprost for
better glaucoma treatment.
Keywords: latanoprost, chitosan, hyaluronic acid, nanoparticles, prolonged drug delivery
OPP1 Synthesis, characterization, and biological activities of Schiff bases and their
iron and zinc metal complexes
Bushra Naureen1, G.A. Miana2, Khadija Shahid2, M.A. Bhatti3, Samreen Tanveer4
1Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur,
Malaysia; 2Riphah Institute of Pharmaceutical Sciences, Riphah International University,
44000 Islamabad, Pakistan; 3Department of Restorative Dentistry, Faculty of Dentistry,
University of Malaya, 50603 Kuala Lumpur, Malaysia; 4Department of Pharmaceutical
Sciences, Superior University, 55150 Lahore, Pakistan
Correspondence: Khadija Shahid (khadijajee@yahoo.com), Bushra Naureen (bushranauren@gmail.com)
Background
Schiff bases, being active biological moieties, possess diverse pharmacological activities.
Metal ions play vital role in various functions of human body, and diseases may occur
due to metal ion deficiencies. The importance of metal complexes of Schiff bases has
been acknowledged in the field of biomedical sciences.
Methods
Herein, two Schiff base ligands (L1, L2) underwent metal complex formation, to produce
their iron and zinc metal complexes, respectively. Original ligands and their metal
complexes were characterized physically as well as by means of spectral characterization
techniques such as Infra-red spectroscopy (IR), nuclear magnetic resonance spectroscopy
(NMR) and mass spectrometry. Pharmacological perspectives of these Schiff base ligands
and their iron and zinc metal complexes such as antibacterial, antifungal and antioxidant
assays were assessed.
Results
All compounds exhibited antibacterial and antifungal activities, but the metal complexes
showed better activities in comparison to the original ligands, especially all zinc
complexes. Zinc complex (L2)2Zn(Ac)2 elicited good antibacterial activity against
all gram positive and gram negative bacterial strains and exceptional activity against
Candida albican strain. Overall, all the compounds showed better antifungal activity
against Candida albican as compared to Candida glabrata. Free ligands illustrated
better antioxidant behaviour as compared to the metal complexes.
Conclusions
These results suggest that all the ligands and metal complexes, being active in one
way or the other, have the potential to be employed as antibacterial, antifungal and
antioxidant agents.
Keywords: Schiff base, Metal complex, Antibacterial, Antifungal, Antioxidant
OPP2 Possible drug-herb interactions between Merunggai (Moringa oleifera) and selected
antihypertensive drugs
Malina Jasamai 1, Endang Kumolosasi 1, Adyani Md Redzuan 2
1 Drugs & Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia,
Jalan Raja Muda Abdul Aziz, 50300, Kuala Lumpur, Malaysia; 2 Faculty of Pharmacy,
Universiti Kebangsaan Malaysia, Malaysia
Correspondence: Malina Jasamai (malina@ukm.edu.my)
Background
Herbal medicines have been widely used in Malaysia for cardiovascular pharmacotherapy.
This is alarming as little is known about drug-herb interactions of conventional cardiovascular
drugs with most Malaysian herbs. Moringa oleifera is a medicinal plant with high nutritional
values and was reported to possess blood pressure (BP) lowering effect. Hypertension
has become a significant health issue globally and is treated with four main classes
of drugs namely; angiotensin converting enzyme inhibitors (ACEIs), angiotensin receptor
blockers (ARBs), β-blockers and calcium channel blockers. This study aimed to investigate
any possible drug-herb interactions between the aqueous leaves extract of M. oleifera
and selected antihypertensive drugs in normotensive rats (NTs) and spontaneously hypertensive
rats (SHRs).
Methods
The study consists of ten groups of SHRs and one group of NTs. The rats were given
either drugs alone or drugs in combination with M. oleifera extract for 14 days. There
were also control groups. Systolic and diastolic blood pressure of the rats were measured
on day 1 prior to the treatment and on day 15.
Results
All treatment groups were found to produce significant blood pressure reduction on
day 15 when compared with negative control but there was no significance difference
when compared with positive controls. Combination of drugs and extract significantly
reduced BP but are comparable with the use of drugs alone.
Conclusions
There is a possibility of drug-herb interaction between M. oleifera and the selected
antihypertensive drugs. Detailed mechanism of actions on how these interactions occur
are worth to be investigated further to ensure the safety of M. oleifera usage in
combination with antihypertensive drugs.
Keywords:
Moringa oleifera; angiotensin converting enzyme inhibitors; angiotensin receptor blockers;
β-blockers; calcium channel blockers
OPP4 Effect of Gynura procumbens and Christia vespertilionis extracts on cell adhesion
molecules in human umbilical vein endothelial cells
Tan Jiah Ning1, Zakiah Jubri2, Khairana Husain1, Ibrahim Jantan3, Fhataheya Buang1,
Azizah Binti Ugusman4, Mohd Faizal Ahmad5, Ani Amelia Zainuddin5, Norsyahida Mohd
Fauzi1
1Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia,
Jalan Raja Muda Abdul Aziz, 50300 Kuala Lumpur, Malaysia; 2Department of Biochemistry,
Faculty of Medicine, The National University of Malaysia Medical Centre (UKMMC), Malaysia;
3School of Pharmacy, Taylor’s University, Lakeside Campus, 47500 Subang Jaya, Selangor,
Malaysia; 4Department of Physiology, National University of Malaysia Medical Centre,
Kuala Lumpur, Malaysia; 5Obstetrics and Gynecology, National University of Malaysia
(UKM), UKMMC, Jalan Yacob Latiff, 56000 Cheras, Kuala Lumpur, Malaysia
Correspondence: Norsyahida Mohd Fauzi (drnorsyahida@ukm.edu.my)
Background
The initiation of atherosclerotic lesion involves endothelial cell pro-inflammatory
state that recruits leukocytes and promotes their movement across endothelium which
requiring endothelial expression of cell adhesion molecules. Gynura procumbens (GP)
and Christia vespertilionis (CV) are herbaceous plants that are traditionally used
for treatment of various inflammation-related ailments. However, there is limited
evidence that points to the protective activity of these plants against inflammation
that occurs in atherosclerosis. In this study, we sought to explore the inhibitory
effect of GP and CV extracts on TNF-α-induced vascular cell adhesion molecule-1 (VCAM-1)
expression and its underlying mechanism.
Methods
Cell viability of HUVEC treated with GP or CV extracts was determined by MTT assay
while protein expression of adhesion molecules and cellular signaling molecules were
determined by Western blot.
Results
GP or CV extracts at concentration ranging from 5 μg/mL to 60 μg/mL were found to
maintain more than 80% cell viability following 24 hours treatment. Selected treatment
concentrations (20, 40 and 60 μg/mL) of CV extract showed no effect on TNF-α-induced
VCAM-1 expression in HUVEC. On the other hand, pretreatment of 60 μg/mL GP extract
demonstrated a significant inhibition on TNF-α-induced VCAM-1 protein expression in
HUVEC (p<0.005). Pretreatment of 60 μg/mL GP extract also showed a dose-dependent
suppression on IKKα/β phosphorylation and significant inhibitory effect (p<0.05) on
protein expression of phosphorylated NFκB.
Conclusions
Results from this study demonstrated that CV extract may not have inhibitory effect
on expression of adhesion molecules but GP extract showed inhibitory effect on VCAM-1
expression by suppressing NFκB signaling pathway. This results implicate that GP extact
may have beneficial use particularly in vascular inflammation.
Keywords:
Gynura procumbens; Christia vespertilionis; vascular cell adhesion molecule; NFκB;
endothelial cells
OPP5 Optimization of solvent extraction method in recovery of testosterone and 6β-hydroxytestosterone
from cell culture media and protein depletion of sample for in vitro CYP3A4 mediated
6β-hydroxylation assay
Mohamad Jemain Mohamad Ridhwan 1, Nurliana Abdul Mutalib 2, Nor Hadiani Ismail1, Normala
Abd Latip2
1Faculty of Applied Sciences, Universiti Teknologi MARA (UiTM), 40450 Shah Alam, Selangor,
Malaysia; 2Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak
Alam, Selangor, Malaysia
Correspondence: Normala Abd Latip (drnormala6351@.uitm.edu.my)
Background
Accurate measurement of testosterone and 6β-hydroxytestosterone is important for in
vitro CYP3A4 mediated 6β-hydroxylation assay. To increase accuracy of measurement,
maximum recovery of analytes from cell culture media must be achieved. Apart from
recovery of analyte, protein depletion of cell culture media is also an important
step before UHPLC quantification to avoid column clogging. The aim of this study is
to investigate optimum solvent extraction method of testosterone and 6β-hydroxytestosterone
from culture media and to determine protein depletion efficiency of the solvent extraction
method.
Methods
Media collected from WRL68 (normal liver cell line) culture was spiked with 20 μM
testosterone and 10 μM 6β-hydroxytestosterone. The analytes were extracted using centrifugation
at 15000 rpm for 20 minutes with different solvent including acetone, acetonitrile,
methanol, ethyl acetate and dichloromethane and were analysed quantitatively using
UHPLC. The protein content in the extracts were determined using Bicinchoninic Acid
protein assay. UHPLC analysis method was optimized for analytes quantification.
Results
The methanol extraction method resulted in the highest percentage of recovery (98.3
% for testosterone and 98.4 % for 6β-hydroxytestosterone) with moderate protein depletion
(79.95 ± 1.87 %). The ethyl acetate extraction method resulted in the highest protein
depletion at 98.8 %, however, the percentage of recovery of analytes is lower than
that of methanol extraction method.
Conclusions
As a conclusion, methanol was found to be the most optimum solvent for extraction
of testosterone and 6β-hydroxytestosterone from cell culture media compared to other
solvents used and the amount of protein left in sample did not interrupt UHPLC analysis.
Keywords: Testosterone, 6β-hydroxytestosterone, UHPLC, metabolism, solvent extraction
OPP6 Phytoestrogens induced apoptosis and phagocytosis through modulation of annexin
A1 in leukemic cell lines
Endang Kumolosasi1, Affidah Sabran1, Masyitah Hasan1, Jamia Azdina Jamal1, Malina
Jasamai1, Norazrina Azmi1, Ibrahim Jantan2, Nor Fadilah Rajab3
1Drug and Herbal Research Centre, Faculty of Pharmacy, Universiti Kebangsaan Malaysia,
Kuala Lumpur, Malaysia; 2School of Pharmacy, Taylor’s University, Lakeside Campus,
47500 Subang Jaya, Selangor, Malaysia; 3Biomedical Science Programme, School of Diagnostic
& Applied Health Sciences, Faculty of Health Sciences, Universiti Kebangsaan Malaysia,
Kuala Lumpur, Malaysia
Correspondence: Endang Kumolosasi (e_kumolosasi@ukm.edu.my)
Background
Phytoestrogens is a non-steroid plant compound that has structurally similar to estrogen
which posses’ anti-cancer properties. Phytoestrogens have the ability to induce apoptosis,
cell cycle arrest and phagocytosis and reducing Annexin A1 in leukemic cell lines.
However, the underlying mechanism of phytoestrogens in inducing cell death is still
not fully understood. The present study aimed to investigate the effects of phytoestrogens
in inducing of cell death is through decreasing ANXA1 level or independently.
Methods
Leukemic cells and ANXA1-knockdown leukemic cells were incubated with estrogen and
phytoestrogens 40 μg/ml for 24 hrs at 37oC. Cells viability were examined by MTT assay
and ANXA1 quantification via ELISA Assay. Apoptosis were examined by flow cytometer
and phagocytosis were evaluated by haematoxylin-eosin staining. Transfection of ANXA1
siRNA was conducted to down-regulate ANXA1 expression.
Results
In Leukemic cells, coumestrol significantly (P<0.05) reduced the total level of ANXA1
in both K562 and U937 cells. Genistein induced a significant (P<0.05) reduction in
the total level of ANXA1 in K562, Jurkat and U937. Estradiol and daidzein induced
similar reduction in U937 and Jurkat cells. Coumestrol and daidzein induced apoptosis
in K562 and Jurkat cells, while genistein and estradiol induced apoptosis in all tested
cells. Coumestrol, genistein and estradiol induced phagocytosis in all cells but daidzein
induced significant (P<0.05) phagocytosis in K562 and Jurkat cells only. In ANXA1
knockdown leukemic cells, the expression of ANXA1 was significantly downregulated
in all cell lines. Genistein significantly induced apoptosis (p<0.001) only in Jurkat
cell, contrary coumestrol and deidzein did not induce apoptosis in all the cell lines
tested. The percentage of phagocytosis and phagocytosis index increased significantly
after treatment with phytoestrogens in all cell lines.
Conclusions
Induction of apoptosis and phagocytosis by phytoestrogens are mediated through decreasing
of annexin A1 expression.
Keywords: Phytoestrogens, Annexin A1, Apoptosis, Phagocytosis, Leukemia
This study was funded by a grant from Universiti Kebangsaan Malaysia (GUP-2018-044).
OPL1 Atheroprotection by antilipidaemic Pediococcus pentosaceus LAB6- and Lactobacillus
plantarum LAB12-fermented cell free supernatant in vitro
Nur Syakila Rohawi1,2, Siong Meng Lim1,2, Hasseri Halim1, Kalavathy Ramasamy1,2
1Faculty of Pharmacy, University Teknologi MARA (UiTM), Cawangan Selangor, Kampus
Puncak Alam, 42300 Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia; 2Collaborative
Drug Discovery Research (CDDR) Group, Pharmaceutical and Life Science Community of
Research, Universiti Teknologi MARA Shah Alam, 40450 Shah Alam, Selangor Darul Ehsan,
Malaysia
Correspondence: Kalavathy Ramasamy (kalav922@gmail.com)
Background
Current treatments against atherosclerosis rely predominantly on lipid lowering in
combination with anti-inflammatory therapies. However, the maximum efficacy of these
treatment strategies appears to be rather modest, often compromised by the lack of
response by high risk patients and adverse effects. There is a need for alternative
approaches that can manage atherosclerosis more effectively. Recent evidence raises
the possibility of using antilipidaemic probiotics for atheroprotection. Nevertheless,
the beneficial effects of probiotics are believed to be strain-dependent. We had identified
unique probiotic lactic acid bacteria (LAB) (i.e. Pediococcus pentosaceus LAB6 and
Lactobacillus plantarum LAB12) with promising cholesterol lowering effects. Capitalising
on this beneficial property, the present study aimed to investigate the atheroprotective
potential of LAB6 and LAB12 in vitro.
Methods
The sub-toxic concentration of 24 h LAB-fermented cell free supernatant (CFS) against
RAW264.7 was determined using the sulforhodamine assay. Sub-toxic CFS was added to
oxLDL-induced foam cell for 24 h before staining with Oil Red O stain. For semi-quantitative
analysis, images captured under light microscopy were analysed for differential intensity
using ImageJ. For quantitative analysis, isopropanol was added, and absorbance was
measured at 540 nm using a spectrophotometer. The effect of CSF against oxLDL-induced
mitochondrial dysfunction was assessed by using the mitochondrial membrane potential
assay.
Results
The highest sub-toxic concentration (IC15) of LAB6- and LAB12-derived CFS against
RAW264.7 were 7 % and 5.6 %, respectively. Subtoxic LAB6- and LAB12-derived CFS significantly
(p<0.05) reduced lipid uptake in oxLDL-induced foam cells by at least 47.06% and 47.12%,
respectively. LAB-derived CFS also prevented oxLDL-induced mitochondrial dysfunction
(early apoptosis) by increasing red (aggregate)/green (monomer) ratio of JC-1 fluorescence
by ≤ 4.
Conclusion
The present findings strongly implied the atheroprotective potential of LAB6- and
LAB12-derived CFS against foam cell formation in the event of atherosclerosis. This
in turn warrants further investigations using in vivo model.
Keywords: Probiotics, cholesterol lowering, HPTLC, atheroprotective
OPL2 Use of xylazine hydrochloride–ketamine hydrochloride for immobilization of captive
large felines in Malaysia: a 15-year retrospective study (1988-2003)
Vellayan Subramaniam and Nur Zahirah Zakaria
Department of Pharmacology and Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Vellayan Subramaniam (vellayan@uitm.edu.my)
Background
Chemical immobilisation by anaesthesia with xylazine hydrochloride (XZH) - ketamine
hydrochloride (KTH) has been widely used in large felines. This study was aimed to
determine the relationship between time of effect and effect of anaesthesia with XZH-KTH.
Methods
Data were retrieved from existing anaesthesia records from different zoos in Malaysia
from 1988 to 2003. A total of 66 large felines belonging to 5 different species namely,
Malayan Tiger (Panthera tigris jacksoni) (n = 4), Bengal Tiger (P. tigris tigris)
(n = 10), African Lion (P. leo) (n = 12), Sumatran Tiger (P. tigris sumatrae) (n =
17) and Gir Lion (P. leo persica) (n = 23) were involved in this study. All the large
felines were successfully anaesthetised using XZH-KTH. The effects of variables such
as body weight, sex, health status, demeanour and fasting time on dose selection were
evaluated. The relationship of dose with effect of anaesthesia and time of effect
were also studied.
Results
The results showed that the effect of anaesthesia and time of effect had no significant
correlation with dose. Among the variables studied, only weight had significant (p
= 0.016 and p = 0.002) effect on dose. When an average dose (KTH = 363.33 mg; XZH
= 185.98 mg) was given to the felines, it gave a weak positive correlation with time
of effect (rketamine = 0.220; rxylazine = 0.324). Similar findings were observed for
the effect of anaesthesia (rketamine = 0.156; rxylazine = 0.227).
Conclusions
Although the time of effect and effect of anaesthesia were independent of the dose,
it is important to determine the weight of the large felines so that the drug administered
were sufficient enough to produce the desired anaesthetic effect.
Keywords: ketamine, xylazine, large felines, dose selection.
OPC1 Development of simultaneous analysis method for determining level of losartan
potassium and hydroclorotiazid in tablets using high performance liquid chromatography
(HPLC)
Sophi Damayanti, Mia Savira, Benny Permana
School of Pharmacy ITB, Ganesha 10 Bandung, 40132, Indonesia
Correspondence: Sophi Damayanti (sophi.damayanti@fa.itb.ac.id)
Background
Losartan potassium and hydrochlorothiazide are combination of antihypertension drugs
from group of angiotensin II receptor blocker (ARB) and diuretic. The assay of both
substances needs a method which is able to determine the substances without performing
prior separation method. Due to its great sensitivity, Reverse-Phase HPLC with UV
detector could be used in simultaneous analysis. This research was conducted to develop
the method of losartan potassium and hydrochlorothiazide assay in tablet simultaneously.
Methods
The assay was performed on a system with Inertsil ODS-3 RP-C18 5μm (4,6x50 mm) as
column, methanol pro HPLC : H3PO4–KH2PO4 (55:45) pH 3 as mobile phase, flow rate 1
mL/minute, and detected at 225 nm.
Results
The retention time for losartan potassium and hydrochlorothiazide were 1,842 and 14,473
minutes. The system was linear for losartan potassium 10-60 μg/mL and hydrochlorothiazide
2,5-15 μg/mL with correlation coefficient 0,999. Limits of detection and quantification
for losartan potassium and hydrochlorothiazide were 2,001; 6,671 μg/mL and 0,626;
2,087 μg/m, respectively. Relative standard deviation (RSD) of intraday precision
for losartan potassium and hydrochlorothiazide were 1,360; 0,959 and 1,455; 1,400
% while the interday precision RSD were 0,333; 0,848 and 0,919; 0,904 %. Percent recovery
for losartan potassium and hydrochlorothiazide in simulation were 100,560 ± 1,032
% and 100,356 ± 0,941 %.
Conclusions
Losartan potassium and hydrochlorothiazide content in sample tablet were in range
of 97,029 – 99,875 % and 98,054 – 101,506 %. It can be concluded that the developed
method is suitable for simultaneous analysis of both active pharmaceutical ingredients.
Keywords: losartan potassium, hydrochlorothiazide, RP-HPLC, simultaneous analysis,
validation
OPC2 Synthesis, in vitro urease inhibitory potential and molecular docking study of
benzimidazole and bi-heterocyclic benzamide analogues
Syed Adnan Ali Shah1,2, Muhammad Afifi1,2, Sadia Sultan1,2, Muhammad Taha3, Muhammad
Athar Abbasi4,5
1Department of Pharmacology and Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA (UiTM) Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor,
Malaysia; 2Atta-ur-Rahman Institute for Natural Products Discovery (AuRIns), Universiti
Teknologi MARA Cawangan Selangor Kampus Puncak Alam, 42300 Bandar Puncak Alam, Selangor
D. E., Malaysia; 3Department of Clinical Pharmacy, Institute for Research and Medical
Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 1982, Dammam
31441, Saudi Arabia; 4Department of Chemistry, Government College University, Lahore
54000, Pakistan; 5College of Natural Sciences, Department of Biological Sciences,
Kongju National University, Gongju 32588, South Korea
Correspondence: Syed Adnan Ali Shah (syedadnan@uitm.edu.my)
Background
Urease is a nickel-containing metalloenzyme that widespread in nature among plants,
bacteria, fungi, algae and invertebrates. Urease producing Helicobacter pylori (H.
pylori), one of the most successful human bacterial parasites, which colonize more
than half of the human population. Urease associated diseases include severe gastroduodenal
pathologies, hepatic encephalopathy, urinary catheter encrustation, pyelonephritis
and hepatic coma. In this regard, a series of analogues benzimidazole and bi-heterocyclic
benzamide were synthesized, characterized and screened for urease inhibitory activity.
Methods
Mixed 1H-benzimidazole-2-thiol with methyl 4- (bromomethyl) benzoate and refluxed
for 5 hrs to give methyl 4-(((1H-benzimidazol-2-yl) thio)methyl)benzoate as intermediate
product. The intermediate product was finally treated and refluxed with different
substituted aldehyde/acetophenone to give the desired benzimidazole and bi-heterocyclic
benzamide analogues.
Results
The targeted benzamides and benzimidazole analogues were synthesized in good yields
and their structures were confirmed by NMR and elemental analysis. The in vitro screening
results showed that most of the ligands exhibited good inhibitory potentials against
the urease. Molecular docking revealed that fluoro analogue of bi-heterocyclic benzamide
exhibited good binding energy value (−8.40 kcal/mol) and was bound within the active
region of urease enzyme. Limited SAR suggested that the variations in the inhibitory
potentials of the analogues are the result of different substitutions on phenyl ring.
Conclusions
We have synthesized benzamides and benzimidazole analogues and screened against urease
inhibitory potential. All analogues revealed more inhibitory potentials than the previously
reported analogues for the urease activity on the basis of IC50 values, binding interactions
of most active compounds & ADMET pharmacokinetics.
Keywords: Bi-heterocycles, Benzamides, Benzimidazole, Urease, Molecular docking
OPC3 Head-to-tail position of two bridged-dimers determines the configuration of oligostilbene
structure
Nurhuda Manshoor and Jean-Frédéric F. Weber
Atta-ur-Rahman Institute for Natural Product Discovery (AuRIns), Universiti Teknologi
MARA (UiTM), 42 300 Bandar Puncak Alam, Selangor, Malaysia); Faculty of Pharmacy,
Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Nurhuda Manshoor (nurhuda15@uitm.edu.my)
Background
The first report on isolation and characterization of isohopeaphenol A was from Vatica
oblongifolia. The following year, a compound with the same spectral data was isolated
from Vatica pauciflora. It was assigned a different stereochemistry and named pauciflorol
C. Recently we isolated from Neobalanocarpus heimii (Dipterocarpaceae), a compound
with the same spectral data. We, therefore, studied the structure in detail. The stereochemistry
of the structure was conferred based on NMR spectroscopy and a three-dimensional computer
generated structural model.
Methods
The extraction of the plant material was by the classical method of repetitive maceration
and lixiviation with methanol. The crude residue was subjected to HPLC for fractionation
and isolation processes. The pure compound was isolated as a dark brown amorphous
powder. Its structural characterization was performed by means of spectrometric methods,
including extensive 2D-NMR. The stereochemistry of the compound was supported by a
3D model, obtained in silico with software, Chem 3D UltraTM.
Results
Preliminary examination of the mass, 1H- and 13C-NMR data suggested a resveratrol
tetramer. Thorough analyses of 2D-NMR confirmed the oligomeric degree and elucidated
the structure. The compound consists of two similar stilbene dimer plane structures,
linked by a bridge. The fact that they are not magnetically equivalent from an NMR
perspective suggested stereoisomeric differences for these two dimeric moieties. A
NOESY experiment contributed to solve the issue. A 3‑dimensional model was performed
and it was showed that such correlation was only possible when the second half of
the molecule is rotated 180° relative to the first half of the molecule. This information
was in agreement with the coupling constant of 11.5 Hz. The absence of cross peak
between further supported a trans configuration.
Conclusions
The present in-depth analyses of NOE data together with 3D modeling strongly suggest
that the initial structure of isohopeaphenol A is correct. It is possible that for
pauciflorol C, the author overlooked the possibility for the two halves of the molecule
to be positioned in a head-to-tail manner, which is the only way to understand some
of the measurements discussed above. As a result, it is concluded that the spectroscopic
data is for isohopeaphenol A.
Keywords: isohopeaphenol A, pauciflorol C, oligostilbenes, phytochemistry, spectroscopy.
OPC4 Design and syntheses of ortho-, meta- and para-xylylguanidinium–zn2+–cyclen complexes
and their interaction with DNA (cyclen = 1,4,7,10–tetraazacyclododecane)
Nor Amin Hassan1, Mohd Zulkefeli2, Jean-Frédéric F. Weber3
1Faculty of Pharmacy, Universiti Teknologi MARA, Bertam, Pulau Pinang, 13200 Malaysia;
2School of Pharmacy, International Medical University, Kuala Lumpur, 57000 Malaysia;
3Faculty of Pharmacy, Universiti Teknologi MARA, Puncak Alam, Selangor, 42300 Malaysia
Correspondence: Jean-Frédéric F. Weber (jffweber@uitm.edu.my)
Background
Three new zinc ions (Zn2+) complexes, C
1
, C
2
and C
3
, were designed and synthesized by coordination of Zn2+ into the integrated 1,4,7,10-tetraazacyclododecane
(cyclen) and ortho-, meta- and para-bromoxylylguanidinium pendants group. The aim
of synthesizing these Zn2+ complexes was to confirm the anticipated interactions of
Zn2+ complexes towards natural DNA as well as to explore the phosphatase activity
of such complexes. A retrosynthetic analysis was carried out to identify and solve
problems with regard the selection of organic reactions.
Methods
The syntheses were performed in five steps including of (i) Gabriel and Ing-Manske
primary amine synthesis, (ii) SN2 substitution reaction, (iii) guanylation of primary
amine, (iv) deprotection of Boc group, and (v) coordination of Zn2+ complex. All the
Zn2+ complexes structures were characterized by 1H- and 13C-NMR spectroscopy, infrared
spectroscopy and mass spectrometry. Ethidium bromide (EB) fluorescence assay and circular
dichroism (CD) spectroscopy were used to ascertain the interaction between Zn2+ complexes
towards natural DNA i.e. calf thymus (ctDNA).
Results
The former assay demonstrated a displacement of EB from its complexes with ctDNA,
thus confirming the affinity of these Zn2+ complexes towards DNA. CD spectroscopic
results also revealed that C
1
has disturbed both base stacking and right handed helicity properties of ctDNA, but
retained the B-form of its structure. By contrast, C
2
and C
3
transformed the conformation of ctDNA from B-form into Z-form. This was further supported
by thermal denaturation studies showing ΔT
m
values of C
1
, C
2
, and C
3
to be +2, +4 and +5, respectively.
Conclusions
The catalytic properties of these complexes for phosphate hydrolysis was evaluated
using phosphodiesters bis(p-nitrophenyl)phosphate (BNPP) as a model and monitoring
by UV spectrometry. The BNPP hydrolysis results (ca. 17% after 8 days incubation)
suggested that C
1
, C
2
, and C
3
were endowed with still modest yet significant catalytic properties.
Keywords: Zn2+ Complex, Guanidinium, DNA Binding, Phosphodiesterase, BNPP Hydrolysis.
OPC5 Persistence of drugs residue in urban river. Case study of Sungai Buloh, Malaysia
Zulhafizal Othman1,2, Marfiah Ab. Wahid1,3, Khuriah Abdul Hamid4 and Jazuri Abdullah3
1Micropollutant and Pathogen in Water Research (WATERμPath), Universiti Teknologi
MARA, 40450 Shah Alam, Selangor, Malaysia; 2Faculty of Civil Engineering, Universiti
Teknologi MARA, Cawangan Pahang, Jengka Campus, 26400 Bandar Tun Abdul Razak Jengka,
Pahang, Malaysia; 3Faculty of Civil Engineering, Universiti Teknologi MARA, 40450
Shah Alam, Selangor, Malaysia; 4Faculty of Pharmacy, Universiti Teknologi MARA, Cawangan
Selangor, Puncak Alam Campus, 42300 Puncak Alam, Selangor, Malaysia
Correspondence: Marfiah Ab. Wahid (marfi851@uitm.edu.my)
Background
Drugs and their metabolites are continually introduced into the environment and are
prevalent at detectable concentrations, which may affect water quality and potentially
impact drinking water supplies, ecosystem and human health. The discharge of micropollutants
without control can have the adverse health impact and at the same time can disturb
the aquatic ecology and systems in a long period of exposure. In addition, the occurrence
at trace levels of several drugs in drinking water raises concerns about possible
implications for human health. Therefore, it is critically needed to conduct the study
on detection of drugs on river water because the data are still insufficient especially
in Malaysia. This study is done to trace the residue of drugs in urban surface water
which is in Sungai Buloh, Malaysia as a selected urban river.
Methodology
The samples were analysed using liquid chromatography coupled with quadrupole-time-of-flight
tandem mass spectrometry (LC-Q-ToF/MS) for compounds tracing purpose.
Results
From the result obtained, several drugs have been traced in river water. All the drugs
detected were classified based to their therapeutic usage. The residues detected consist
of β-blockers, analgesics and psychoanaleptics.
Conclusion
The river contains drugs that may affect the environment. Further analysis needs to
be done to get a more accurate concentration of the drug residue that contaminated
the river.
Acknowledgement
The authors would like to acknowledge Universiti Teknologi MARA for providing great
facilities throughout the research project, Ministry of Higher Education Malaysia
for assisting with SLAB/SLAI scholarship.
OPE1 CDIO approach method for supply chain education improve pharmacy students’ skills
Nguyen Huu Khanh Quan1, Nguyen Thi Ngoc Yen2, Thai Hong Thuy Khanh3
1Department of Clinical Pharmacy, Faculty of Pharmacy, Nguyen Tat Thanh University,
300A Nguyen Tat Thanh street, Ho Chi Minh City, Viet Nam; 2Department of Microbiology
- parasites, Faculty of Pharmacy, Nguyen Tat Thanh University, 300A Nguyen Tat Thanh
street, Ho Chi Minh City, Viet Nam; 3Faculty of Finance and Accounting, 300A Nguyen
Tat Thanh Street, Ho Chi Minh City, Viet Nam
Correspondence: Nguyen Huu Khanh Quan (nhkquan@ntt.edu.vn)
Background
Engineering education and real-world demands on engineers have in recent years led
engineering schools in the USA and Europe to form the Conceive Design Implement Operate
(CDIO) initiative. It is a worldwide collaboration to conceive and develop a new vision
of engineering education. The main objective of this research was to determine the
implementation of CDIO training methods to pharmacy education (knowledge-skills-attitudes)
in the pharmaceutical supply chain can improve the students; skills.
Methods
A cross sectional survey was conducted to assess the current level and level of expectation
from stakeholders for the skills of pharmacy students in pharmaceutical industry training
universities in Ho Chi Minh City.
Results
Findings from the current study revealed that there are differences between the current
level and the level of expectation of the stakeholders on the skills to be trained
for students to meet the requirements of employers for work needs.
Conclusions
The findings from this study are the basis of developing pharmaceutical supply chain
education and the application of CDIO training methods to the universities in Ho Chi
Minh City. This is essential for the students to know and prepare to meet the demand
of the workforce and society after graduation.
Keywords: Mapping CDIO skills, CDIO, pharmaceutical supply chain
Poster presentation
PPT1 Evaluation of quality and stability of matrix tablet contained monoammonium glycyrrhizinate
Otgonsuren.Daramzav1, T S Davaasuren1, Enkhtuul Bayarsaikhan 2, Damdinjav Davaadagva1,
Enkhjargal. Dorjbal2, Jambaninj Dambiinyam 1
1Department of Pharmaceutical Technology, School of Pharmacy, Mongolian National University
of Medical Sciences; 2Department of Pharmaceutical Chemistry and Pharmacognosy, School
of Pharmacy, Mongolian National University of Medical Sciences
Correspondence: Jambaninj Dambiinyam (jambaninj@mnums.edu.mn)
Background
Monoammonium glycyrrhizinate of Glycyrrhiza root has been used as an expectorant,
detoxificator, anti-allergic, and antioxidant. We have isolated monoammonium glycyrrhizinate
from Glycyrrhiza root, grown in Mongolia by previous study. The objective of the study
was to develop prolonged release matrix tablet with hepatoprotective effect and to
evaluate their pharmacotechnical qualities and stability.
Methods
The matrix tablets were prepared by wet granulation method. In order to develop appropriate
tablets various excipients such as matrix former, diluents, binder, lubricant and
glidiant were added. APIs and matrix former, diluent and binder were mixed properly
and were granulated with the 5% solution of PVP K-30 as a binder solution. The wet
mass was granulated by wet granulator through the sieve with 2 mm diameter holes and
generated wet granules were dried at room temperature. Dry granules were lubricated
with talc and magnesium stearate. The matrix tablets were prepared by the compression
of the tablet mixture using rotary tablet machine. The quality of the prepared tablets
was evaluated according to Mongolian National Pharmacopoeia’s methods by criterias
such as appearance, average weight, weight variation, hardness, friability, mocrobiological
contamination and in-vitro dissolution study. Licozinat matrix tablets contained monoammonium
glycyrrhizinate 140 mg; glycine 50 mg; LD-methionin 50 mg in each tablet.
Results
Formulations were evaluated and satisfied the quality criteria by Mongolian National
Pharmacopoeia methods. The stability of matrix tablet tested by long term method for
12 months and by accelerated method for 6 months according to standard MNS 6439:2014.
stability testing results by both long term and accelerated method, Licozinat matrix
tablet was stable for 12 months. Stability testing of matrix tablet is continuing
by long term method.
Conclusion
Controlled release “Licozinat” matrix tablets were prepared by wet granulation method.
Formulation (F5) containing 20% HPMC K4000 releases in the desired manner and was
determined to be the appropriate design. Licozinat matrix tablet was stable for 12
months. Stability testing of matrix tablet is continued by long term method.
Keywords: Glycyrrhiza uralensis, monoammonium glycyrrhizinate, matrix tablet, stability
testing
PPT2 Formulation and evaluation of in situ gelling system for ophthalmic delivery
of Erythromycin
Abdullah Khan1, Reeshanteni Balasingam2, Anandarajagopal Kalusalingam1
1School of Pharmacy, KPJ Healthcare University College, Kota Seriemas, 71800 Nilai,
Negeri Sembilan; 2DiethelmKellerSiberHegner (DKSH) Healthcare, Malaysia
Correspondence: Abdullah Khan (abdullahkhan@kpjuc.edu.my)
Background
Conventional ophthalmic dosage forms provide low bioavailability and less pre-corneal
drug residence time due to nasolacrimal drainage and blinking action of the eyes.
The major challenge is to formulate a system to improve the contact time of the drug
in the eyes. The present study was aimed to prepare and evaluate in situ gelling system
for the effective delivery of Erythromycin to combat ophthalmic infections.
Methods
Development of novel in situ gelling system using Erythromycin was based on the concept
of ion triggered in-situ gelation. Sodium Alginate was used as a gelling agent in
combination with Hydroxypropyl methylcellulose (HPMC K100) as a viscosity enhancing
agent. The prepared formulations were evaluated for physical appearance, pH, gelling
capacity, viscosity, stability studies, drug content, in vitro diffusion study and
s spreadability test.
Results
All formulations were found to be clear and free from undissolved particles. The pH
of the formulations was within the range of 6.8 – 6.92 which is safe for ophthalmic
use. Formulation F4 (Sodium Alginate 1.2% and HPMC 0.5%) showed optimum viscosity
of 48cps, good spreadability and gelling capacity that will improve residence time
of the drug in eyes. All the formulations were found to have drug content uniformity
of 98 ±2% p. In vitro, drug release studies showed that the drug was released in the
of order F2<F1<F3<F4 over the period of 8 hours. All formulations F1 to F4 followed
zero order drug release kinetic with a correlation coefficient of (R2=0.990) followed
by the Korsmeyer-Peppas model showed drug released from the system by diffusion mechanism.
Conclusion
The developed in situ gelling systems may provide greater ocular bioavailability and
it may be proposed to treat ocular infections by retaining the drug for a prolonged
period in the eyes.
Keywords: In situ gel, ophthalmic, Erythromycin, HPMC, Sodium Alginate.
PPT3 Development of glucomannan nano-emulsion formulation as non-steroidal treatment
for atopic dermatitis
Mohd Hafiz Mohd Jaafar1, Khuriah Abdul Hamid1, Munira Shahbuddin2, Zahid Hussain1,
Tommy Julianto Bustami Affendi1, Nor Amlizan Ramli1
1Department of Pharmaceutics, Faculty of Pharmacy, Universiti Teknologi MARA (UiTM),
42 300 Bandar Puncak Alam, Selangor, Malaysia; 2Department of Biotechnology Engineering,
Kuliyyah of Engineering, International Islamic University Malaysia (IIUM), Gombak
50728, Kuala Lumpur
Correspondence: Nor Amlizan Ramli (nor.amlizan@uitm.edy.my)
Background
Atopic dermatitis is a chronically relapsing pruritic inflammatory disease which affects
15% to 30% of children and 10% of adults in industrialized country. Konjac glucomannan
(KGM) isolated from Amorphophallus konjak K. Koch exhibit high water solubility, biocompatibility,
biodegradability and non-toxic properties. There are vast applications of KGM including
biomedical studies such as cholesterol and obesity studies, anti-inflammatory effect,
antioxidant study, and wound healing property. In this research, we developed KGM
nano-emulsion as drug carrier that acts as hydrogel which stabilized the formulation
and moisturize the skin for relieving atopic dermatitis.
Methods
Cream formulations were developed using variable ratios of glucomannan (1%-1.5%),
Olive oil (0%-20%) and avocado oil (0%-20%). Oil phase and aqueous phase were mixed
under constant stirring using Ika-Werke Eurostar with propeller mixer at 900 rpm for
10 min. The formulations will be tested and measured for particle size and zeta potential
using zetasizer (Nano ZS, Malvern Instrument, UK); and Firmness and viscosity using
rheometer (Physica MCR 301).
Results
The mean particle size for KGM nano-emulsion ranged from 326.93±11.14 to 586.7±26.48
nm with polydispersity index ranges from 0.41±0.04 to 0.56±0.02. The zeta potentials
of KGM nano-emulsion showed low values indicate stable formulations which ranged from
-45.83±2.30 to -47.70±354 mV. The firmness of nano-emulsion formulations were lower
than control (753.20±7.53 g) which were measured from 477.45±8.52 to 658.84±10.20
g. Finally, viscosity of nano-emulsion also lower than control group (2773±632.64
Pa·S), where the values were ranged from 1393±210.32 to 2033±32.15 Pa·S.
Conclusions
Glucomannan showed promising application in cream development as it exhibits non-toxic
and high bioavailability. Development of glucomannan cream using 1.5% glucomannan
concentration combination of both avocado oil and olive oil (Formulation C) provides
small mean particle size and uniform polydispersity index with good zeta potential.
The firmness and work of shear of Formulation C also provides comparable results to
control group. Finally, non-Newtonian pseudoplastic properties of these creams provide
an even spreadibility on skin.
Keywords: Nanoemulsion, Glucomannan, Atopic dermatitis, Anti-steroidal treatment
PPT4 Preparation and characterisation of fast-dissolving oral films
Muhammad Qayiem Razali, Muhammad Sahmi Mohd Sairi, Nor Hayati Abu Samah
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Selangor Branch, Puncak Alam
Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Nor Hayati Abu Samah (norhay2975@uitm.edu.my)
Background
Fast-dissolving oral films (ODF) are thin sheets designed to rapidly disintegrate
when in contact with saliva to release the incorporated active, without the need for
swallowing. Difficulty in swallowing solid dosage forms (e.g. tablets) has been identified
as one of the factors affecting the non-compliance of patient populations such as
paediatric and geriatric. Thus, ODF may serve as an alternative to existing dosage
forms. This study aimed to formulate and characterise a series of ODFs made from hydroxypropyl
methylcellulose (HPMC) and carboxymethylcellulose (CMC), plasticised with glycerol
and sorbitol.
Methods
Three formulae of each HPMC and CMC were prepared by solvent casting technique. The
resulting films were characterised physically (i.e. visual appearance) and mechanically
(i.e. mass and thickness variation, folding endurance and tensile strength). Furthermore,
the placebo films were also assessed in terms of their disintegration time and contact
angle.
Results
The films produced were not sticky, easy to handle and acidic in nature. They had
an average mass between 19 to 30 mg and thickness between 41 to 78 μm. Films of CMC
were significantly thicker than the HPMCs (p<0.05). For CMC films, reduction in CMC
and increase in plasticiser contents were found to slightly enhance their tensile
strength and elasticity, indicative of weaker and softer films. On the other hand,
the HPMC films exhibited greater tensile strength, but lower extensibility than the
CMC films. Films dissolved within 180 s and 25 s for CMC and HPMC, respectively. The
CMC films took longer time to disintegrate than the HPMC films due to their higher
contact angles values with water. The disintegration of all films increased in corresponding
to an increase in tensile property.
Conclusion
Formulation HPMC-3 was considered as the best candidate for further optimisation for
drug loading as it possessed the ideal balance between toughness and flexibility.
Keywords: hydroxypropyl methylcellulose; carboxymethylcellulose; fast-dissolving;
oral film
PPP1 L-Stepholidine (SPD) treatment ameliorates learning and memory deficits in ICR
mice
Arunkumar Karunanidhi1, Kalavathy Ramasamy2,3, Siong Meng Lim1,3 Fazlin Mohd Fauzi1
1Department of Pharmacology and Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA, Selangor Branch, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor Darul
Ehsan, Malaysia; 2Department of Pharmaceutical Life Sciences, Faculty of Pharmacy,
Universiti Teknologi MARA, Selangor Branch, Puncak Alam Campus, 42300 Bandar Puncak
Alam, Selangor Darul Ehsan, Malaysia; 3Collaborative Drug Discovery Research (CDDR)
Group, Pharmaceutical and Life Sciences Community of Research, Universiti Teknologi
MARA, 40450 Shah Alam, Selangor Darul Ehsan, Malaysia
Correspondence: Fazlin Mohd Fauzi (fazlin5465@uitm.edu.my)
Background
L-Stepholidine (L-SPD) was recently identified through our virtual screening exercise
in search of potential drugs for Alzheimer’s disease (AD). L-SPD is an active ingredient
of the Chinese herb Stephania intermedia. Prior research has reported beneficial effects
of L-SPD on dopamine D1- and D2-type receptors, suggesting promising treatment/prevention
approach for neurodegenerative diseases. This study evaluated the effect of SPD on
spatial learning and memory in lipopolysaccharide (LPS)-induced murine neuroinflammation
model.
Methods
ICR male mice (n=8/group) were randomly grouped as follows: controlsaline, LPSsaline,
LPS SPD 3 mg/kg b.w., LPS SPD 5 mg/kg b.w., LPS SPD 10 mg/kg b.w. and positive control:
LPS D-Serine (30 mg/kg). The mice were allowed to acclimatize for 3 days prior to
treatment with SPD (i.p.) for 5 days (i.e. on day 1, 2, 3, 4, 5). Except for the controlsaline
group, all mice received LPS (1 mg/kg b.w.). Following treatment, the mice were subjected
to Morris water maze (MWM) test to evaluate the spatial learning and memory function.
Finally, a probe trial was conducted on day 6 to evaluate their memory retention.
Results
SPD treatments at 5 and 10 mg/kg bw displayed earliest measure of learning, with an
escape latency of ~18-25 secs compared to ~26-35 secs of control. SPD-treated groups
(3, 5 and 10 mg/kg bw; 2.04-2.33) entered the platform zone more frequently compared
to positive (1.41) and negative control (1.79). SPD treated mice showed better spatial
learning (shorter escape latency and travelled distance) than the LPS control. A high
SPD dose (10 mg/kg) showed a significant increase in the number of entries to the
platform zone and time spent in the target quadrant.
Conclusions
Based on the swimming time in the target quadrant and the frequency of crossing the
platform, SPD treatment may ameliorate cognitive deficits in learning and memory functioning
in ICR mice.
Keywords: L-Stepholidine; lipopolysaccharide; neuroinflammation; memory deficits;
behavioral test.
This project is funded by the Ministry of Education of Malaysia with Universiti Teknologi
MARA (UiTM) through the Fundamental Research Grant Scheme (FRGS; 600-RMI/FRGS 5/3
(0020/2016).
PPP2 Synthesis, characterization, and antioxidant potential of biodegradable polyurethane
based on polypropylene fumarate as polyol
Bushra Naureen1, A.S.M.A. Haseeb2, W.J. Basirun1,3, F.B. Muhamad4
1Department of Chemistry, Faculty of Science, University of Malaya, 50603 Kuala Lumpur,
Malaysia; 2Department of Mechanical Engineering, Faculty of Engineering, University
of Malaya, 50603 Kuala Lumpur, Malaysia; 3Institute of Nanotechnology and catalyst
(NANOCAT), University of Malaya, 50603 Kuala Lumpur, Malaysia; 4Department of Biomedical
Engineering, Faculty of Engineering, University of Malaya, 50603 Kuala Lumpur, Malaysia
Correspondence: A.S.M.A. Haseeb (haseeb@um.edu.my)
Background
Prominent biomaterials for various biomedical applications include natural or synthetic
polymers. Among synthetic polymers, polyurethanes (PUs) are unique due to their versatile
physiochemical and mechanical properties. Free radicals in body e.g. nitrogen and
oxygen are very reactive and cause oxidative damage of cells and tissues, thus affecting
normal healing and regeneration processes. There is a need to develop and explore
antioxidant potential of ligands, capable of neutralizing reactive free radicals.
In the present study, novel biodegradable PU was synthesized, based on polypropylene
fumarate diol as polyol, hexamethylene diisocyanate (HDI) and poly-3-hydroxy butyrate
as chain extender via two step growth polymerization process.
Methods
The prepared samples were characterized by using Fourier Transform Infrared Spectrophotometer
(FTIR), Nuclear Magnetic Resonance (NMR), mass spectrometry and Scanning Electron
Microscope (SEM).
Results
The FTIR spectrum of PU prepolymer, exhibiting C=C at 1645 cm-1and C=O at 1726 cm-1
confirmed the presence of polypropylene fumarate.
Conclusion
The aim of the present study is to exploit antioxidant activity of the synthesized
novel polyurethane via DPPH (2,2-diphenyl-1-picryl hydrazyl-hydrate) Assay. The results
supported antioxidant potential of the synthesized novel polyurethane, to be employed
further in biomedical applications.
Keywords: Polyurethane, Polypropylene Fumarate, Poly-3-hydroxy butyrate, Antioxidant
PPP3 Polyethyleneimine cytotoxicity against human cancer cell lines
Akmal Arif Daud1, A’edah Abu Bakar2, Ramli Salfarina1, Hasseri Halim1
1Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam,
Selangor, Malaysia; 2Petroliam Nasional Berhad, Level 15, Tower 3, Petronas Twin Towers,
50088 Kuala Lumpur City Centre, W.P. Kuala Lumpur
Correspondence: Hasseri Halim (hasseri2945@uitm.edu.my)
Background
Polyethyleneimine (PEI) is a simple and cost-effective reagent for condensing and
linking plasmid DNA to cells for gene delivery. However, its cytotoxicity has not
yet to be reported. The aim of this study was to determine the lethal dose (IC10)
of PEI against breast cancer (MCF7), lung cancer (A549) and liver cancer (HepG2) cell
lines.
Methods
MCF7, A549 and HepG2 cancer cell lines were treated with various concentrations of
PEI for 24 hours. The viability of the cells was determined using the MTS assay.
Results
The IC10 of PEI for MCF7, A549 and HepG2 cell line were 73.2 μg/mL, 62.0 μg/mL and
70.5 μg/mL, respectively. This indicated that PEI is more cytotoxic towards A549 cancer
cell line.
Conclusion
The IC10 results obtained from this study is useful to optimise transfection parameters
of PEI on A549, MCF7 and HepG2 cell lines.
Keywords: Transfection, polyethyleneimine, cancer
PPP4 Antibacterial activity of selected Cambodia medicinal plants in vitro
Kanika Heng1, Sothea Kim2, Monidarin Chou1
1Rodolphe Mérieux Laboratory University of Health Sciences, 73, Bd Monivong, Phnom
Penh, Cambodia; 2Laboratory of Phytochemistry IRPF/UHS, University of Health Sciences,
73,Bd Monivong, Phnom Penh, Cambodia
Correspondence: Kanika Heng (h_kanika@uhs.edu.kh)
Background
Antimicrobial resistance has become a serious problem of public health. It creates
a constant need for either new antimicrobial compounds or inhibitors of mechanisms
that underlie antibiotic resistance. Cambodia is one of the well-known South-East
Asia countries where natural substances are widely used for treatment of many diseases,
especially for infectious diseases. As such, the study of antibacterial activity of
plants traditionally used by Cambodian traditional healers to treat infectious diseases
is important. This study aimed to screen the antimicrobial activity of 138 extracts
from 67 plants that are traditionally used by Cambodian traditional healers.
Methods
The plants were collected in eight provinces and cities of Cambodia. The extraction
was performed using ethanol:water (50/50 v/v) to obtain the majorities of the compounds
present in plants. The antibacterial activities of plants extracts were first tested
against reference strains, Staphylococcus aureus (ATCC 6553; cocci; Gram positive
bacteria) and Pseudomonas aeruginosa (ATCC 9027; rod; Gram negative bacteria), and
then against clinical strains using micro-dilution and macro-dilution tests, respectively.
Results
A total of 138 extracts isolated from 67 species of plants were tested. Most of the
extracts were very active against S. aureus but less active against P. aeruginosa.
Only 5 extracts derived from 5 plants were highly active against both standard and
isolated strain of S. aureus. Three plant extracts were highly active against standard
strain of P. aeruginosa but weakly active against its isolated strain.
Conclusions
Our results showed a great variability of the bacteriostatic qualities of extracts
between isolated and standard strains. These results warrant selection of the most
active extracts for development of antimicrobial products based on medicinal plants.
Keywords: Antibacterial activities, Staphylococcus aureus, Pseudomonas aeruginosa,
Micro-dilution, Macro-dilution
PPP5 Body mass index is not correlated to blood glucose levels in Down Syndrome individuals
Maziana Mahamood, Mizaton Hazizul Hasan, Aishah Adam
Department of Pharmaceutical Pharmacology and Chemistry, Faculty of Pharmacy, Universiti
Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia.
Correspondence: Maziana Mahamood (maziana2795@uitm.edu.my)
Background
Down syndrome (DS) is a common chromosomal abnormality that occurs in about 1 in 700
live births. Previous studies found that DS is associated with higher obesity rates.
There is a wide spectrum of medical complications among individuals with DS, which
include diabetes mellitus that are associated with increased susceptibility to weight
gain. Therefore, the present study was carried out to evaluate the association between
body mass index (BMI) and fasting blood glucose levels in DS individuals.
Methods
Measurement of height and weight was done, and BMI was calculated. Blood was collected
with informed consent from the parents or guardians of DS individuals (n=52) and controls
(n=52). Fasting blood glucose level was measured by using the Reflotron® Plus System.
Results
The mean BMI of individuals with DS ranged from 11.1 to 37.2 kg/m2 with 13.5% (n=7)
being overweight and 7.7% (n=4) obese. The mean BMI of controls ranged from 13.8 to
33.3 kg/m2 with 19.2% (n=10) being overweight and 3.8% (n=2) obese with no significant
difference (p>0.05) between DS and controls. There was also no significant difference
(p>0.05) in the fasting blood glucose levels in DS (mean=5.22 mmol/L) when compared
to controls (mean=5.35 mmol/L). With respect to the association of BMI and fasting
blood glucose, the present results failed to prove the relationship in both groups
(p>0.05).
Conclusions
It can be concluded that there was no significant difference in the levels of fasting
blood glucose in DS individuals when compared to controls. This study also found no
prove of association between fasting blood glucose levels and BMI in both DS and controls
group.
Keywords: Down syndrome, BMI, Glucose
PPP6 Effects of Myrmecodia platytyrea methanolic tuber extract on sub-acute cancer-induced
severe combined immunodeficiency (SCID) mouse model
Nurhafizah Ibrahim1,2, Mizaton Hazizul Hasan1, Aisyah Hasyila Jahidin1, Aishah Adam1
1Faculty of Pharmacy, Universiti Teknologi MARA, 42300 Puncak Alam, Selangor Darul
Ehsan;
2Faculty of Engineering and Life Sciences, Universiti Selangor, 45600 Bestari Jaya,
Selangor Darul Ehsan.
Correspondence: Mizaton Hazizul Hasan (mizaton_hazizul@uitm.edu.my)
Background
Myrmecodia platytyrea (Ant’s plant) is member of Rubiaceae family. Tuber of M. platytyrea
is used traditionally as decoction to treat various mild and severe diseases including
cancer. Other species of Myrmecodia including M. platytyrea have been reported for
their antiproliferative effect against various cancer cells in vitro. Hence, this
study was carried out to investigate the effect of sub-acute administration of M.
platytyrea methanolic tuber extract (MPMTE) on hepatocellular carcinoma (HCC)-induced
SCID mice.
Method
A total of 36 SCID mice were divided into 6 groups (n=6/group): control 1 (non HCC-induced
mice treated with normal saline), control 2 (HCC-induced mice treated with normal
saline), control 3 (HCC-induced mice treated with 10 mg/kg doxorubicin) and 3 groups
of HCC-induced mice treated with 100, 200 and 400 mg/ kg of MPMTE, respectively. NS
and MPMTE were given orally twice daily, for 28 days whereas doxorubin was given intraperitoneally
once daily to control 3 at 3-day intervals. Mortality, body weight, food and water
intake were recorded throughout the experiment. Physical and behavioural changes were
also observed. All mice were sacrificed on day 29. Tumour was excised and weighed.
Result
Control 1, 2 and the HCC-induced mice treated with MPMTE showed no mortality. No significant
changes in terms of body weight, food intake and water intake were observed in all
groups. However, HCC-induced mice treated with doxorubicin showed symptoms of toxicity
and 100% mortality was recorded after 9 days of treatment. Remarkably, sub-acute oral
administration of MPMTE (100 and 400 mg/kg, p.o.) suppressed tumour development at
13% and 6%, respectively. The tumour volume of mice treated with 200 mg/kg, on the
other hand, was found to increase by14%.
Conclusion
SCID mice treated with MPMTE (100 and 400 mg/kg, p.o., bid) for 28 days showed tumour
suppression, suggesting potential therapeutic value of the plant.
Keywords:
Myrmecodia platytyrea; hepatocellular carcinoma; tumour suppression; severe combined
immunodeficiency mouse model
PPP7 Antagonistic interactions between Chromolaena odorata ethanolic extract and cisplatin
against breast cancer cell lines MCF-7 and MDA-MB-231
Nurliana Abd Mutalib1, Zulhilmi Mohamad Bakri1, Khairuddin Abdul Jalil1, Normala Abd
Latip1
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor,
Malaysia
Correspondence: Normala Abd Latip (drnormala6351@.uitm.edu.my)
Background
In Malaysia, breast cancer, which was ranked as the number one disease among female
in 2016, has seen its incidence increased between 2007 to 2011. Cisplatin has been
commonly used as the first line treatment against breast cancer. However, the combination
uses of alternative medicine (CAM) together with conventional therapy by many cancer
patients could possibly lead to unwanted interactions. This study had evaluated Chromolaena
odorata, locally known as pokok kapal terbang for its potential to interact with cisplatin
in combination therapy.
Methods
C. odorata was extracted using maceration method with 70% ethanol. Antiproliferative
activity of the extract was screened against a panel of cell lines using the MTT assay.
For combination study, MCF-7 and MDA-MB-231 breast cancer cell lines were treated
with C. odorata ethanolic extract in combination with cisplatin. Isobologram and combination
index (CI) were derived from the combination treatments.
Results
The yield of extraction was 2.69%. The IC50 values of C. odorata antiproliferative
activity against MCF-7, MDA-MB-231, WRL68 and CRL2522 were 0.15 ± 0.00 mg/mL, 0.43
± 0.02 mg/mL, 0.31 ± 0.00 mg/mL and 0.63 ± 0.00 mg/mL, respectively. Co-treatment
of cisplatin and C. odorata ethanolic extract at IC10, IC15 and IC25 against MCF-7
and MDA-MB-231 resulted in CI greater than one.
Conclusions
Combination treatment of cisplatin and C. odorata ethanolic extract leads to antagonistic
interactions.
Keywords:
Chromolaena odorata, cisplatin, MTT, isobologram, combination index
PPP8 In silico prediction of bile pigments binding affinity towards CYP2A6 enzyme
Nurnadia Majid1, Siti Azma Jusoh1, Aedah Abu Bakar3, Hasseri Halim1, Salfarina Ramli1,2
1Faculty of Pharmacy, Universiti Teknologi MARA Cawangan Selangor, Kampus Puncak Alam,
42300 Puncak Alam, Selangor, Malaysia; 2Integrative Pharmacogenomics Institute (iPROMISE),
Universiti Teknologi MARA Cawangan Selangor, Kampus Puncak Alam, 42300 Puncak Alam,
Selangor, Malaysia; 3Petroleum Nasional Berhad (PETRONAS), Level 63, Tower 2, PETRONAS
Twin Towers, Kuala Lumpur City Centre, 50088 Kuala Lumpur, Malaysia
Correspondence: Salfarina Ramli (salfarina2892@uitm.edu.my
)
Background
Binding of cytochrome P450 2A6 (CYP2A6) enzyme to tobacco-specific N-nitrosamine,
4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK) results in electrophilic species
that would later react with DNA to form DNA adduct. Bile pigments such as bilirubin
and biliverdin, which are substrates for CYP2A6 enzyme, may inhibit the binding of
NNK to CYP2A6 enzyme. Therefore, the aim of this study was to predict the binding
properties and affinity of bile pigments towards CYP2A6 using in silico approach.
Methods
Molecular docking using AutoDock software was performed to computationally predict
the binding properties and calculate the binding affinity of bile pigment towards
the wildtype and CYP2A6 variant proteins. DoGSiteScorer and Allopred programs were
used to predict potential drug binding and allosteric pockets on the CYP2A6.
Results
The binding affinity of bilirubin and biliverdin to the active site of CYP2A6 enzyme
(with an average of 26.6 kcal/mol and 28.0 kcal/mol, respectively) was lower than
that of NNK to CYP2A6 (with an average of -6.77 kcal/mol). Several potential binding
pockets were identified on the CYP2A6 enzyme using DoGSiteScorer and Allopred programs.
Bilirubin and biliverdin showed high binding affinity to allosteric site as compared
to the active site of CYP2A6 enzyme.
Conclusion
High binding affinity of bile pigments indicates their potential to inhibit the binding
of NNK to CYP2A6 enzyme. However, this requires further confirmation by enzymology
studies.
Keywords: NNK, CYP2A6, Bilirubin, Biliverdin, Molecular docking
PPP10 Study on the effect of some medicinal plants on in vitro proliferation of peripheral
blood mononuclear cells and their antioxidant activity
Thao-Nguyen Le-Thi1, Minh-Thuan Nguyen-Thi2
1Department of Biochemistry, Faculty of Pharmacy, Lac Hong University (LHU), 10 Huynh
Van Nghe Street, Bien Hoa City,810000 Dong Nai, Vietnam ; 2Department of Biochemistry,
Faculty of Pharmacy, University of Medicine and Pharmacy Ho Chi Minh City (UMP), 43
Dinh Tien Hoang Street, Ben Nghe Ward, District 1, 760000 Ho Chi Minh, Vietnam
Correspondence: Thao-Nguyen Le-Thi (thaonguyen@lhu.edu.vn)
Background
Medicinal plants have been used widely in the treatment of immune-related diseases
such as immunodeficiency, hypersensitivity, inflammation, or autoimmune diseases,
yet little is known about their mechanisms of action. Therefore, this study was conducted
to study the effect of some medicinal plants on in vitro proliferation of peripheral
blood mononuclear cells (PBMCs) and their antioxidant activity.
Methods
PBMCs were isolated from whole blood of healthy donors. MTT assay was used to evaluate
the effect of 13 extracts in 96% ethanol and 24 fractionated extracts on PBMCs in
vitro proliferation. IL–2 concentrations secreted by extracts–treated PBMCs were quantitated
using ELISA. The plant extract with the strongest antiproliferative activity was chosen
for further evaluation on the apoptosis/necrosis and ratios of TCD3+/CD4+ and TCD3+/CD8+
of PBMCs. Antioxidant activities of 96% ethanol extracts and fractionated extracts
were assessed using DPPH assay.
Results
Of the 13 ethanol extracts, 6 extracts inhibited and 2 extracts stimulated the in
vitro proliferation of PBMCs. The extracts with inhibitory effects reduced the amount
of IL–2, whilst the extracts with stimulatory effects showed no effect on IL–2 expression
compared to untreated cells (control). The chloroform extract of Wedelia chinesis
showed strongest inhibitory activity with an IC50 value of 16.1 ppm, exerting an increase
of 19.1% in apoptosis and a decrease of 4.18% in TCD3+/CD4+ ratio compared to untreated
cells. The chloroform extract of Piper betle showed a strong antioxidant activity
with an EC50 of 1.94 ppm, 2.1 times higher than that of vitamin C.
Conclusions
The chloroform extract of Wedelia chinensis had a potential of being used in the treatment
of autoimmune diseases. Further studies are needed to isolate and identify the compounds
responsible for this activity.
Keywords: PBMCs, interleukine–2, TCD3+CD4+/ TCD3+CD8+, cytotoxicity, antioxidant
PPP11 MDA-MB-231 cells are resistant to low concentrations of medroxyprogesterone
Nur Anis Sahira Abd Rahman1, Nor Anisa Aisyah Nor Hasrin1, Sharifah Nurfazilah Wan
Yusop2, Sadia Sultan1, 2, Nur Syamimi Ariffin1
1Department of Pharmaceutical Pharmacology and Chemistry, Faculty of Pharmacy, Universiti
Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia; 2Atta-ur-Rahman
Institute for Natural Product Discovery (AuRins), Faculty of Pharmacy, Universiti
Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Nur Syamimi Ariffin (nursyamimi.ariffin@uitm.edu.my)
Background
Breast cancer is the most prevalent cancer among women worldwide. Despite treatment
options available for breast cancer, the rate of mortality is high with over 500,000
deaths reported annually. The aggressiveness of triple-negative breast cancer (TNBC)
makes the treatment challenging and this is especially true in preventing the cells
from migrating to other sites in the body. Therefore, identifying compounds that can
inhibit TNBC cells from metastasizing to other regions is crucial before it develops
a secondary cancer. Medroxyprogesterone (MP) is a synthetic derivative of progesterone
and it shares similar pharmacological actions to progestin. The cytotoxic effect of
MP has never been reported in MDA-MB-231 cells, a metastatic TNBC cell line. Therefore,
in this study, the effect of MP on MDA-MB-231 cells was first determined.
Methods
MDA-MB-231 cells were seeded in a number of 2,000 cells per well in 96-well plates
and incubated overnight at 37oC. The cells were then treated with a range of MP concentrations
from 0 to 8.5 μM for 24h and cytotoxicity was determined by a colorimetric MTT assay.
Absolute DMSO was used to break the formazan crystal formed and absorbance was measured
at 550nm using a microplate reader.
Results
The results show that within the concentration range tested, MP did not cause any
cytotoxic effect to MDA-MB-231 cells as indicated by a non-significant difference
in the percentage of cell viability compared to the control group (p>0.05). This indicates
that MDA-MB-231 cells are resistant to MP at least at this concentration range and
therefore, it is safe to be tested for anti-metastatic activity in the future.
Conclusions
It is confirmed that MDA-MB-231 cells are safe to be treated with MP at a concentration
of 0-8.5μM within 24h exposure. This is important to determine the inhibitory effect
of MP against the metastatic capability of TNBC cells.
Keywords: Triple-negative breast cancer, Breast cancer metastasis, Medroxyprogesterone
PPP12 Thymoquinone protects against cigarette smoke extract-induced vascular dysfunction
through inhibition of the RhoA/Rho-kinase signaling pathway
Mohamed A. El-Mahdy1, Gamal A. El Sherbiny2, Raed S. Ismail3, Ahmed M. Mansour3
1Center for Environmental and Smoking Diseases, College of Medicine, The Ohio State
University, Columbus, Ohio 43210, USA; 2Department of Pharmacology and Medicinal Chemistry,
Faculty of Pharmacy, Universiti Teknologi MARA, Cawangan Selangor, Kampus Puncak Alam,
42300, Malaysia; 3Department of Pharmacology and Toxicology, Al-Azhar University College
of Pharmacy, Cairo, Egypt.
Correspondence: Gamal A. El Sherbiny (gamal@uitm.edu.my)
Background
There is an ever-growing focus on the role of natural products in modulating reactive
oxygen species (ROS) and RhoA/Rho kinase-mediated vascular disease. Thymoquinone (TQ),
a constituent of the volatile oil derived from Nigella sativa seeds, possesses promising
antioxidant and vasodilating properties via its effect on multiple signaling pathways;
however, the effect of TQ on the RhoA/Rho-Kinase pathway remains to be investigated.
The aims of the present study were to examine whether TQ protects against CSE-induced
vascular dysfunction and to identify the underlying mechanisms of TQ on CSE-induced
ED in isolated rat aorta.
Methods
Cigarette smoke extract (CSE)-exposed rat aortic rings were mounted onto a wire myograph
and subjected to contraction and relaxation. Quantitative assessment of RhoA activation
was determined using G-LISA RhoA Activation Assay Kit. Phosphorylation of myosin light
chain-20, myosin phosphatase-targeting subunit 1 and protein kinase CPI-17 were determined
by Western blot analysis of the whole tissue protein extracts.
Results
TQ protected against CSE-induced impairment of acetylcholine-induced endothelium-dependent
relaxation, and decreased CSE-induced ROS generation and glutathione depletion. Preincubation
of aortic rings for 20 min with TQ attenuated the CSE-enhanced phenylephrine-induced
vascular tension in endothelium-denuded rings. TQ-pretreated rings showed a decrease
in CSE-induced RhoA activation and phosphorylation of myosin light chain-20, myosin
phosphatase-targeting subunit 1 and protein kinase CPI-17.
Conclusions
These data indicate that TQ inhibited ROS generation-induced RhoA/Rho kinase pathway
activation, protecting against CSE-induced vascular dysfunction. This study provides
mechanistic insight for understanding the molecular basis and efficacy of TQ on vascular
disease management.
Keywords: Thymoquinone, Cigarette smoke, RhoA/Rho kinase.
PPP13 A potential role of norethisterone (ED-4) as an anti-metastatic drug against
triple-negative breast cancer cells
Nuralia Sadiqin Lokmanulhakim1, Syed Muhammad Muzaffar Syed Mohd Hamdan1, Sharifah
Nurfazilah Wan Yusop1-2, Syed Adnan Ali Shah1-2, Nur Syamimi Ariffin1-2 Sadia Sultan1-2
1Department of Pharmaceutical Pharmacology and Chemistry, Faculty of Pharmacy, Universiti
Teknologi MARA, Puncak Alam Campus, Bandar Puncak Alam, 42300 Selangor, Malaysia;
2Atta-ur-Rahman Institute for Natural Product Discovery (AuRins), Universiti Teknologi
MARA, Puncak Alam Campus, Bandar Puncak Alam, 42300 Selangor, Malaysia
Correspondence: Sadia Sultan (drsadia@uitm.edu.my)
Background
Breast cancer is one of the most common malignant cancer in women. It is a heterogeneous
disease that affects one in every eight women worldwide. Breast cancer metastasis
is the most life-threatening aspect of breast cancer. It is a multiple step process
involving an invasion of a primary tumour cell and followed by a subsequent colonization
of the cell at the secondary sites in the body like bone, brain, liver, and lung.
It was hypothesized that norethisterone (ED-4) might have the ability to inhibit the
migration of metastatic breast cancer cells.
Methods
The MDA-MB-231 cells were treated with a range of ED-4 concentrations, from 0 till
8.5 μM, specifically, the cells were incubated with the drug for 18h at 37°C at the
concentration of 0, 2.5, 3.5, 4.5, 5.5, 6.5 and 8.5μM and their cytotoxicity was performed
using a colorimetric MTT assay.
Results
The result showed that ED-4 did not induce cytotoxicity on MDA-MB-231 cells within
the concentration range of 1μM up to 8μM (p>0.05). Therefore, ED-4 at this concentration
range can be used to determine its efficacy as anti-metastasis against triple negative
breast cancer cells.
Conclusions
To date, there is no drug available for a prevention of breast cancer metastasis and
therefore, norethisterone (ED-4) was proposed as a new drug candidate to inhibit breast
cancer metastasis. This potential could have benefits on future studies on the management
of breast cancer metastasis among breast cancer patients.
Keywords: Breast cancer, Norethisterone (ED-4), Triple Negative Breast Cancer, Metastasis,
MDA-MB-231 cells.
PPP14 Characterization and cytotoxic activity of semi-purified Fucoidan extract from
Sargassum polycystum C. Agardh (Sargassaceae) against Acute Myelogenous Leukemia (AMLK)
cell line using MTT assay
Cecilia D. Santiago, Mariane O. Magahis, Mica Anjanel R. Hernandez, Federica Angelica
T. Inciong, Justin Dave M. Manantan, Rachel Leah T. Menez, Vaniah Grace B. Soriano,
Jan Karlo T. Ecalne
School of Pharmacy, Centro Escolar University, Mendiola, Manila, Philippines
Correspondence: Cecilia D. Santiago (cdsantiago@ceu.edu.ph)
Background
Leukemia is one of the most prevalent cancer types for Filipinos becoming the 7th
leading form of cancer in both sexes. In 2012, the Philippines estimated national
standardized mortality of leukemia were of 3.9 per 100,000. The brown macroalgae specifically
from the Sargassum are considered as rich sources of phytochemicals such as Fucoidan
and Fucoxanthin that act on multi-signaling pathways needed to combat cancer.
Methods
Isolation of the semi-purified Fucoidan extract was based on a process developed by
Mak. W. (2012), in which pre-treatment of the sample with ethanol, precipitation with
Calcium Chloride and ethanol concentrations, with centrifugation steps in between.
The study evaluated the physicochemical characteristics including the following: i)
organoleptic, ii) solubility, iii) phytochemical assay, iv) fucose, sulfate and glucoronic
content using UV-VIS spectroscopy, instrumental analysis using Fourier Transform Infrared
Spectroscopy (FTIR) and the cyototoxic activity of semi purified Fucoidan extract
against Acute Myelogenous Leukemia (AMLK) cell line using MTT assay using doxorubicin
as the positive control.
Results
The obtained percentage yield showed that 440.15 g of the pretreated Sargassum polycystum
contained 1.13% semi-purified fucoidan extract. Solubility test confirm the solubility
of the extract to water and hydrochloric acid. The semi-purified Fucoidan isolate
was characterized of its fucose, sulfate, and glucuronic acid content, with results
of 26.23%, 23.52%, and 32.71%, respectively. FTIR spectrum confirms the presence functional
moieties i.e. isothiocyanate and sulfonyl that are also found on fucoidan standard
and sulfated polysaccharides, these functional groups may be attributed to the different
biological activities that Fucoidan exhibits. Cytotoxic activity was evaluated using
MTT assay, wherein results showed that the semi-purified Fucoidan extract from S.
polycystum C. Agardh (Sargassaceae) exhibits cytotoxic activity against AMLK cell
line, with concentration of 6.25 μg/mL having the highest inhibitory rate of 44.08%.
Statistical treatment showed significant difference between the semi-purified Fucoidan
extract and the standard drug, doxorubicin.
Conclusions
In conclusion, the semi-purified Fucoidan extract from S. polycystum C. Agardh (Sargassaceae)
may exhibit anti-proliferative effect against AMLK cell line.
Keywords: Sargassum, Cytotoxicity, Fucoidan, MTT assay, AMLK cell line
PPP15 Formulation of antibacterial ointment from the ethanolic crude extract of ikmo
leaves (Piper betle Linn. Piperaceae family)
Mylene S. Andal, Lois Stephanie B. Calalo, Paola Noreen A. Dela Merced, Ezli Laine
F. Perez, Gary Jr. C. Quebec, Serie S. Shimomura, Regine F. Valderama, Cecilia D.
Santiago
School of Pharmacy, Centro Escolar University, Manila, Philippines
Correspondence: Mylene S. Andal (maandal@ceu.edu.ph)
Background
According to World Health Organization cases of Antimicrobial Resistance (AMR) have
exponentially increased yet fewer antibacterial agents are discovered on the past
years. AMR hampers the control of infectious diseases resulting to an increase in
health care cost and risk of spreading resistant microorganisms in the community,
these events is a growing public health challenge and poses a global health crisis
if remain uncontrolled. Ikmo leaves on the otherhand has been well studied and has
shown abundant and potential source of phytoconstituents that may be developed as
antimicrobial agent and incorporate it to an applicable dosage form, therefore to
address this concern the researchers formulate a plant-derived antibacterial ointment
from the ethanolic crude extract from Piper betlle locally known as Ikmo.
Methods
Mature Ikmo leaves were collected, dried and extracted. The extract was then subjected
to physicochemical characterization and antibacterial assay by means of agar-plate
method. The plant concentration that exhibits the most active effect against Staphylococcus
aureus and Pseudomonas aeruginosa (p<0.05) will be used in the formulation of antibacterial
ointment. To ensure the safety of the formulated product, initial dermal irritation
test was conducted using rabbits.
Results
The yield of ethanolic extract of Ikmo leaves extract is 9.922% and is found to have
greenish-black color, creosote-like odor and has syrupy consistency. The ethanolic
crude extract was soluble in acetone, ethanol, and ether and insoluble in water. The
optimized extract concentration of 60% was further develop to ointment and is the
subjected to antibacterial assay against Staphylocococcus aureus and Pseudomonas aeruginosa
resulting to a zone of inhibition of 23.05±1.35 mm and 26.40±0.89 mm compared to mupirocin
(14.93 ±0.03 mm and 17.55±0.03 mm). Dermal irritation test has also shown that the
formulated extract does not show any skin reactions to test animals.
Conclusion
Based on the result of the study, the formulated ointment of the optimized ethanolic
crude extract of Ikmo leaves has shown to be a potential agent to be further studied
considering its good preliminary antibacterial effect and dermal irritation test.
Keywords: Piper betle Linn. Ikmo leaves, Staphylococcus aureus, Pseudomonas aeruginosa,
antibacterial, ointment
PPP16 Antibacterial activity of Musa paradisiaca stem extracts against isolated UTI
pathogens
Anita Gnana Kumari, Logananthini
Department of basic sciences, Faculty of pharmacy, KPJ Healthcare University College
(KPJUC), Kotaseremas, Nilai, 71800, Malaysia
Correspondence: Anita Gnana Kumari (av.anita@kpjuc.edu.my)
Background
Urinary tract infection (UTI) has become a more serious problem today, due to multidrug
resistance of Gram-positive (GP) and Gram-negative (GN) bacteria. Musa paradisiaca
is used as a medicinal plant in traditional system of healing many infectious diseases.
The goal of our research was to evaluate antimicrobial efficiency of Musa paradisiaca
(banana) stem extracts against isolated UTI pathogens.
Methods
Banana stem extracts were obtained with maceration technique using two solvents separately:
distilled water and methanol . Agar well diffusion assay was used for evaluation of
antimicrobial properties of stem extracts against isolated UTI pathogens. Minimum
inhibitory concentrations and minimum bactericidal concentrations were determined
by broth dilution method and agar plate method. The preliminary phytochemical analyses
of the plants were carried out using standard procedure.
Results
A total of 5 UTI pathogens were isolated from the UTI patients attending in the hospital
such as Pseudomonas aeruginosa, Klebsiella pneumoniae, E. coli, Enterococcus faecalis
and Staphylococcus aureus. Aqueous and ethanol extracts expressed antimicrobial activity
against isolated UTI pathogens except S.aureus at 500 mg/ml. Zone of inhibition of
the extracts were compared with ciprofloxacin (250mg/ml). Ethanolic extracts of M
paradisiaca inhibited the growth of P. aeruginosa and E. faecalis at 62.5 mg/ml and
K. pneumoniae at 125 mg/ml. Aqueous extracts of M paradisiaca inhibited the growth
of K. pneumoniae and E.coli at 250mg/ml. Ethanol extracts of M. paradisiaca exhibited
bactericidal activity against P. aeruginosa and E. faecalis at 250 mg/ml. Ethanolic
extracts exhibited better antibacterial activity against tested strains than water
extracts. The antibacterial activity of the M paradisiaca was due to the presence
of alkaloids, tannins, flavanoids, terpenoids and sugars.
Conclusions
Hence, the plant M. paradisiaca stem contains potential antimicrobial compounds against
UTI pathogens.Further study is required to identify the bioactive compounds, mode
of action and in vivo toxic effect of M. paradisiaca.
Keywords: antibacterial activity, M paradisiaca stem extracts, minimum inhibitory
concentration, phytochemicals
PPL2 Locomotor, exploratory and anxiety-like behavior assessment of aged rats following
intrahippocampal injection with streptozotocin: A novel Alzheimer’s disease rodent
model
Mazzura Wan Chik1, Nur Hidayah Elias1, Nur Faiqah Fauzi1, Nurul Aqmar Mohd Nor Hazalin1,
Gurmeet Kaur Surindar Singh1,2,
1 Department of Pharmaceutical Life Sciences, Faculty of Pharmacy, Universiti Teknologi
MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia; 2Brain Degeneration and
Therapeutics Group, Pharmaceutical and Life Sciences Community of Research, Universiti
Teknologi MARA (UiTM), 40450, Shah Alam, Selangor
Correspondence: Gurmeet Kaur Surindar Singh (gurmeet9952@uitm.edu.my)
Background
Alzheimer’s disease (AD) is a progressive neurodegenerative disorder associated with
a series of pathophysiological changes, accumulation of amyloid plaques and tau tangles.
The hippocampal region which is responsible for long-term memory and spatial navigation
demonstrated neuronal loss in AD patients. Peripheral exposure of streptozotocin (STZ)
used in diabetic studies showed AD pathogenesis in 8 months. A reliable AD rat model
should resemble the brain metabolic and behavioral disturbances in humans. Thus, the
present study was conducted to investigate the effects of intrahippocampal (IH)-STZ
administration that directly target the insulin receptors on the locomotor activity
and anxiety-like behavior at two time points (3 and 12 weeks) post-STZ injection.
Methods
Forty-male (12 months old) Sprague-Dawley rats (350-450 g) were divided into two groups
to monitor the progression of AD at two time points (3 weeks and 12 weeks, n=20 respectively).
The rats were further divided to control (no treatment, n=5), sham-operated (received
PBS, n=5) and treatment (IH-STZ, n=10). STZ (3 mg/kg; 5 μl) was administered bilaterally
as a single injection into the dorsal hippocampus of the rats using a stereotaxic
apparatus. The open field test using the open square maze (50 cm x 50 cm) tracked
with software (ANY-maze) was used to record the rat’s behavior.
Results
There were no significant differences in spontaneous locomotor, exploratory activity
and time spent in the central area between the groups. Rats from group 3 and 12 weeks
also did not show significant changes in all the parameters when compared between
the two time points (p < 0.05).
Conclusions
STZ when administered intrahippocampally did not impair the rats’ locomotor activity,
absent of any signs of anxiety and exhibited normal exploratory behavior. The rodent
IH-STZ is a suitable model to study treatment and prevention of AD as the behavior
and pathology resembled AD patients.
Keywords: Alzheimer’s disease, Intrahippocampal, Rodent model, Streptozotocin, Locomotor
PPL3 Machine learning based prediction of potential interaction between leukaemia-related
proteins and Centella asiatica compounds
Norodiyah Othman1,2, Mohd Ilham Adenan3, Fazlin Mohd Fauzi
1
1Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Selangor Branch, Puncak Alam
Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia; 2Haematology Unit, Cancer Research
Centre, Institute for Medical Research (IMR), 50588 Kuala Lumpur, Malaysia; 3Faculty
of Applied Sciences, Universiti Teknologi MARA (UiTM), Shah Alam, 40450 Selangor,
Malaysia
Correspondence: Fazlin Mohd Fauzi (fazlin5465@uitm.edu.my)
Background
Leukaemia is one of the leading causes of morbidity and mortality in adult and children
worldwide. Finding specific targets for anti-leukaemic activity is challenging, due
to the limited understanding of target selectivity features and compounds. For this
purpose, a one vs one (OvO) classification model was built on bioactivity data of
23 leukaemia-related proteins to assess potential compound-target interaction of 4
main Centella asiatica compounds.
Methods
An OvO classification model was trained on bioactivity data containing protein-ligand
interactions between 23 leukaemia-related proteins and 17,637 compounds. The data
was obtained from ChEMBL (https://www.ebi.ac.uk/chembl/) database. The compounds were
converted to ECFP_4 fingerprint and Random Forests was used as the machine learning
algorithm to deduce a mathematical correlation between compound structure and protein
receptor in the training set. The model was validated using a 5-fold cross validation
and potential target interaction of C. asiatica compounds; Asiaticoside, Madecassoside,
Asiatic acid and Madecassic acid were then identified using the model.
Results
In the internal validation, the OvO model exhibited an average sensitivity of 0.87,
specificity of 0.96, q2 value of 0.57, and root-mean-square error (RMSE) of 0.22.
In the prediction of potential protein targets for C. asiatica compounds, 3 potential
proteins (CHEMBL1997, CHEMBL1825 and CHEMBL2034) may interact with the tested compounds.
The next phase of the study will involve testing the 4 compounds against the 3 predicted
proteins in vitro.
Conclusions
Machine learning based prediction of interaction between protein target and bioactive
compounds may serve as a valuable tool in searching for potential lead compounds in
leukemic diseases.
Keywords: One vs one classification; target prediction; machine learning; interaction;
leukaemia-related protein
PPL4 Centella asiatica extract (CAE) improves motor performance of methamphetamine-treated
rats
Nursyamila Shamsuddin1, Mohd Shihabuddin Ahmad Noorden1, Mazatulikhma Mat Zain2
1Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam,
Selangor, Malaysia; 2Institute of Science (IOS), Universiti Teknologi MARA (UiTM),
40450 Shah Alam, Selangor, Malaysia
Correspondence: Mohd Shihabuddin Ahmad Noorden (shiha@uitm.edu.my)
Background
Methamphetamine or METH, a psychostimulant with devastating neurotoxic effects on
the central nervous system. METH’s abuser has been associated with Parkinson’s disease
(PD)-like motor deficits. Centella asiatica or “pegaga” is remarkably known to improve
behavioural and motor impairment.Therefore, in this study, narrow beam test was performed
to evaluate motor performance of rats following METH and CAE treatments.
Methods
Male Sprague-Dawley rats were assigned into Group I (Control), Group II (50mg/kg METH
twice per day for 4 days), Group III (300mg/kg CAE for 21 days), Group IV (500mg/kg
CAE for 21 days), Group V (50mg/kg METH + 300mg/kg of CAE for 21 days) and Group VI
(50mg/kg METH + 500mg/kg CAE for 21 days). Rats were subjected to narrow beam test
on the 1st day after the last treatment. Rats were placed at the initial start of
wooden narrow beam with smooth surface of 100cm in length and 6mm in width and 100cm
of height. Total time of 120s was set as a maximum limit. Time taken for each rat
to cross beam or reach escape box (escape latency) was recorded. Error was recorded
as any failed attempt to reach escape box, loss of balance and fall from the beam
before 120s of maximum total time. P<0.05 was indicated as statistically significant.
Results
No significant change of body weight was observed on each treatment group. All rats
were able to perform in the narrow beam test. A longert time taken for escape latency
was showed by Group II, V and VI compared to control group. Group III and IV were
showed significant shorter time for escape latency as compared to Group II. Meanwhile,
Group II was exhibited significant increases in the number of error and difficulties
as compared to control group.
Conclusions
Results demonstrated that CAE able to improve motor performance of METH-treated rats.
Keywords: Methamphetamine, Centella asiatica extract, motor performance, narrow beam
test
PPL5 Intrahippocampal administration of streptozotocin induces spatial learning and
memory impairment in rats
Norhazwani Mohd Zaid1, Gurmeet Kaur Surindar Singh2,3, Mazzura Wan Chik3, Nurul Aqmar
Mohamad Nor Hazalin2
1Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam,
Selangor, Malaysia; 2Department of Pharmaceutical Life Sciences, Faculty of Pharmacy,
UiTM, 42300 Bandar Puncak Alam, Malaysia; 3Brain Degeneration and Therapeutics Group,
Pharmaceutical and Life Sciences Community of Research, UiTM, 40450, Shah Alam, Selangor,
Malaysia
Correspondence: Nurul Aqmar Mohamad Nor Hazalin (nurulaqmar@uitm.edu.my)
Background
Alzheimer’s disease (AD) is the most common neurodegenerative disorder characterized
by a progressive decline of memory, cognitive impairments, and changes in behaviour
and personality. The past decade has seen extensive intervention directed to AD treatment,
but with little success to fully cure AD. In the search for new therapeutic interventions
and to better understand the disease, various animal models have been developed. The
ideal AD model should mimic the pathological aspects of human AD. Intracerebroventricular
(ICV) injection of streptozotocin (STZ) has been widely used to induced sporadic AD
in the rodent. However, insulin receptors (IR) which are very sensitive to STZ are
more abundant in the hippocampal region but there have been no studies on the effect
of intrahippocampal (IH) injection of STZ. Therefore, the present study was conducted
to investigate the effects of bilateral IH injection of STZ on spatial reference learning
and memory in rats.
Methods
Male Sprague Dawley rats (350–4 50g) were administered with a single bilateral intrahippocampal
injection of STZ (3 mg/kg) or an equal volume of PBS. Two weeks post-surgery, the
spatial learning and memory of the rats were assessed using the Morris Water Maze
task.
Results
Rats subjected to bilateral IH-STZ injection took longer latency to locate the hidden
platform in acquisition trials and spent less time in the target quadrant than the
control group which indicate impaired spatial memory retention.
Conclusions
The present study demonstrates the potential of STZ to promote spatial learning and
memory impairment in rats through IH injection that can be used as a reliable rodent
model for AD.
Keywords: Alzheimer’s Disease, Memory, Rat Model, Streptozotocin, Morris Water Maze
PPL6 Ceftriaxone attenuates oxidative stress and enriched antioxidants in memory dysfunction
in aging rodent models
Rohana Che Nordin1, Abu Bakar Abdul Majeed1,, Kalavathy Ramasamy2, Vasudevan Mani3,
Atish Prakash4,
1Brain Degeneration & Therapeutic Group and 2Collaborative Drug Discovery Research
(CDDR) Group, Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Puncak
Alam, Selangor, Malaysia; 3Department of Pharmacology and Toxicology, College of Pharmacy,
Qassim University, Buraidah 51452, Kingdom of Saudi Arabia; 4Johns Hopkins School
of Medicine, 733 N Broadway, Baltimore, MD 21205, USA
Correspondence: Rohana Che Nordin (anazahari@gmail.com)
Background
Excessive zinc (Zn) levels in the brain are known to impair cellular energy production
through an inhibitory action on mitochondria. Mitochondrial dysfunction is known to
be a factor in the pathogenesis of neurodegenerative disorders, like Alzheimer’s disease
(AD). Zn is an essential trace element in the brain, however, too much Zn has been
associated with the pathogenesis of AD. Similarly, a surplus of glutamate has also
been implicated in the development of AD. Ceftriaxone (CTX) is a beta lactam antibiotic
with neuroprotective activity. The aim of this study was to investigate the effectiveness
of CTX compared to donepezil (Don), an established drug for alleviating AD symptoms,
in improving memory impairment induced by an excess of Zn in the senescent mice model.
Method
In this study we applied a behavioural tool, Morris Water Maze (MWM), followed by
biochemical assays. The MWM task is a widely accepted method for investigating spatial
learning and memory of rodents by measuring escape latency (EL), distance travelled
(DT), the distance travelled before reaching the platform; and the time spent in the
target quadrant (TQ). Accelerated senescence was induced through subcutaneous injection
of d-galactose (D-gal) and oral administration of Zn daily for six weeks, an established
model of aging. Mice were divided into 5 groups: the memory intact, untreated wild
type (WT); memory-impaired via Zn-D-gal combination (control); and Zn-D-gal induced
memory impaired treated with donepezil (Don) or 100 mg/kg (CTX-100) or 200 mg/kg (CTX-200)
ceftriaxone. On days 35 to 37 of the treatment, all groups were put through MWM test.
Results
Based on the MWM test, treatment with CTX provides protection against Zn-D-gal induced
toxicity. Both CTX-100 and CTX-200 groups appeared to have reversed memory impairment
in the Zn-D-gal treated animals, evidenced by the shorter EL and DT, and longer TQ
compared to the control group. The Don group also had improved memory. However, these
improvements did not exceed the performance of the WT. The levels of lipid peroxidation
and nitrite estimation were increased in the disease model while the superoxide dismutase
(SOD) and reduced gluthathione were decreased, in these groups compared to groups
treated with Don and CTX.
Conclusion
CTX provides protection against Zn-D-gal-induced toxicity, presumably by alleviating
mitochondrial dysfunction of this model.
Keywords: Ceftriaxone, Zinc, Neurotoxicity, Alzheimer’s Disease, D-galactose
PPL7 Tth111i Single nucleotide polymorphism (SNP) among Malay subjects as detected
by polymerase chain reaction (PCR) and DNA sequencing methods
Siti Nooraishah Hussin, Nor Syuhada Shaari, Siti Zuhairah Zainuddin
1Department of Life Science, Faculty of Pharmacy, UiTM Cawangan Selangor, Kampus Puncak
Alam, 42300 Bandar Puncak Alam, Selangor
Correspondence: Siti Nooraishah Hussin (nooraishah0352@uitm.edu.my)
Background
Glucocorticoid receptor (GR) plays an integral role in regulating body functions.
Polymorphism of the Tth111I theoretically increases the sensitivity of the GR receptor,
with prominent evidence at higher HDL-C levels. Thus, this study aims to screen and
to find the Tth111I SNP association with the HDL-C level by using polymerase chain
reaction (PCR) and DNA sequencing methods among Malay subjects.
Methods
DNA was extracted and amplified from blood samples of 24 Malay subjects, which consist
of 12 normal lean and 12 obese respondents.
Results
Among the ten sequenced samples however, none was detected as mutant. Since, all the
samples were wild-types (WTs), hence, the association between the Tth111I SNP with
the HDL-C level could not be made.
Conclusions
A larger sample size must be recruited, and further studies need to be conducted to
determine the impact of this SNP on the HDL-c level to explain the potential roleof
Tth111I SNP in preventing cardiovascular disease (CVD) among the Malay Malaysians.
Keywords: glucocorticoid receptor gene, single nucleotide polymorphism, Tth111I, HDL-C
PPL8 Ciproxifan protects the effects of D-galactose/aluminium chloride-induced memory
impairment in mice through BDNF and neuronal cell marker
Suraya Mohd Noh1,2, Abu Bakar Abdul Majeed1,2, Kalavathy Ramasamy1,2 , Vasudevan Mani3
1Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300
Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia; 2Brain Degeneration and Therapeutics
Group, Collaborative Drug Discovery Research (CDDR) Group, Pharmaceutical & Life Sciences
CoRe, Universiti Teknologi MARA (UiTM), 40450 Shah Alam, Selangor Darul Ehsan, Malaysia;
3Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University,
Buraidah 51452, Kingdom of Saudi Arabia.
Correspondence: Suraya Mohd Noh (sue_adam90@yahoo.com)
Background
Alzheimer’s disease (AD) type of dementia is related to β-amyloid deposition and formation
of neurofibrillary tangles leading to the neuronal loss. Currently, only a handful
of drugs are used to treat AD such as antagonists of acetylcholinesterase (AChE) and
NMDA. Histamine H3-receptor is an autoreceptor that controls the brain histamine release
as well as other neurotransmitters such as acetylcholine and dopamine (heteroreceptor).
Ciproxifan is a H3-receptor antagonist that binds to the receptor and induces more
histamine to be released, by blocking the negative feedback inhibition. It has also
been shown to enhance cognition and memory.
Methods
Combination of D-galactose (D-gal) and aluminum chloride (AlCl3) was used to induce
memory impairment in ICR mice. Groups of mice were injected with ciproxifan (1 & 3
mg/kg, i.p.) for 42 consecutive days and administered with D-galactose by subcutaneous
injection (100 mg/kg, s.c.) for 42 days, while AlCl3 (100 mg/kg) was added in the
water bottle, except for control. After 42 days, brain samples were harvested to determine
the levels of brain-derived neurotrophic factor (BDNF)) and mRNA of PSD-95 and MAP2.
Results
Level of BDNF in the D-gal/AlCl3 group was significantly lower (P <0.01) than the
control group. Conversely, BDNF levels in ciproxifan-treated mice (1 mg/kg and 3 mg/kg)
were significantly higher (P < 0.01 and P <0.001, respectively) than the D-gal/AlCl3
group (negative control). Also, the administration of ciproxifan (3 mg/kg) in D-gal/AlCl3-induced
mice significantly upregulated the mRNA expression of PSD-95 gene (P<0.05) as compared
to the control group. Moreover, the mRNA expression of MAP2 gene was significantly
upregulated in ciproxifan-treated mice (1 mg/kg and 3 mg/kg) as compared to the control
group (P <0.05 and P<0.01, respectively).
Conclusions
Ciproxifan may have the potential to increase neuronal activity through enhancement
of the BDNF signaling pathway and neuronal cell markers (PSD-95 and MAP2).
Keywords: histamine H3-receptor antagonist, ciproxifan, memory impairment, Brain-Derived
Neurotrophic Factor (BDNF), PSD-95, MAP2
PPL9 Amyloid-beta aggregation inhibitory compounds isolated from fermented tea (Camellia
japonica)
Kee Dong Yoon
College of Pharmacy and Integrated Research Institute of Pharmaceutical Sciences,
The Catholic University of Korea, Bucheon, 14662, Republic of Korea
Correspondence: Kee Dong Yoon (kdyoon@catholic.ac.kr)
Background
Alzheimer's disease (AD) is a progressive neurodegenerative disorder, and is associated
with the formation of amyloid-β (Aβ) plaques which are generated from the cleavage
of amyloid precursor protein. Thus far, (–)-epigallocatechin gallate(EGCG), curcumin
and resveratrol are some of the natural product based compounds that possess inhibitory
activities against Aβ aggregation. The current study was desingned to discover Ab
aggregation inhibitory compounds from fermented tea (Camellia japonica).
Methods
Fermented tea was provided by Amore Pacific Co., and was extracted using acetone and
ethanol. The etanol soluble extract was separated by diverse column chromatography
methods. Isolated compounds were identifed by interpretation of spectroscopic data
including one-, two-dimentional NMR, UV, IR and ESI-Q-TOF-MS. Amyloid-beta aggregation
inhibitory activity was evaluated using Thioflavin T beta-amyloid aggreation kit and
negative -stained transmission electron microscopy. The protective effect of the compounds
was tested in Aβ-treatedSH-SY5Y cells by estimating the viability using the CCK-8
assay kit.
Results
Phytochemical investigation of the fermented tea led to isolation of 31 phenolic compounds
including three new flavonoid glycosides. Among the compounds,, (–)-catechin gallate
(CG), (–)-epicatechin gallate (ECG), and (–)-epigallocatechin gallate (EGCG) showed
strong Aβ aggregation inhibitory effect whilstCG exhibited high protection in SH-SY5Y
cells against Aβ-induced cytotoxicity.
Conclusions
CG and ECG showed more potent anti- Aβ aggregation effects than EGCG, a well-known
natural Aβ aggregation inhibitor. The current study provides scientific evidences
that compounds from fermented tea possess beneficial actions against neurodegeneration
in vitro.
Keywords:
Camellia japonica, phenolic compounds, anti-Aβ aggregation
Copyright permission
The content of this study was published [Phytochemistry 160 (2019) 11–18] previously
but received the copyright permission from Elsevier Copyright Clearance Center (licence
# 4631220464146) for the poster presentation.
PPL10 Agmatine prevents mitochondrial dysfunction in 3-nitropropionic acid-induced
experimental Huntington’s Disease
Nor `Awatif Osmanudin 1,2, Atish Prakash 2,6 , Vasudevan Mani 5 , Kalavathy Ramasamy
1,3,4 , Abu Bakar Abdul Majeed 1,2,4
1Faculty of Pharmacy, Puncak Alam Campus, Universiti Teknologi MARA (UiTM), 42300
Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia; 2Brain Degeneration and Therapeutics
Group &; 3 Collaborative Drug Discovery Research (CDDR) Group; 4Pharmaceutical Life
Sciences CoRe, Universiti Teknologi MARA (UiTM), 40450 Shah Alam, Selangor Darul Ehsan,
Malaysia; 5Department of Pharmacology and Toxicology, College of Pharmacy, Qassim
University, P.O. Box 6800, Buraidah, 51452, Kingdom of Saudi Arabia; 6John Hopkins
School of Medicine, Baltimore, Maryland, United State of America
Correspondence: Nor `Awatif Osmanudin (awatif.osmanudin@gmail.com)
Background
Huntington’s disease (HD) is an inherited genetic disorder, caused by the mutation
of abnormally expanded and unstable CAG repeat within the coding region of the huntingtin
protein gene. At the molecular level, mitochondrial dysfunction plays a significant
role in the pathogenesis of HD. 3-nitropropionic acid (3-NP) is a neurotoxin which
induces neurodegeneration in the animal model of Huntington’s disease (HD). It is
an irreversible inhibitor of mitochondrial complex II (SDH) enzyme of the electron
transport chain. Agmatine is the metabolite of arginine by arginine decarboxylase
and has been suggested to be a neuroprotective agent. The objective of this study
was to investigate the protective effect of agmatine on 3-NP-induced neurodegeneration
through the estimation of mitochondrial enzymatic profile in Wistar rats.
Methods
The experimental protocol design includes systemic 3-NP (10 mg/kg, i.p.) treatment
thrice, i.e. on day 1, 5 and 9. Agmatine (40 and 80 mg/kg) was also given i.p. daily,
from day 9 to day 15.
Results
Enzymatic levels in mitochondrial complexes-I, II, III and IV were found to be significantly
lowered in the brain of rats treated with 3-NP. Mitochondrial SDH contributes to cell
viability reduction, hence, the decrease of cell viability approves irreversible inhibition
of SDH by 3-NP. The level of enzymes of all complexes in groups treated with agmatine
(40 and 80 mg/kg) was significantly increased.
Conclusion
The present study provides evidence that agmatine exerts protective action over 3-NP-induced
neurodegeneration by preventing mitochondrial dysfunction and thus, may be potentially
used as a neuroprotective agent.
Keywords: Huntington’s disease, 3-NP, agmatine, mitochondrial dysfunction
PPL11 Towards the discovery of novel dengue NS3 antiviral drug: Application of proteochemometric
(PCM) modelling and in vitro validation in drug repurposing
Zafirah Liyana Abdullah1, Chee Hui Yee2, Fazlin Mohd Fauzi1
1Department of Pharmaceutical Pharmacology and Chemistry, Faculty of Pharmacy, Universiti
Teknologi MARA, Selangor Branch, Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor,
Malaysia; 2Department of Microbiology and Parasitology, Faculty of Medicine and Health
Sciences, Universiti Putra Malaysia, 43400 Serdang, Selangor, Malaysia
Correspondence: Fazlin Mohd Fauzi (fazlin5465@uitm.edu.my)
Background
The current treatment for DENV infection is only supportive care involving fluid replacement,
analgesics and bed rest. Dengvaxia®, a DENV vaccine was recently approved by FDA but
its usage is age-limited and only for patients with confirmed previous dengue infection.
Antivirals for DENV infection that can reducethe risk of severe cases of patients
from any background is crucial. Hence this study aims to screen currently available
drugs (a process known as drug repurposing) for potential antiviral activity that
targets the NS3 protease of DENV through proteochemometric (PCM) modeling and subsequent
in vitro validation.
Methods
The PCM model was built on a training set which comprises of 62,746 bioactivity data
from ten serine proteases available from public databases. Aitchison-Aitken kernel
and sequence identity were used to calculate chemical and biological similarity respectively
while Parzen-Rosenblatt Window was used as the classification algorithm. The performance
of the model was validated to measure the accuracy of the prediction model. Drugs
from the SWEETLEAD database were then screened for potential activity against NS3
protease using the validated model and further tested in vitro for their ability to
inhibit DENV activity. Molecular docking was performed to model the interaction between
drugs and NS3 protease.
Results
The performance of the model was validated internally (goodness of fit RMSE = 0.315,
predictive ability Q2 = 0.567) and externally (RMSE = 0.466, and Q2 = -1.509). The
screening showed that Zileuton and Trimethadione have the potential as antiviral with
good binding affinity at the active sites. The in vitro assay further validated that
Trimethadione possess better anti-DENV activity with 80% foci reduction when tested
at 20 mM drug concentration.
Conclusions
Drug repurposing through PCM modelling is a promising technique to accelerate the
discovery of novel dengue antiviral drug.
Keywords: Dengue virus, antiviral drug, proteochemometric (PCM) modelling, drug repurposing
This project is funded by the Ministry of Education of Malaysia with Universiti Teknologi
MARA (UiTM) through the Fundamental Research Grant Scheme (FRGS; 600-RMI/FRGS 5/3
(0020/2016).
PPL12 Amplification of purine rich site from COL4A3 gene for triple helix study in
keratoconus eye disease
Mohd Shihabuddin Ahmad Noorden, Qishtina Mizan, Nur Serene Sofia Nor Azri, Fazleen
Haslinda Mohd Hatta
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM), 42 300 Bandar Puncak Alam,
Selangor, Malaysia
Correspondence: Mohd Shihabuddin Ahmad Noorden (shiha@puncakalam.uitm.edu.my)
Background
Keratoconus (KC) eye disease is a non-inflammatory disorder characterized by eye bulging
due to corneal thinning and results in blurred vision and astigmatism. Several factors
lead to KC development include genetic factor and polymorphism of COL4A3. Triple helix
is DNA structure where third single strand of DNA fragment bind to the purine rich
site of DNA duplex in reverse Hoogsteen hydrogen bonds. This triplex structure is
enable to suppress gene expression by inhibiting the initiation of transcription.
The objective of the study was to identify and amplify the purine rich site in COL4A3
gene.
Methods
The desired purine rich site of COL4A3 gene was amplified using designed PCR primers
based on sequence from NCBI (NG_011591.1). The PCR steps were repeated for 30 cycles
by using 54.5 oC annealing temperature (Tm). The amplicon then subjected for 1% agarose
gel electrophoresis for DNA separation and observed under UV light through ethidium
bromide staining before advancing for sequencing.
Results
The PCR product bands with size of 429 nucleotides were successfully observed. Based
on the sequencing analysis, 88.8% of amplicon aligned with original sequence from
NCBI and there was one base deletion from the amplicon. This shows that the purine
rich region of COL4A3 gene was successfully amplified.
Conclusions
Results demonstrated that the purine rich region of COL4A3 gene was successfully identified
and amplified and it can be used as triple helix forming oligonucleotides binding
site.
Keywords: keratoconus eye disease, COL4A3 gene, triple helix
PPL13 Photodamage attenuating effects of marine endophytic fungus (MV) fractions against
fibroblast cell line
Asma Genari@Azhari, Siti Alwani Ariffin
Marine Pharmaceutical Research Group (Mareg), Department of Life Sciences, Faculty
of Pharmacy, Universiti Teknologi MARA (UiTM), 42300 Bandar Puncak Alam, Selangor,
Malaysia
Correspondence: Siti Alwani Ariffin (alwani229@uitm.edu.my)
Background
Over exposure to sunlight increased UVB radiation, lead to potential photoaging and
skin cancer. As these trends are likely to continue for the foreseeable future, the
adverse effect of UVB has become a major human health concern.
Methods
Marine endophytic fungus isolated from red seaweed, Gracilaria arcuata Zanardini (MV)
collected from Port Dickson, Negeri Sembilan, Malaysia was investigated for its potential
in attenuating the photodamage effects of UVB against fibroblast (CRL 2522) cell line
by MTT assay.
Results
The aim of this study was to investigate the potential of marine endophytic fungus
(MV) fractions in stimulating DNA repair of CRL 2522 cells against UVB-induced DNA
damage. About 13 of MV fractions showed increased of CRL 2522 cell viability (70-80%)
after 30 min exposure to UVB radiation. Five of fractions (MV14, MV35, MV41, MV45
and MV50) significantly increased (p<0.05) cell viability. These data suggest a greater
potential of marine endophytic fungus (MV) fractions in stimulating DNA-repair against
UVB-induced damaging cells. Further study of these 13 active fractions should be carried
out to determine the photodamage attenuating effects of MV fractions against fibroblasts
and Hacat cell lines.
Conclusions
These five potential MV fractions might be useful as a starting point for developing
dermatological products to prevent oxidative skin damage.
Keywords: seaweed, marine endophytic fungi, photodamage, UVB
PPC1 The study of effect of method and time of extraction on antioxidant, total phenolic
content and total flavonoid content of Ficus deltoidea
Muhammad Fikriey Bin Shafie1 , Kamran Ashraf 1,2
1
Department of Pharmacology & Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA, Campus Puncak Alam, Selangor Darul Ehsan, Malaysia;
2
Atta-urRahman Institute for Natural Products Discovery (AuRIns), Universiti Teknologi
MARA, Puncak Alam Campus, Bandar Puncak Alam, Selangor Darul Ehsan, Malaysia
Correspondence: Kamran Ashraf (kamran1368@uitm.edu.my)
Background
Ficus deltoidea is a well-known medicinal plant which has long been used by the Malay
community in treating various health problems. Due to its antioxidant property and
the presence of phenolics and flavonoids, the plant contributes the various biological
activities. These properties vary significantly with different extraction methods
and time. This study aimed to evaluate the effect of method and time of extraction
on antioxidant, total phenolic content (TPC) and total flavonoid content (TFC) of
Ficus deltoidea.
Methods
Different extraction methods like continuous shaking extraction (CSE) with time (30,160
and 360 min), ultrasonic extraction (USE) with time (5, 15 and 30 min) and microwave
assisted extraction (MAE) with time (1, 3 and 5 min) were applied to see the effect
on total antioxidant activity, TPC and TFC quantitatively. The antioxidant and total
phenolic and total flavonoid content of extracts were evaluated by DPPH (2,2-diphenyl-1-picrylhydrazyl)
radical scavenging activity, Folin-Ciocalteu and aluminum chloride (AlCl3) tests,
respectively.
Results
The microwave extraction method provided good extractive yield, superior scavenging
activity and higher yield of TPC and TFC compared to the other two methods used. The
outcome of this experiment also indicates that TPC and TFC increases as the increase
in extraction time in each different methods of extraction.
Conclusions
MAE showed good results even in shorter time of extraction may be due to the rapid
heating mechanism of microwave. The hot solvent produced in MAE penetrated easily
into the matrix and extract compounds from the lysed plant cells. Therefore, the MAE
method is more efficient in extracting phenolic and flavonoid compounds and showed
better antioxidant effect compared to USE and CSE methods.
Keywords:
Ficus deltoidea, antioxidant, total phenolic content, total flavonoid content, microwave
assisted extraction
PPC2 Investigation of some metals in underground part of the Adenophora stenanthiana
(Ledeb) Kitag)
Zhang ha dan bao li gao1, Д.Энхжаргал2, Д.Даваадагва2,Bu ren ba tu1, Wang xiu lan1,
He chen lin1
1China Inner Mongolian University for Nationalities; 2School of Pharmacy, Mongolian
National University of Medical Science
Correspondence: Д.Энхжаргал (enkhjargal.d@mnums.edu.mn)
Background
Adenophora stenanthiana (Ledeb) Kitag, family of Campanulaceae, is widely grown in
China. It is documented in the Chinese Medical Encyclopedia to be beneficial for gout,
rheumatism, leprosy, some bacterial infections and cancer. The part grown under ground
contained glycosides, terpenes, and small amount of alkaloids. To determine the safety
of the raw material of Adenophora stenanthiana (Ledeb) Kitag, the content of some
heavy metals were determined by atomic absorption spectrometer.
Methods
Eight samples of Adenophora stenanthiana were collected from different geographical
regions of China, according to the Chinese pharmacopoeia. Heavy metals such as lead,
cadmium and copper were measured in the samples with standard atomic absorption spectrometric
method (CP- A/59).
Results
The heavy metal content of the 8 samples were determined. According to the Medicinal
Plasma Standard (GAPS) the permissible content were as follow: (Cu ≤ 20.0 μg /g, Pb
≤ 5.0 μg/g, Cd ≤ 0.3 μg /g). Sample 6 and 8 were relatively high in lead with 18.85
μg/g and 41.92 μg/g, respectively, However, both samples did not exceed the acceptable
concentration for cadmium and copper.
Conclusions
Adenophora stenanthiana grown in different geographical regions presented with different
concentrations of heavy metals.
Keywords
Adenophora stenanthiana, copper, cadmium, lead, atomic absorption spectrometer
PPC5 Analysis of methanolic extract of Aloe vera by reverse phase high performance
liquid chromatography (RP-HPLC)
Razuan Hilmi Md Sulji, Kathleen J. Jalani, Hannis Fadzillah Mohsin, Ibtisam Abdul
Wahab
Department of Pharmacology & Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA (UiTM), 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Ibtisam Abdul Wahab (ibtisam@uitm.edu.my)
Background
Aloe vera is also known as Aloe barbadensis Miller, a plant that has been used for
the purpose of medication and cure for health conditions.The Aloe vera extract was
studied by using reversed phase high performance liquid chromatographic (RP-HPLC)
method.
Methods
The RP-HPLC system included a Model 1100 pump supplied with a multi solvent delivery
system, an Agilent C18 (5 μm, 4.6 x 250 mm) column and a photodiode array detector.The
solvent consisted of acetonitrile (CH3CN) and water (0.01% formic acid). It was set
up to run in a gradient elution as follows: 0 min, 10:90; 3 min, 10:90; 30 min, 90:10;
35 min, 90:10; 36 min, 10:90; and 45 min, 10:90. The flow rate was set as 1 mL/min
(temperature of the column = 25oC) and the UV absorbances were measured at λ = 210,
254 and 280 nm. The peaks in the chromatograms were recorded and reviewed. A triplicate
trial was performed for each sample volume = 10 μL, per injection.
Results
The compounds with the highest absorbance values were eluted within nine minutes,
whereby the solvent ratio was 30:70 (CH3CN:H2O). It is suggested that aloe emodin
was separated much earlier, at retention time, RT = 1.676 minutes. Later, the anthrone
C-glycosides [aloin A (barbaloin) and aloin B (isobarbaloin) could be eluted, respectively
at RT = 8.171 and 8.721 minutes.
Conclusions
The Aloe compounds could be identified by comparing their retention times with the
monograph. Some unresolved, minor peaks, that were not well isolated (RT = 2.2 and
8.3 minutes) could be attributed to the less polar metabolites of aloins, for example,
the aloe emodin anthraquinone and rhein. The RP-HPLC technique appears to be adequate
for routine analysis of the Aloe extract.
Keywords:
Aloe, chromatography, extraction, separation
PPC7 Phytochemical investigation of Combretum indicum leaves extracts
Sabarina Binti Azzizi, Humera Naz
Department of Pharmacology and Chemistry, Faculty of Pharmacy, Universiti Teknologi
MARA (UiTM), Puncak Alam, Selangor, Malaysia
Correspondence: Humera Naz (humera@uitm.edu.my)
Background
Combretum indicum is also known as Akar Dani or Rangoon Creeper and can be found throughout
Asia and tropical Africa. C. indicum is a plant species belonging to the Combretum
genus and the family of Combretaceae. Numerous studies proved the therapeutic effects
of this plant including anti-obesity, anti-inflammatory, antioxidant, insecticidal,
antimicrobial, cytotoxic and immunomodulatory properties. The previous phytochemical
studies of Combretum indicum has revealed the presence of tetracyclic triterpenes,
trigonelline (alkaloid), rutin (flavonoid), tannins, L-proline (α-amino acid), L-asparagine
(α-amino acid) and quisqualic acid. In addition, isoenzyme A and isoenzyme B (Enzyme),
the two forms of the cysteine synthase are also present in C. indicum.
Methods
The chemical constituents of leaves of C. indicum were extracted using organic solvents.
The TLC profile of chloroform extract of C. indicum was established and chemical constituents
were purified by PTLC.
Results
Two long chain fatty acids derivatives were successfully isolated from the crude chloroform
extract and the structures were confirmed by using NMR analysis.
Conclusions
The phytochemical study on Malaysian C. indicum confirmed the presence of terpenes
in chloroform extract.
Keywords:
Combretum indicum, Combretaceae, Phytochemical study
PPC8 Analysis of saponins in Vietnamese ginseng cultivated in Lam Dong Province, Vietnam
by HPLC-PDA/CAD
Huy Truong Nguyen1, Quoc Dung Tran Huynh2, Hong Van Le Thi3, Jeong Hill Park4, Minh
Duc Nguyen1
1Faculty of Pharmacy, Ton Duc Thang University, Ho Chi Minh City, Vietnam; 2Department
of Pharmacy, Traditional Medicine Institute, 179 Nam Ky Khoi Nghia Street, Ho Chi
Minh city, Vietnam; 3Department of Pharmacognosy, University of Medicine and Pharmacy
Ho Chi Minh City, 41 Dinh Tien Hoang street, dist. 1, Ho Chi Minh city, Vietnam; 4College
of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University,
Seoul 08826, Korea
Correspondence: Minh Duc Nguyen (nguyenminhduc@tdtu.edu.vn), Jeong Hill Park (hillpark@snu.ac.kr)
Background
Panax vietnamens is, namely Vietnamese ginseng (VG), was discovered under the canopy
of Ngoc Linh mountain in Kon Tum and Quang Nam provinces in 1973. Since then, VG had
been believed to be an herbaceous perennial plant native to this area only until recently
it was acclimatized to Lam Dong province and cultivated successfully. In this comparative
study, we analyzed the saponin composition in both VG cultivated in Lam Dong (VG-LD)
and VG cultivated in Ngoc Linh area (VG-NL).
Methods
Saponins in the underground part of VG-LD from 2-4 years old were analyzed in comparison
with with those of VG-NL. Separation, qualitative and quantitative analysis of twelve
main VG saponins including N-R1, M-R1, G-Rg1, G-Re, M-R2, P-RT4, V-R11, V-R2, G-Rh1,
G-Rb1, G-Rc, and G-Rd were obtained by HPLC coupled with diode array (PDA) and charge
aerosol (CAD) detectors.
Results
VG-LD not only yielded the same chemical composition but also exhibited the considerably
higher total saponin content than that of VG-NL at all ages. For instance, total saponin
contents of 2-4 years old VG-LD roots, on average, were 9.95%, 11.73%, and 12.84%,
respectively, whereas those of VG-NL, on average, were 2.91%, 4.18%, and 10.31%, respectively.
Similarly, total saponin contents of 2-4 years old VG-LD rhizomes, on average, were
11.39%, 17.21%, and 14.96%, respectively, whereas those of VG-NL were 3.94%, 5.77%,
and 9.59%, respectively.
Conclusions
The result indicates that, regarding the saponin composition, the cultivation of VG
in Lam Dong province is successful and, therefore, deserves the support from both
central and local governments to nurture and develop the achievement. Further comparative
study on the saponin composition of VG-NL and VG-LD at different ages is now in progress
to observe the accumulation of saponins over years.
Keywords: Vietnemese ginseng, Panax vietnamensis, HPLC-PDA/CAD, analysis of saponin
composition
PPC9 Development and validation of a HPLC method for the determination of hippadine
in the bulbs of Crinum latifolium L.
Nguyen Thi Tuyet Nhung1, Nguyen Thi Ngoc Ha1, Vo Thi Bach Hue 2
1Department of Analytical chemistry and Drug quality control, Faculty of Pharmacy,
Lac Hong University, 10 Huynh Van Nghe, Dong Nai, Viet Nam; 2Department of Analytical
chemistry and Drug quality control, Faculty of Pharmacy, University of Medicine and
Pharmacy at Ho Chi Minh city, 41 Dinh Tien Hoang, Ho Chi Minh City, Viet Nam
Correspondence: Nguyen Thi Tuyet Nhung (tuyetnhung@lhu.edu.vn)
Background
Hippadine is a biologically active alkaloid isolated from Crinum latifolium L. It
has been shown to decrease the heart rate and blood pressure due to α1 and β1 adrenoceptor
inhibition.
Methods
An isocratic HPLC method was developed to determine hippadine in the bulbs of Crinum
latifolium L. The chromatographic separation was achieved using a mobile phase consisted
of acetonitrile – phosphoric acid pH 3 (46:54 v/v) on a C18 column (100 x 4.6 mm,
3.5 μm) and detection was carried out at 299 nm. The injection volume was 10 μL, the
flow rate was 1 mL/min and column temperature was set at 30 °C. The method was validated
with respect to system suitability, specificity, linearity, accuracy and precision.
Results
The content of hippadine in the bulbs of Crinum latifolium L. collected from Binh
Dinh province (Viet Nam) was found as 315.8 mcg/g (0.0316%). The method was precised
with an intra-day RSD = 0.6% and inter-day RSD = 1.16%. The detector’s response was
linear (R2> 0.999) and reliable for hippadine quantitation from 1 up to 20 ppm. Through
recovery studies, accuracy of the method was averagely estimated to be 98.06 – 99.65%.
Conclusions
The HPLC method was proved to determine hippadine in the bulbs of Crinum latifolium
L. with sufficient accuracy and precision.
Keywords: HPLC, hippadine, Crinum latifolium L.
PPC10 Synthesis and antibacterial activity of some new chlorobenzothiazole derivatives
Phung Thi Thu Thuy1, Nguyen Thi Ngoc Ha2, Truong Phuong3
1Department of Pharmaceutical chemistry, Faculty of Pharmacy, Lac Hong University,
10 Huynh Van Nghe, Dong Nai, Viet Nam; 2Department of Analytical chemistry and Drug
quality control, Faculty of Pharmacy, Lac Hong University, 10 Huynh Van Nghe, Dong
Nai, Viet Nam; 3Department of Pharmaceutical chemistry, Faculty of Pharmacy, University
of Medicine and Pharmacy at Ho Chi Minh city, 41 Dinh Tien Hoang, Ho Chi Minh city,
Viet Nam
Correspondence: Phung Thi Thu Thuy (thuyphungds@lhu.edu.vn)
Background
Benzothiazole derivatives are well known as antibacterial agents. In the present study,
a series of novel amides containing chlorobenzothiazole were synthesized, characterized
and evaluated for their antibacterial properties.
Methods
In this research, we synthesized some new 2-acetamido-chlorobenzothiazole derivatives
from 2-chloroanilin and 2,4,5-trichloroanilin through four reactions. The evaluation
of the synthesized compounds for antibacterial activities were carried out by using
agar diffusion method.
Results
Seven 2-acetamido-chlorobenzothiazole derivatives were obtained. All of the newly
synthesized compounds were characterized by melting point, thin layer chromatography,
structural elucidation by UV, IR, 1H-NMR, 13C-NMR and MS. This research also presents
the result of the investigation antibacterial activities of the 2-acetamido-clorobenzothiazole
derivatives on the Escherichia coli ATCC 25922, Staphylococcus aureus (MRSA) ATCC
43300, Pseudomonas aeruginosa ATCC 27853; Streptococcus faecalis ATCC 29212. Tests
on biological activity showed that 5 of the synthesized derivatives (3b, 3c, 4g, 4h,
4r) were effective against two referenced strains of bacteria. 4g and 4r showed higher
antibacterial effect against the MRSA (MIC4g = MIC4r = 16 mg/ml).
Conclusions
We have discovered some new chlorobenzothiazole derivatives and bioassay results showed
that some of these synthesized derivatives displayed medium antibacterial activities
against various bacterial species. These results are the basis for synthesis of new
antimicrobial drugs which can be suitable for this current.
Keywords: Benzothiazole, 2-chloroanilin, 2,4,5-trichloroanilin, Antibacterial activity.
PPC11 Study and establish of process of synthesis some 2-hydrazinylthiazolopyridine
derivatives
Van-Thong Huynh1, Thu-Thuy Thi Phung1, Phuong Truong2
1 Faculty of Pharmacy, Lac Hong University, Bien Hoa City, Viet Nam; 2Faculty of Pharmacy,
University of Medicine and Pharmacy, Ho Chi Minh City, Viet Nam
Correspondence: Van-Thong Huynh (thonghuynhvan63@gmail.com)
Background
The derivatives contain thiazolopyridine ring show that many potential biological
activities have been reported in literature as antitumoral activity, anticonvulsant,
cytotoxicity, antibacterial activity and antifungal.Therefore, the aim of this study
was to establish an effective process for synthesis some thiazolopyridine derivatives.
Methods
Similar benzothiazole ring, thiazolopyridine heterocycle can be synthesized with various
methods such as Hugerchoff’s cyclization reaction with bromine agent or Jacobsen reaction
with K3[Fe(CN)6] agent. In this research, we synthesized 2-hydrazinylthiazolopyridine
derivatives by thiazolopyridine cyclization reaction in dimethyl sufoxide with sodium
methoxide agent.
Results
The derivatives containing thiazolopyridine ring are synthesized through 5 stages.
A compound N-(pyridylcarbamothioyl)benzamide was obtained from the reaction between
4-methyl-2-chloro-3-aminopyridine and benzoyl isothiocyanate. N-(pyridylcarbamothioyl)
benzamide was cyclized by CH3ONa agent in DMSO to form the structure of thiazolopyridine.
Hydrolyzing benzamide in sulfuric acid 70% agent lead to formation of 2-aminothiazolopyridine.
Then condensate the obtained derivative with hydrazine sulfate to obtain 2-hydrazinylthiazolopyridine.
Finally reacted with different aldehydes and obtained 6 new derivatives. All of the
synthesized compounds were characterized by melting point, thin layer chromatography,
structural elucidation by UV, IR, 1H-NMR, 13C-NMR and MS.
Conclusions
This study have established procedure to synthesize 2-hydrazinylthiazolopyridine derivatives
from the initial material 4-methyl-2-chloro-3-aminopyridine with good performance.
The intermediate and final derivatives are precisely defined chemical structures with
the expected formula. Therefore, we propose to synthesize thiazolopyridine derivatives
according to the process that has been investigated and tested for biological activity
to receive compounds with good biological activity.
Keywords: Thiazolopyridine, 2-hydrazinylthiazolopyridine, thiazole
PPC12 Determination of amygdalin in “Xuefu Zhuyu” capsules by HPLC - PDA method for
use in the drug quality control
Tran Khanh Duy1, Vo Thi Bach Hue2
1Department of Analytical Chemistry and Drug Quality Control, Faculty of Pharmacy,
Lac Hong University, 10 Huynh Van Nghe, 76100 Bien Hoa, Dong Nai, Viet Nam; 2Department
of Analytical Chemistry and Drug Quality Control, Faculty of Pharmacy, University
of Medicine and Pharmacy at Ho Chi Minh City, 41 Dinh Tien Hoang, 71000 District 1,
Ho Chi Minh city, Viet Nam
Correspondence: Tran Khanh Duy (duytk018@gmail.com)
Background
Xuefu Zhuyu is a famous traditional Chinese medicine widely used in the treatment
of cardiovascular diseases such as thrombosis, angina pectoris, heart attack, strokes.
Xuefu Zhuyu comprises of 11 herbs: Semen Persicae, Flos Carthami tinctorii, Radix
Angelicae sinensis, Rhizoma Ligustici wallichii, Radix Paeoniae, Radix Bupleuri, Radix
Rehmanniae glutinosae, Fructus Aurantii, Radix Platycodi grandiflori, Radix Achyranthis
bidentatae, Radix Glycyrrhizae. The determination of amygdalin, a bioactive component
in Xuefu Zhuyu capsules was developed by using liquid chromatography with photo diode
array detector (HPLC - PDA). This HPLC method was validated and applied to the quality
assessment of Xuefu Zhuyu capsules.
Methods
The sample preparation method and the chromatographic conditions were optimized to
quantify amygdalin in the Xuefu Zhuyu capsules by HPLC. The optimization was obtained
when the peak area of amygdalin in the chromatogram of sample solution was maximum
and chromatographic parameters met requirements such as theoretical plate number (N
> 5000), resolution (Rs > 1.5), asymmetry (0.8 - 1.5) and peak purity (purity factor
> 999.000). This method was subsequently validated according to the ICH guideline
Q2 (R1) (ICH 2005) with respect to system suitability, specificity, linearity, repeatability,
intermediate precision, accuracy and range of analytical procedures.
Results
The optimal sample preparation method was found. The powder of Xuefu Zhuyu was extracted
with methanol in ultrasonic bath for 15 min. The chromatographic conditions were as
follows: Mobile phase methanol - water (21.5 : 78.5), column Phenomenex Gemini C18
(250 × 4.6 mm; 5 μm), column temperature 25 oC, photo diode array detector set at
210 nm, flow rate 1.0 mL/min, injective volume 20 μL. The developed method showed
system suitability, specificity, linearity within 2.4 - 48.0 μg/mL (
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= 18.104x, R2 = 1), repeatability (RSD = 0.3%), intermediate precision (RSD = 0.6%),
accuracy with recovery rate 98.1 - 101.1% and the range 9.6 - 38.4 μg/mL.
Conclusions
In the present study, a simple, accurate and reliable analytical method for determination
of amygdalin in Xuefu Zhuyu capsules was developed by using HPLC - PDA. The result
of this study would be helpful to build the quality control standard of Xuefu Zhuyu
capsules.
Keywords: Amygdalin, Xuefu Zhuyu, determination, traditional Chinese medicine, HPLC.
PPR1 Perception of problem-based learning among academic staff of Faculty of Pharmacy,
UiTM
Nurafifah Shazreen Kamarul Mohd Sham, SIti Aisyah Zulkifli, Aida Azlina Ali, Nur Suraya
Adina Suratman
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM) Cawangan Selangor Puncak Alam
Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Nur Suraya Adina Suratman (suereya@uitm.edu.my)
Background
Problem-based learning is an approach that is focused on self-directed learning and
small group discussion whereupon students work through a given case to acquire knowledge.
It is a learning strategy that is commonly adopted in higher education institutions,
including pharmacy schools throughout the world. Perception, whether good or bad,
can have an impact on the effectiveness of PBL implementation. This study aimed to
determine the perception of PBL among academic staff at the Faculty of Pharmacy, UiTM
Puncak Alam Campus.
Methods
Cross sectional study was conducted from March to May 2018. Data was collected through
a 27 item, self-administered questionnaire. Descriptive analyses were performed using
frequency counts, percentages, means and standard deviations.
Results
A total of 74 questionnaires were distributed to academic staff involved in the Bachelor
of Pharmacy (B. Pharm) curriculum, with a 56.94% response rate. The majority of respondents
agree that PBL is an effective learning strategy, with several advantages, among others,
a more thorough knowledge gain and enhancement of public speaking skills.
Conclusions
PBL is viewed by the academic staff as an effective teaching and learning approach.
Nonetheless, it is important to ensure careful planning of PBL and adequate training
of faculty members to ensure its successful implementation in the UiTM B.Pharm programme.
Keywords: Perception, Problem-based learning, Teaching-learning, Pharmacy
PPR2 Preliminary study on medicinal plants used in the treatment of arthritis among
medicinal plant practitioners in Kampot Province, Cambodia
Cheng Monineath, Koem Dany, Mam Phuongdanin
Faculty of Pharmacy, University of Health Sciences, 12201 Daun Penh, Phnom Penh, Cambodia
Correspondence: Cheng Monineath (chengmonineath@gmail.com)
Background
This research is based on an ethnobotanical investigation which focused on medicinal
plants used to treat arthritis by traditional healers as well as local people in Kampot
province. According to the WHO, about 80% of the world population including Cambodia
uses medicinal plants for treatment since the ancient time. This survey was conducted
on the uses of medicinal plants for arthritic treatment. Tis study was aimed to document
all of this indigenous knowledge to for sustainability and improvement of usage as
arthritis was seen commonly occurring in the society of Cambodia.
Methods
The data collection was conducted in Kampot province among traditional healers and
local people. Five traditional healers and 45 local people who are also medicinal
plant practitioners responded to the following the semi-structured interviews.
Results
Twenty eight medicinal plants were listed with information on local, scientific and
family name, plant parts used, mode of preparation and administration. Leea rubra
Blume., Achyranthes aspera Linn., Morus alba Linn., and Zingiber officinale Rose.
were the most identified and mentioned by various sources (book, international papers,
survey). Leaves were the most common to use for the treatment of arthritis, which
represents 20% among the other plant parts. The frequent preparation method and administration
was drying and decoction, taken orally which represented 64% of all methods used.
Conclusions
Throughout this research, it illustrates the diversity of plants which have been used
among traditional healers and local people who were mentioned differently in therapeutic
practices. Interestingly, 5 medicinal plants have been identified and Leea rubra Blume.
was considered as one of the most potential plants which should be focused for further
investigation.
Keywords: Ethnobotanical investigation, traditional healers, indigenous knowledge
PPR3 Exploration of pharmacology facilitators’ satisfaction level in problem-based
learning at Pharmacy School
Nurul Hasanah Zainul Ariffin, Muhammad Amzar Safiy Raduan, Nur Suraya Adina Suratman,
Mohd Shahezwan Abd Wahab, Aida Azlina Ali
Faculty of Pharmacy, Universiti Teknologi MARA (UiTM) Cawangan Selangor Puncak Alam
Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia
Correspondence: Aida Azlina Ali (aidaaz2790@uitm.edu.my)
Background
Problem-based learning (PBL) is a constructivist teaching-learning method by which
students are to construct idea based on their existing knowledge. Facilitators on
the other hand plays a less active role by facilitating students learning. Because
of this, the characteristics and skills of effective facilitators have received relatively
more attention. Therefore, this study was conducted to investigate facilitators’ satisfaction
of PBL and to determine correlation between the facilitators’ position and their satisfaction
level on PBL.
Methods
Subjects of this study were lecturers who have been involved in facilitating PBL in
Pharmacology subjects. A total of 14 subjects were asked to assess their satisfaction
on PBL using a self-administered questionnaire. The questionnaire consisted of 21
items group as seven factors related to student’s role, tutor’s role, designated problems,
environment of classroom, allotted time, evaluation process and overall satisfaction.
Results
The result indicate that facilitators were moderately satisfied with the PBL method.
Interestingly, their position i.e. senior lecturer or professor determines their satisfaction
level.
Conclusions
In conclusion, the role of the facilitator is of pivotal importance, providing students
with proper guidance during the PBL process. As such, a PBL training program is desirable
to prepare tutors for facilitation of PBL.
Keywords: satisfaction, problem-based learning, facilitator, Pharmacology, Pharmacy
PPR4 A case study research prevalence of Alcohol Consumption among women in Phnom
Penh Capital City and Kampong Cham Province 2018
Ly Ratanak, Heach Lyheang, Salot Saloem, Chheang Sena
Faculty of Pharmacy, University of Health Sciences, Phnom Penh, Cambodia
Correspondence: Chheang Sena (sena_chheang@uhs.edu.kh)
Background
Alcoholic drinks have been a part of the community life and up until now societies
have always found it difficult to understand or restrain their use. The aim of this
study was to find out the prevalence of alcohol consumption among women in community
of Phnom Penh and Kampong Cham.
Methods
The review was conducted at two sites (Kampong Cham and Phnom Penh). These questionnaires
were pretested and proved to be well understood by responders. Data analyses are achieved
using SPSS version 18. Results was counted in number (n) and percentage (%).
Results
The study reveals that among the 384 respondents, prevalence of consuming alcohol
among women was 65.4%. About 69.3% and 61.5% of women in Phnom Penh and Kampong Cham,
respectively consumed alcohol beverages. The factors that prompted these women to
take alcohol were due to the influence of society and family members, self-medication,
and during postpartum.
Conclusion
In conclusion, there are more women in Phnom Penh that consumed alcohol than women
who lives in Kampong Cham.
Keyword: Alcohol, Prevalence, Women, Cambodia
PPR5 Pain Control and Analgesic Dosing Deviation in Patients with Chronic, Non-Cancer
Pain
Harun Mohammad Akmal, Ahmad Nurul Fateehah, Cheah Huey Miin
Department of Pharmacy, Kuala Lipis Hospital, Kuala Lipis, 27200 Pahang, Malaysia
Correspondence: Cheah Huey Miin (hueymiin@moh.gov.my)
Background
Chronic pain places a tremendous burden on the sufferers’ quality of life. Several
studies have reported treatment inadequacy involving patients with chronic pain. The
objective of the study is to investigate the prevalence of discrepancy between prescribed
dose and the actual dose taken in analgesic use, as well as its relationship with
pain control in chronic, non-cancer pain.
Methods
This was a cross-sectional study. Subjects were recruited into the study through convenience
sampling. Data was collected using Brief Pain Inventory (BPI) form. Pearson chi-square
test was used to study the relationship between dosing deviation of analgesic regimen
and pain control (pain management index, PMI). Statistical significance was defined
as p<0.05.
Results
A total of 127 patients were recruited. The median value for the worst pain score
was 8 while the least pain score was 1. As much as 70.9% of patients reported inadequate
pain control with current analgesic(s), depicted as negative PMI. There was discrepancy
between prescribed dose and the actual dose taken by patients in analgesic use. 11.8%
and 34.7% patients did not follow prescriber’s instruction for oral and topical analgesic
use respectively. However, no significant result was found between dosing deviation
and pain control (p>0.95). The study also discovered that 98% patients did not know
the maximum dose of analgesic(s) which they were taking.
Conclusions
Although there was dosing deviation in analgesic use between what was prescribed and
what was actually taken by patients, the relationship between the deviation and pain
control was not significant.
Keywords: chronic pain, pain control, pain management index, brief pain inventory,
analgesic
PPR6 A preliminary study on ethnobotanical survey of medicinal plants used by traditional
healers to treat toothaches
Them Seydaduong, Kak Nika, Brang Nita
Faculty of Pharmacy, University of Health Sciences, 12201, Daun Penh, Phnom Penh,
Cambodia
Correspondence: Them Seydaduong (daduongg@yahoo.com)
Background
Medicinal plants have potential in treating different kinds of diseases since many
centuries. They have been the primary solution to care for people's oral health due
to the inexpensive costs and potentials. The aim of this study was to document the
types of medicinal plants and therapeutic methods used by traditional healers to relieve
toothaches and also the use of these plants to produce an effective modern medicine.
Methods
The study was conducted from 25th September to 30th October in 2017 using questionnaires,
following the WHO guideline. The information was collected from three key traditional
healers, who are from National Center of Traditional Medicine and Faculty of Pharmacy,
University of Health Sciences, due to their vast knowledge on medicinal plants.
Results
A total 37 medicinal plants were identified for the use in treating toothaches, which
were collected from three references. Among these plants, 3 medicinal plants (Spilanthes
acmella, Syzygium aromaticum and Piper lolot) were commonly used for the toothache
treatment. This study shows that leaves and barks were the most frequently used parts
of the plants, followed by resin, flower, root and stem. These plants were applied
directly to the infected area of the tooth in different ways such as decoction, maceration,
pounding or chewing.
Conclusions
This study shows that the diversity of each plants has different effect as remedies
to treat toothaches. Three medicinal plants have been recognised as potential cure.
Moreover, leaves were the most common plants part used which were generally prepared
through decoction.
Keywords: Toothache, Medicinal plant, Traditional healer, Ethnobotany
PPR7 A case study research of self-medication as a daily living behavior of people
in community of Kampong Cham province and Phnom Penh capital
Sreypich Prak, Vouchmeng Hun, Chhumsophearath Loeung, Sena Chheang
Faculty of Pharmacy, University of Health Sciences, 12201 Daun Penh, Phnom Penh, Cambodia
Correspondence: Sreypich Prak (sena_chheang@uhs.edu.kh)
Background
According to WHO (2000), self-medication is the use of medicinal products to treat
self-recognized disorder or symptoms. There are several circumstances arising from
self-medication, including irrational use of drug, mistreatment and risk of drug abuse.
However, no research has addressed the extent of self-medication practice in local
community of Cambodia.
Methods
A quantitative cross-sectional study was conducted with a total of 312 samples, 156
samples in Phnom Penh and 156 in Kampong Cham, were selected randomly among patients
who purchased medicines from pharmacies. The study used questionnaires as the study
tool for face-to-face semi-direct interview. Data analysis is achieved through using
SPSS version 18. Results were presented as count (n) and percentage (%).
Results
In Phnom Penh, 91% of 156 respondents, self-medicate, where the prevalence rate in
Kampong Cham was 70.2% of 156 respondents. Cost efficiency was the main reason of
self-medication in both areas. The most common illness was flu (15.3% of all reported
cases) and the most prescribed medicine was analgesics (24.9%). Respondents from both
areas prefer pharmacy as the first choice for healthcare service. Practice of patient
counselling was very low in Phnom Penh (1.3%) compared to Kampong Cham (79.5%).
Conclusions
Prevalence rate of self-medication was higher in Phnom Penh compared to Kampong Cham
(22.52% difference). Although pharmacy is the first choice of healthcare service,
awareness should be raised as serious illnesses require proper diagnosis and treatment.
Dependency may develop due to the misuse of analgesics. Good pharmacy practice should
be applied to ensure safety, efficacy and efficiency use of medication.
Keywords: Self-medication; Pharmacy practice; Dependency
PPR8 Cross-sectional study of fever management of Influenza among undergraduate student
in Phnom Penh, Cambodia: Preliminary result in 2018
Chhay Chhingsrean, Chhorn Hangthida, Chea Sreytouch
Faculty of Pharmacy, University of Health Sciences, 12201 Daun Penh, Phnom Penh, Cambodia
Correspondence: Chhay Chhingsrean (chhingsrean.chhay@gmail.com )
Background
In low income country, fever is common among adolescents and adults seeking for healthcare.
Fever is one of the symptoms of influenza (flu) which happened every year in Cambodia.
This research aims to expose the experiences and attitudes of undergraduate students
from different universities on fever and flu medication and care.
Methods
A cross-sectional survey of 453 undergraduate students was conducted in Phnom Penh
using semi-structured questionnaire which was prepared and validated. Epidata was
used to insert data before analyzed by STATA version 12.
Results
A total number of 453 undergraduate students from 30 universities in Phnom Penh successfully
consented and completed the questionnaire. Alternative methods were mostly used to
confirm the body temperature; however, 61.22% used thermometer. 58.72% of participants
relied on both medication and selfcare while flu medicines (55.06%) was commonly used
following by unknown medication, antipyretic and antibiotic that were used for less
than 3 days (45.19%). Besides, resting (68.56%), hot bath, wiping, home remedies,
coining and exercise were preferable practices for selfcare. Although the respondents
preferred both methods, they felt more confident to use medication than self-care.
Conclusions
Medication and self-care are widely practiced among undergraduate students to manage
fever and flu. Education about fever management relying on medication and self-care
should be promoted in Cambodia.
Keywords: Cross-sectional study, Fever management, Undergraduate students