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题名: The Inhibitory Effect of 20(S)-Protopanaxatriol (ppt) Towards UGT1A1 and UGT2B7
作者: He, Ya-Jun1, 3;  Fang, Zhong-Ze2;  Ge, Guang-Bo2;  Jiang, Peng3;  Jin, Hui-Zi1;  Zhang, Wei-Dong1, 3;  Yang, Ling2
关键词: ginseng ;  UDP-glucuronosyltransferases (UGTs) ;  herb-drug interaction
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2013-04-01
DOI: 10.1002/ptr.4755
卷: 27, 期:4, 页:628-632
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Medicinal ;  Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
英文摘要: Ginseng, a commonly used natural product, has been frequently reported to induce herbdrug interaction with many clinical drugs. The intestinal bacterial metabolites of ginsenosides have been widely regarded as the substance basis for ginsengdrug interactions. To date, little is known about the inhibitory effect of intestinal bacterial metabolites of ginsenosides towards UDP-glucuronosyltransferases (UGTs). In vitro investigation of the inhibition of 20(S)-protopanaxatriol (ppt) towards UGT1A1 and UGT2B7 was carried out. The results showed that ppt exhibited strong noncompetitive inhibition towards UGT1A1 and competitive inhibition towards UGT2B7. The inhibition kinetic parameters (Ki) were calculated to be 8.8 and 2.2 M for UGT1A1 and UGT2B7, respectively. Using the maximum plasma concentration of ppt, the alteration of area under the concentrationtime curve was calculated to be 20% and 70% respectively for UGT1A1-mediated and UGT2B7-mediated metabolism. However, given that the varied contribution of these two UGT isoforms towards drug metabolism and the influence of herb complexity and individual difference, the explanation of these results should be paid more caution. Copyright (c) 2012 John Wiley & Sons, Ltd.
关键词[WOS]: INTESTINAL BACTERIAL METABOLITE ;  UDP-GLUCURONOSYLTRANSFERASES ;  HUMAN LIVER ;  CYTOCHROME-P450 ENZYMES ;  GINSENOSIDE METABOLITES ;  DRUG INTERACTIONS ;  GLUCURONIDATION ;  BIOACTIVATION ;  SPECIFICITY ;  CYP2C9
语种: 英语
WOS记录号: WOS:000317685800021
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/137942
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.Shanghai Jiao Tong Univ, Sch Pharm, Shanghai 200240, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
3.Second Mil Med Univ, Sch Pharm, Shanghai 200433, Peoples R China

Recommended Citation:
He, Ya-Jun,Fang, Zhong-Ze,Ge, Guang-Bo,et al. The Inhibitory Effect of 20(S)-Protopanaxatriol (ppt) Towards UGT1A1 and UGT2B7[J]. PHYTOTHERAPY RESEARCH,2013,27(4):628-632.
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