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题名: Investigation of the in Vitro Metabolism of Evodiamine: Characterization of Metabolites and Involved Cytochrome P450 Isoforms
作者: Sun, Hong-Zhi1, 5, 6;  Fang, Zhong-Ze2, 3, 4, 5, 6;  Cao, Yun-Feng2, 5, 6;  Sun, Xiao-Yu2, 5, 6;  Hong, Mo2, 5, 6
关键词: evodiamine ;  cytochrome P450 (CYP) ;  human liver microsomes (HLMs)
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2013-05-01
DOI: 10.1002/ptr.4766
卷: 27, 期:5, 页:705-712
收录类别: SCI
文章类型: Article
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: Evodiamine is the main active alkaloid of Evodia rutaecarpa (E. rutaecarpa) and has been demonstrated to exhibit many pharmacological activities including vasorelaxation, uterotonic action, anoxia and control of body temperature. The present study focused on the metabolism of evodiamine. Human and phenobarbital-induced rat liver microsomal incubation of evodiamine in the presence of NADPH resulted in the formation of five major metabolites (M-1, M-2, M-3, M-4, M-5). Four metabolites (M-1, M-2, M-3 and M-5) were identified to mono-hydroxylated evodiamine and one metabolite (M-4) was identified to be N-demethylated evodiamine. CYP3A4, CYP2C9 and CYP1A2 were identified to be the main CYP isoforms involved in the metabolism of evodiamine in human liver microsomes. Finding new metabolites can help us decipher novel substance basis of efficiency and toxicity. Elucidation of drug metabolizing enzymes will facilitate explaining the individual difference for response to the same drugs or herbs and the potential drugdrug interaction or herbdrug interaction. Taken together, these results are of significance for better understanding the pharmacokinetic behaviour of evodiamine and helpful for clinical application of evodiamine and E. rutaecarpa. Copyright (c) 2012 John Wiley & Sons, Ltd.
关键词[WOS]: PHARMACOLOGICAL-PROPERTIES ;  GALENICAL PREPARATION ;  LIVER MICROSOMES ;  IDENTIFICATION ;  RUTAECARPINE ;  RATS ;  PHARMACOKINETICS ;  ALKALOIDS ;  APOPTOSIS ;  CELLS
语种: 英语
WOS记录号: WOS:000318031500011
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/137496
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.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
3.Liaoning Med Univ, Jinzhou 121001, Peoples R China
4.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA
5.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian 116023, Peoples R China
6.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China

Recommended Citation:
Sun, Hong-Zhi,Fang, Zhong-Ze,Cao, Yun-Feng,et al. Investigation of the in Vitro Metabolism of Evodiamine: Characterization of Metabolites and Involved Cytochrome P450 Isoforms[J]. PHYTOTHERAPY RESEARCH,2013,27(5):705-712.
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