Emodin: A Review of its Pharmacology, Toxicity and Pharmacokinetics

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Abstract

Emodin is a natural anthraquinone derivative that occurs in many widely used Chinese medicinal herbs, such as Rheum palmatum, Polygonum cuspidatum and Polygonum multiflorum. Emodin has been used as a traditional Chinese medicine for over 2000 years and is still present in various herbal preparations. Emerging evidence indicates that emodin possesses a wide spectrum of pharmacological properties, including anticancer, hepatoprotective, antiinflammatory, antioxidant and antimicrobial activities. However, emodin could also lead to hepatotoxicity, kidney toxicity and reproductive toxicity, particularly in high doses and with long‐term use. Pharmacokinetic studies have demonstrated that emodin has poor oral bioavailability in rats because of its extensive glucuronidation. This review aims to comprehensively summarize the pharmacology, toxicity and pharmacokinetics of emodin reported to date with an emphasis on its biological properties and mechanisms of action. Copyright © 2016 John Wiley & Sons, Ltd.

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Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 interaction

Tin-Yun Ho, Shih-Lu Wu, Jaw-Chyun Chen … (2006)

Severe acute respiratory syndrome (SARS) is an emerging infectious disease caused by a novel coronavirus (SARS-CoV). SARS-CoV spike (S) protein, a type I membrane-bound protein, is essential for the viral attachment to the host cell receptor angiotensin-converting enzyme 2 (ACE2). By screening 312 controlled Chinese medicinal herbs supervised by Committee on Chinese Medicine and Pharmacy at Taiwan, we identified that three widely used Chinese medicinal herbs of the family Polygonaceae inhibited the interaction of SARS-CoV S protein and ACE2. The IC50 values for Radix et Rhizoma Rhei (the root tubers of Rheum officinale Baill.), Radix Polygoni multiflori (the root tubers of Polygonum multiflorum Thunb.), and Caulis Polygoni multiflori (the vines of P. multiflorum Thunb.) ranged from 1 to 10 μg/ml. Emodin, an anthraquinone compound derived from genus Rheum and Polygonum, significantly blocked the S protein and ACE2 interaction in a dose-dependent manner. It also inhibited the infectivity of S protein-pseudotyped retrovirus to Vero E6 cells. These findings suggested that emodin may be considered as a potential lead therapeutic agent in the treatment of SARS.

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Emodin inhibits current through SARS-associated coronavirus 3a protein

Silvia Schwarz, Kai Wang, Wenjing Yu … (2011)

The open-reading-frame 3a of SARS coronavirus (SARS-CoV) had been demonstrated previously to form a cation-selective channel that may become expressed in the infected cell and is then involved in virus release. Drugs that inhibit the ion channel formed by the 3a protein can be expected to inhibit virus release, and would be a source for the development of novel therapeutic agents. Here we demonstrate that emodin can inhibit the 3a ion channel of coronavirus SARS-CoV and HCoV-OC43 as well as virus release from HCoV-OC43 with a K 1/2 value of about 20 μM. We suggest that viral ion channels, in general, may be a good target for the development of antiviral agents.

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Rhein: A Review of Pharmacological Activities

Yan-Xi Zhou, Wei-Xiong Xia, Wei Yue … (2015)

Rhein (4, 5-dihydroxyanthraquinone-2-carboxylic acid) is a lipophilic anthraquinone extensively found in medicinal herbs, such as Rheum palmatum L., Cassia tora L., Polygonum multiflorum Thunb., and Aloe barbadensis Miller, which have been used medicinally in China for more than 1,000 years. Its biological activities related to human health are being explored actively. Emerging evidence suggests that rhein has many pharmacological effects, including hepatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. The present review provides a comprehensive summary and analysis of the pharmacological properties of rhein, supporting the potential uses of rhein as a medicinal agent.

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Author and article information

Journal

Journal ID (nlm-ta): Phytother Res

Journal ID (iso-abbrev): Phytother Res

Journal ID (doi): 10.1002/(ISSN)1099-1573

Journal ID (publisher-id): PTR

Title: Phytotherapy Research

Publisher: John Wiley and Sons Inc. (Hoboken )

ISSN (Print): 0951-418X

ISSN (Electronic): 1099-1573

Publication date (Electronic): 18 May 2016

Publication date (Print): August 2016

Volume: 30

Issue: 8 ( doiID: 10.1002/ptr.v30.8 )

Pages: 1207-1218

Affiliations

[ ¹ ] School of Chinese Materia Medica Beijing University of Chinese Medicine Beijing 100102 PR China

[ ² ] Affiliated Hospital, Inner Mongolia University for Nationalities Tongliao 028000 PR China

Author notes

[*] [* ] Correspondence to: Jian Ni, School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 100102, PR China.

E‐mail: njtcm@ 123456263.net

[†]

These authors contributed equally to this work.

Article

Publisher ID: PTR5631 Other ID: PTR-16-0009.R2

DOI: 10.1002/ptr.5631

PMC ID: 7168079

PubMed ID: 27188216

SO-VID: 9bb8cbd3-0679-419c-83ba-562a0353e1f3

License:

This article is being made freely available through PubMed Central as part of the COVID-19 public health emergency response. It can be used for unrestricted research re-use and analysis in any form or by any means with acknowledgement of the original source, for the duration of the public health emergency.