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题名: Identification of CYP isoforms involved in the metabolism of thymol and carvacrol in human liver microsomes (HLMs)
作者: Dong, Rui-Hua1;  Fang, Zhong-Ze2, 3;  Zhu, Liang-Liang2;  Ge, Guang-Bo2;  Cao, Yun-Feng2;  Li, Xiao-Bao4;  Hu, Cui-Min;  Yang, Ling2;  Liu, Ze-Yuan1
刊名: PHARMAZIE
发表日期: 2012-12-01
DOI: 10.1691/ph.2012.2534
卷: 67, 期:12, 页:1002-1006
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine ;  Physical Sciences
类目[WOS]: Chemistry, Medicinal ;  Chemistry, Multidisciplinary ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy ;  Chemistry
英文摘要: Carvacrol and thymol are phenolic compounds with similar structures isolated from many aromatic plants, and have been demonstrated to exert multiple pharmacological effects. The metabolic and pharmacokinetic behaviour of thymol and carvacrol has received much attention. Carvacrol and thymol have been demonstrated to undergo phase I metabolism such as hydroxylation reaction. However, drug-metabolizing enzymes involved in this process remain unclear. Given that cytochrome P450 s (CYPs) are involved in most phase I metabolism, the aim of the present study was to investigate the role of CYPs in the metabolism of thymol and carvacrol. After incubation with human liver microsomes (HLMs) in the presence of NADPH, a new metabolite and two metabolites were detected for thymol and carvacrol, respectively. A combination of chemical inhibition studies and assays with recombinant CYP isoforms demonstrated that CYP2A6 was the predominant drug-metabolizing enzyme involved in the metabolism of thymol and carvacrol. All these results remind the researchers that special attention should be paid on pharmacokinetic and clinical outcomes when thymol or carvacrol was co-administrated with other compounds mainly undergoing CYP2A6-mediated metabolism.
关键词[WOS]: CYTOCHROME-P450 ENZYMES ;  DRUG INTERACTIONS ;  INHIBITION ;  EXPRESSION ;  POPULATION ;  MODEL
语种: 英语
WOS记录号: WOS:000311883800008
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/143107
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.Acad Mil Med Sci, Affiliated Hosp, Dept Clin Pharmacol, Beijing 100071, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian, Peoples R China
3.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA
4.Acad Mil Med Sci, Affiliated Hosp, Dept Breathing Gastroenterol, Beijing 100071, Peoples R China

Recommended Citation:
Dong, Rui-Hua,Fang, Zhong-Ze,Zhu, Liang-Liang,et al. Identification of CYP isoforms involved in the metabolism of thymol and carvacrol in human liver microsomes (HLMs)[J]. PHARMAZIE,2012,67(12):1002-1006.
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