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学科主题: 物理化学
题名: Metabolism of evodiamine by human cytochrome P450 enzymes
作者: Fang ZZ(房中则) ;  Yang L(杨凌)
会议名称: 3rd Asian Pacific Regional Meeting of the International-Society-for-the-Study-of-Xenobiotics
会议日期: 2009-5-10
出版日期: 2009-05-10
会议地点: 泰国
其他题名: 人细胞色素P450酶对吴茱萸碱的代谢
通讯作者: Ling Yang
ISSN: 0360-2532
部门归属: 十八室
摘要: Abstract: Evodiamine is the main active alkaloid of Evodia rutaecarpa and has been demonstrated to have many pharmacological activities. In the present study, the phase I metabolites of evodiamine and the cytochrome P450 isoforms involved were profiled. Human 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). Three major metabolites (M-1, M-3, and M-5) were identified to be monohydroxylated evodiamine and one metabolite (M-4) was identified to be N-demethylated evodiamine by liquid chromatography /mass spectrometry (LC/MS). M-2 was proposed to be 5,6-dehydro evodiamine based on its mass spectrum and retention time. CYP3A4 and CYP1A2 were identified to be the isoform primarily involved in the formation of M-1, M-3, M-4, M-5 in studies with specific P450 inhibitors, recombinant P450s, and correlation analysis. In human liver microsomes, the Km values ranged from 4.7 to 18.4 μM, and the Vm values ranged from 86.3 to 447.5 pmol/min/mg for M-1, M-3, M-4 and M-5. Clarification of the metabolite profile and kinetic properties of evodiamine by human P450s provide important information relevant to the pharmacology and toxicology of evodiamine and E.rutaecarpa.
语种: 中文
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内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/113560
Appears in Collections:中国科学院大连化学物理研究所_会议论文

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Recommended Citation:
Fang ZZ,Yang L. Metabolism of evodiamine by human cytochrome P450 enzymes[C]. 见:3rd Asian Pacific Regional Meeting of the International-Society-for-the-Study-of-Xenobiotics. 泰国. 2009-5-10.
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