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Structure-Activity Relationship and Substrate-Dependent Phenomena in Effects of Ginsenosides on Activities of Drug-Metabolizing P450 Enzymes

文献类型：期刊论文

作者Hao, Miao1; Zhao, Yuqing2; Chen, Peizhan1; Huang, He3; Liu, Hong3; Jiang, Hualiang3; Zhang, Ruiwen4; Wang, Hui1
刊名PLOS ONE
出版日期2008-07-16
卷号3期号:7
ISSN号1932-6203
DOI10.1371/journal.pone.0002697
文献子类Article
英文摘要Ginseng, a traditional herbal medicine, may interact with several co-administered drugs in clinical settings, and ginsenosides, the major active components of ginseng, may be responsible for these ginseng-drug interactions (GDIs). Results from previous studies on ginsenosides' effects on human drug-metabolizing P450 enzymes are inconsistent and confusing. Herein, we first evaluated the inhibitory effects of fifteen ginsenosides and sapogenins on human CYP1A2, CYP2C9, CYP2C19, CYP2D6 and CYP3A4 enzymes by using commercially available fluorescent probes. The structure-activity relationship of their effects on the P450s was also explored and a pharmacophore model was established for CYP3A4. Moreover, substrate-dependent phenomena were found in ginsenosides' effects on CYP3A4 when another fluorescent probe was used, and were further confirmed in tests with conventional drug probes and human liver microsomes. These substrate-dependent effects of the ginsenosides may provide an explanation for the inconsistent results obtained in previous GDI reports.
资助项目Science and Technology Commission of Shanghai Municipality[00000000] ; Pujiang Talent Program[00000000] ; Ministry of Science and Technology of China (973 Program)[00000000] ; Knowledge Innovation Program of Chinese Academy of Sciences, Food Safety Research Center and Key Laboratory of Nutrition and Metabolism in INS[00000000] ; NIH/NCI[00000000] ; [06DZ19021] ; [06PJ14107] ; [2007CB947100] ; [R01 CA112029] ; [R01 CA121211]
WOS研究方向Science & Technology - Other Topics
语种英语
WOS记录号WOS:000264057200040
出版者PUBLIC LIBRARY SCIENCE
源URL[http://119.78.100.183/handle/2S10ELR8/272864]  
专题药物化学研究室
药物发现与设计中心
通讯作者Hao, Miao
作者单位1.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Nutr Sci, Key Lab Nutr & Metab, Shanghai, Peoples R China;
2.Shenyang Pharm Univ, Shenyang, Peoples R China;
3.Chinese Acad Sci, Shanghai Inst Mat Med, Drug Discovery & Design Ctr, Shanghai, Peoples R China;
4.Univ Alabama, Comprehensive Canc Ctr, Div Clin Pharmacol, Dept Pharmacol & Toxicol, Birmingham, AL USA
推荐引用方式
GB/T 7714		 Hao, Miao,Zhao, Yuqing,Chen, Peizhan,et al. Structure-Activity Relationship and Substrate-Dependent Phenomena in Effects of Ginsenosides on Activities of Drug-Metabolizing P450 Enzymes[J]. PLOS ONE,2008,3(7).
APA Hao, Miao.,Zhao, Yuqing.,Chen, Peizhan.,Huang, He.,Liu, Hong.,...&Wang, Hui.(2008).Structure-Activity Relationship and Substrate-Dependent Phenomena in Effects of Ginsenosides on Activities of Drug-Metabolizing P450 Enzymes.PLOS ONE,3(7).
MLA Hao, Miao,et al."Structure-Activity Relationship and Substrate-Dependent Phenomena in Effects of Ginsenosides on Activities of Drug-Metabolizing P450 Enzymes".PLOS ONE 3.7(2008).

入库方式： OAI收割

来源：上海药物研究所

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