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Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes
Li, W.1,5; Liu, Y.1; He, Y. -Q.2; Zhang, J. -W.1; Gao, Y.3; Ge, G. -B.1,5; Liu, H. -X.1,5; Huo, H.1; Liu, H. -T.1,5; Wang, L. -M.3; Sun, J.3; Wang, Q.4; Yang, L.1; Yang L(杨凌); Yang L(杨凌)
关键词Triptolide Cytochrome P450 Mono-hydroxylated Metabolite
刊名XENOBIOTICA
2008
DOI10.1080/00498250802503359
38期:12页:1551-1565
收录类别SCI
文章类型Article
部门归属18
项目归属1806
产权排名1;1
WOS标题词Science & Technology ; Life Sciences & Biomedicine
类目[WOS]Pharmacology & Pharmacy ; Toxicology
研究领域[WOS]Pharmacology & Pharmacy ; Toxicology
关键词[WOS]WILFORDII HOOK-F ; TRIPTERYGIUM-WILFORDII ; DRUG-METABOLISM ; ENZYMES ; TRIPDIOLIDE ; CLEARANCE ; TUMORS
英文摘要Triptolide, the primary active component of a traditional Chinese medicine Tripterygium wilfordii Hook F, has a wide range of pharmacological activities. In the present study, the metabolism of triptolide by cytochrome P450s was investigated in human and rat liver microsomes. Triptolide was converted to four metabolites (M-1, M-2, M-3, and M-4) in rat liver microsomes and three (M-2, M-3, and M-4) in human liver microsomes. All the products were identified as mono-hydroxylated triptolides by liquid chromatography-mass spectrometry (LC-MS). The studies with chemical selective inhibitors, complementary DNA-expressed human cytochrome P450s, correlation analysis, and enzyme kinetics were also conducted. The results demonstrate that CYP3A4 and CYP2C19 could be involved in the metabolism of triptolide in human liver, and that CYP3A4 was the primary isoform responsible for its hydroxylation.
语种英语
原文出处查看原文
WOS记录号WOS:000261174400008
引用统计
被引频次:47[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/100901
专题中国科学院大连化学物理研究所
通讯作者Yang L(杨凌); Yang L(杨凌)
作者单位1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
2.Shanghai Univ Tradit Chinese Med, Shanghai, Peoples R China
3.Dalian Med Univ, Affiliated Hosp 2, Dalian, Peoples R China
4.Dalian Univ Technol, Dalian, Peoples R China
5.Chinese Acad Sci, Grad Univ, Beijing, Peoples R China
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GB/T 7714
Li, W.,Liu, Y.,He, Y. -Q.,et al. Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes[J]. XENOBIOTICA,2008,38(12):1551-1565.
APA Li, W..,Liu, Y..,He, Y. -Q..,Zhang, J. -W..,Gao, Y..,...&杨凌.(2008).Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes.XENOBIOTICA,38(12),1551-1565.
MLA Li, W.,et al."Characterization of triptolide hydroxylation by cytochrome P450 in human and rat liver microsomes".XENOBIOTICA 38.12(2008):1551-1565.
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