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题名: Inhibitory Effects of Curcumenol on Human Liver Cytochrome P450 Enzymes
作者: Sun, Dong-Xue1;  Fang, Zhong-Ze2, 3;  Zhang, Yan-Yan2, 3;  Cao, Yun-Feng1;  Yang, Ling2;  Yin, Jun1
通讯作者: 殷军
关键词: cytochrome P450 (CYP) ;  curcumenol ;  drug-drug interaction ;  human liver microsomes ;  inhibition ;  enzyme kinetics
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2010-08-01
DOI: 10.1002/ptr.3102
卷: 24, 期:8, 页:1213-1216
收录类别: SCI
文章类型: Article
部门归属: 18
项目归属: 1806
产权排名: 2;2
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Curcumenol, one of the major components of Zedoary turmeric oil, has been widely used to treat cancer and inflammation. As an antibiotic or anticancer drug, curcumenol is highly likely to be used in combination with various synthetic drugs in most cases, thus it is necessary to evaluate potential pharmacokinetic drug-drug interactions induced by curcumenol. In this study, the inhibitory effects of curcumenol on seven CYP isoforms were investigated, and the results demonstrated that only CYP3A4 was strongly inhibited (IC(50) = 12.6 +/- 1.3 mu M). Kinetic analysis showed the inhibition type was competitive with K, value of 10.8 mu M. Time- and NADPH-dependent inhibitions were also investigated to show curcumenol is not a mechanism-based inhibitor. Employing these in vitro data and maximum plasma concentration of curcumenol in human predicted from beagle dog's in vivo pharmacokinetic data, the change in AUC of victim drugs was predicted to be 0.4%, which suggested that curcumenol may be safely used without inducing metabolic drug-drug interaction through P450 inhibition. Nevertheless, due to the limited pharmacokinetic data available for curcumenol in humans, it is still not possible to evaluate its potential clinical effects on human patients from in vitro data. Thus, the magnitude of drug-drug interaction (DDI) induced by curcumenol warrants further investigation. Copyright (C) 2010 John Wiley & Sons, Ltd.
关键词[WOS]: DRUG-DRUG INTERACTIONS ;  METABOLITES ;  PREDICTION ;  EXTRACT
语种: 英语
原文出处: 查看原文
WOS记录号: WOS:000281006500017
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/103165
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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作者单位: 1.Shenyang Pharmaceut Univ, Sch Tradit Chinese Med, Shenyang 110016, Peoples R China
2.Chinese Acad Sci, Lab Pharmaceut Resource Discovery, Dalian Inst Chem Phys, Dalian 116023, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China

Recommended Citation:
Sun, Dong-Xue,Fang, Zhong-Ze,Zhang, Yan-Yan,et al. Inhibitory Effects of Curcumenol on Human Liver Cytochrome P450 Enzymes[J]. PHYTOTHERAPY RESEARCH,2010,24(8):1213-1216.
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