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学科主题物理化学
Toxicity of triptolide not due to inhibition of CYPs
Li W(李巍); Liu Y(刘勇); Zhang JW(张江伟); Yang L(杨凌)
会议名称第三届中日双边药理学和临床药理学会议
会议日期2007-8-23
2007-08-23
会议地点中国
页码327/1
部门归属十八室
主办者中国药理学会
英文摘要Triptolide, a purified component of a traditional Chinese Medicine, has been shown to have anti-inflammatory, antifertility, antineoplastic, and immunosuppressive activity, however, its clinical usage is limited to some extent due to its toxicity. The aim is to discover the correlation of triptolide toxicity with cytochrome P450 (CYPs). METHODE The metabolism properties and the inhibitory effects against cytochrome P450 (CYPs) of triptolide were studied in vitro. Triptolide was incubated with human liver microsome in the presence of NADPH-generating system. The inhibitory effects of triptolide (5μM, 50μM) against the activities of seven CYP isoforms including CYP1A2, CYP2A6, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 were examined in human liver microsomes (HLM). To identify time-dependent inhibition, triptolide (50μM, 500μM) was preincubated with microsomes and NADPH-generating system for 0-60 min, and then the extent of inhibition towards seven CYP isoforms were examined. RESULTS Triptolide was slightly NADPH-dependently metabolized in HLM, and four possible products were detected by HPLC. There were no inhibitory effects against tested CYPs activities or time- and NADPH- dependent inhibition against tested CYPs found. CONCLUSION Triptolide was slightly NADPH-dependently metabolized in HLM. And the toxicity of triptolide has no relevance with CYPs inhibition or CYPs-mediated bioactivation. Key words: triptolide; cytochrome P450; metabolism; inhibition.
语种中文
文献类型会议论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/112716
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌)
推荐引用方式
GB/T 7714
Li W,Liu Y,Zhang JW,et al. Toxicity of triptolide not due to inhibition of CYPs[C],2007:327/1.
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