Investigation of UDP-glucuronosyltransferases (UGTs) Inhibitory Properties of Carvacrol
文献类型：期刊论文
| 作者 | Dong, Rui-Hua2; Fang, Zhong-Ze1,3; Zhu, Liang-Liang1,3; Liang, Si-Cheng1; Ge, Guang-Bo1; Yang, Ling1; Liu, Ze-Yuan2 |
| 刊名 | phytotherapy research
 |
| 出版日期 | 2012 |
| 卷号 | 26期号:1页码:86-90 |
| 关键词 | UDP-glucuronosyltransferases (UGTs) carvacrol drug-drug interactions (DDIs) |
| 产权排序 | 2,2 |
| 通讯作者 | 房中则 |
| 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. |
| 学科主题 | 物理化学 |
| 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 |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000298876700013 |
| 公开日期 | 2013-10-11 |
| 源URL | [http://159.226.238.44/handle/321008/118366]  |
| 专题 | 大连化学物理研究所_中国科学院大连化学物理研究所 |
| 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.,...&Liu, Ze-Yuan.(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. |
入库方式： OAI收割
来源：大连化学物理研究所
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