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学科主题物理化学
Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol
Dong, Rui-Hua2; Fang, Zhong-Ze1,3; Zhu, Liang-Liang1,3; Liang, Si-Cheng1; Ge, Guang-Bo1; Yang, Ling1; Liu, Ze-Yuan2; Fang ZZ(房中则)
关键词Udp-glucuronosyltransferases (Ugts) Carvacrol Drug-drug Interactions (Ddis)
刊名PHYTOTHERAPY RESEARCH
2012
DOI10.1002/ptr.3525
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
关键词[WOS]DRUG-DRUG INTERACTIONS ; CYTOCHROME-P450 ENZYMES ; METABOLISM ; EXPRESSION ; CYP3A4
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.
语种英语
WOS记录号WOS:000298876700013
引用统计
被引频次:57[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/321008/118366
专题中国科学院大连化学物理研究所
通讯作者Fang ZZ(房中则)
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
推荐引用方式
GB/T 7714
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.
APA Dong, Rui-Hua.,Fang, Zhong-Ze.,Zhu, Liang-Liang.,Liang, Si-Cheng.,Ge, Guang-Bo.,...&房中则.(2012).Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol.PHYTOTHERAPY RESEARCH,26(1),86-90.
MLA Dong, Rui-Hua,et al."Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol".PHYTOTHERAPY RESEARCH 26.1(2012):86-90.
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