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      Toxicity and Antioxidant Activity of Fullerenol C 60,70 with Low Number of Oxygen Substituents

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          Abstract

          Fullerene is a nanosized carbon structure with potential drug delivery applications. We studied the bioeffects of a water-soluble fullerene derivative, fullerenol, with 10-12 oxygen groups (F10-12); its structure was characterized by IR and XPS spectroscopy. A bioluminescent enzyme system was used to study toxic and antioxidant effects of F10-12 at the enzymatic level. Antioxidant characteristics of F10-12 were revealed in model solutions of organic and inorganic oxidizers. Low-concentration activation of bioluminescence was validated statistically in oxidizer solutions. Toxic and antioxidant characteristics of F10-12 were compared to those of homologous fullerenols with a higher number of oxygen groups:F24-28 and F40-42. No simple dependency was found between the toxic/antioxidant characteristics and the number of oxygen groups on the fullerene’s carbon cage. Lower toxicity and higher antioxidant activity of F24-28 were identified and presumptively attributed to its higher solubility. An active role of reactive oxygen species (ROS) in the bioeffects of F10-12 was demonstrated. Correlations between toxic/antioxidant characteristics of F10-12 and ROS content were evaluated. Toxic and antioxidant effects were related to the decrease in ROS content in the enzyme solutions. Our results reveal a complexity of ROS effects in the enzymatic assay system.

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          C60: Buckminsterfullerene

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            Solid C60: a new form of carbon

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              Reactive oxygen species: from health to disease.

              Upon reaction with electrons, oxygen is transformed into reactive oxygen species (ROS). It has long been known that ROS can destroy bacteria and destroy human cells, but research in recent decades has highlighted new roles for ROS in health and disease. Indeed, while prolonged exposure to high ROS concentrations may lead to non-specific damage to proteins, lipids, and nucleic acids, low to intermediate ROS concentrations exert their effects rather through regulation of cell signalling cascades. Biological specificity is achieved through the amount, duration, and localisation of ROS production. ROS have crucial roles in normal physiological processes, such as through redox regulation of protein phosphorylation, ion channels, and transcription factors. ROS are also required for biosynthetic processes, including thyroid hormone production and crosslinking of extracellular matrix. There are multiple sources of ROS, including NADPH oxidase enzymes; similarly, there are a large number of ROS-degrading systems. ROS-related disease can be either due to a lack of ROS (e.g., chronic granulomatous disease, certain autoimmune disorders) or a surplus of ROS (e.g., cardiovascular and neurodegenerative diseases). For diseases caused by a surplus of ROS, antioxidant supplementation has proven largely ineffective in clinical studies, most probably because their action is too late, too little, and too non-specific. Specific inhibition of ROS-producing enzymes is an approach more promising of clinical efficacy.
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                Author and article information

                Contributors
                Role: Academic Editor
                Journal
                Int J Mol Sci
                Int J Mol Sci
                ijms
                International Journal of Molecular Sciences
                MDPI
                1422-0067
                15 June 2021
                June 2021
                : 22
                : 12
                : 6382
                Affiliations
                [1 ]Institute of Biophysics SB RAS, FRC KSC SB RAS, 660036 Krasnoyarsk, Russia; n-qdr@ 123456yandex.ru
                [2 ]Institute of Physics SB RAS, FRC KSC SB RAS, 660036 Krasnoyarsk, Russia; nata_hd@ 123456rambler.ru (N.G.V.); churilov@ 123456iph.krasn.ru (G.N.C.)
                [3 ]FRC KSC SB RAS, 660036 Krasnoyarsk, Russia; khyzylsyg@ 123456mail.ru
                [4 ]Institute of Fundamental Biology and Biotechnology, Siberian Federal University, 660041 Krasnoyarsk, Russia; stepin-kirill@ 123456mail.ru
                Author notes
                [* ]Correspondence: kkovel@ 123456yandex.ru ; Tel.: +7-3912-494-242
                Author information
                https://orcid.org/0000-0002-4524-6413
                https://orcid.org/0000-0003-2889-490X
                https://orcid.org/0000-0001-5315-8002
                Article
                ijms-22-06382
                10.3390/ijms22126382
                8232284
                34203700
                71dc22ba-c383-4c52-bfb3-5df50433cf71
                © 2021 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( https://creativecommons.org/licenses/by/4.0/).

                History
                : 15 May 2021
                : 10 June 2021
                Categories
                Article

                Molecular biology
                fullerenol,toxicity,antioxidant activity,reactive oxygen species,bioluminescent assay,hormesis

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