Evaluation of the anti-inflammatory and cytotoxic effects of anthraquinones and anthracenes derivatives in human leucocytes

Rong Fu Chen, Yuh Chiang Shen, Hsu Shan Huang, Jyh Fei Liao, Li Kang Ho, Yueh Ching Chou, Wen Yen Wang, Chieh Fu Chen

研究成果: 雜誌貢獻文章同行評審

29 引文 斯高帕斯(Scopus)

摘要

A variety of anthracene- and anthraquinone-related derivatives, modified from three types of lead structures, including 9-acyloxy 1,5-dichloroanthracene (type I), 1,5-bisacyloxy-anthraquinones with O-linked substituents (type II) and 1,5-bisacyloxy-anthraquinones with S-linked substituents (type III), were synthesized and evaluated by an in-vitro bioassay for their anti-inflammatory and cytotoxic effects in human leucocytes. Among these derivatives, type I compounds displayed potent anti-inflammatory activity against phorbol-12-myristate-13-acetate (PMA)-induced superoxide anion production, a bio-marker of inflammatory mediator production by neutrophils, with 50% inhibition (IC50) concentrations (μM) for compounds 1f, 1g, 1h and 1m being 13.8 ± 3.0, 6.3 ± 4.1, 33.2 ± 1.3 and 33.9 ± 5.7, respectively. Type II and type III derivatives (i.e., 1,5-bisacyloxy anthraquinone-related compounds) and the reference compound, emodin, exhibited relatively minor (20-40%) inhibitory effect against superoxide production by neutrophils. Furthermore, none of these compounds showed a significant cytotoxic effect in human neutrophils. In conclusion, these results suggest that compounds modified from 9-acyloxy 1,5-dichloroanthracence (type I) are more powerful than the other two types as anti-inflammatory drugs. This is the first demonstration that derivatives modified from anthracenes or anthraquinones possess anti-inflammatory activity with no significant cytotoxicity in human neutrophils.
原文英語
頁(從 - 到)915-919
頁數5
期刊Journal of Pharmacy and Pharmacology
56
發行號7
DOIs
出版狀態已發佈 - 7月 2004
對外發佈

ASJC Scopus subject areas

  • 藥理
  • 藥學科學

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