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学科主题: 物理化学
题名: Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol
作者: Dong, Rui-Hua2;  Fang, Zhong-Ze1, 3;  Zhu, Liang-Liang1, 3;  Liang, Si-Cheng1;  Ge, Guang-Bo1;  Yang, Ling1;  Liu, Ze-Yuan2
通讯作者: 房中则
关键词: UDP-glucuronosyltransferases (UGTs) ;  carvacrol ;  drug-drug interactions (DDIs)
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2012
DOI: 10.1002/ptr.3525
卷: 26, 期:1, 页:86-90
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
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: UDP-glucuronosyltransferases (UGTs), the most important phase II drug metabolizing enzymes (DMEs), could metabolize many drugs and various endogenous substances including bilirubin, steroid hormones, thyroid hormones, bile acids and fat-soluble vitamins. Evaluation of the inhibitory effects of compounds on UGTs is clinically important because inhibition of UGT isoforms could not only result in serious drug-drug interactions (DDIs), but also induce metabolic disorders of endogenous substances. The aim of the present study was to investigate the inhibitory effects of carvacrol on major UGT isoforms. The results showed that carvacrol could inhibit the activity of UGT1A9 with negligible effects on other UGT isoforms. When 4-methylumbelliferone (4-MU) was used as a nonspecific probe substrate and recombinant UGT enzymes were utilized as an enzyme resource, the inhibition of UGT1A9 was best fit to the competitive type and the inhibition kinetic parameter (K(i)) was calculated to be 5.7 mu m. Furthermore, another specific probe substrate, propofol, was employed to determine the inhibitory kinetics of UGT1A9, and the results demonstrated that the inhibitory type was noncompetitive. The inhibition kinetic parameter (K(i)) was determined to be 25.0 mu m. Because this substrate-dependent inhibition of UGT1A9 might confuse the in vitroin vivo extrapolation, these in vitro inhibition kinetic parameters should be interpreted with special caution. Copyright (C) 2011 John Wiley & Sons, Ltd.
关键词[WOS]: DRUG-DRUG INTERACTIONS ;  CYTOCHROME-P450 ENZYMES ;  METABOLISM ;  EXPRESSION ;  CYP3A4
语种: 英语
WOS记录号: WOS:000298876700013
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/118366
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.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
2.Acad Mil Med Sci, Affiliated Hosp, Dept Clin Pharmacol, Beijing 100071, Peoples R China
3.Chinese Acad Sci, Grad Sch, Beijing 100049, Peoples R China

Recommended Citation:
Dong, Rui-Hua,Fang, Zhong-Ze,Zhu, Liang-Liang,et al. Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol[J]. PHYTOTHERAPY RESEARCH,2012,26(1):86-90.
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