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题名: Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7
作者: Huang, Yin-Peng1;  Cao, Yun-Feng2, 3;  Fang, Zhong-Ze2, 3, 4;  Zhang, Yan-Yan2, 3;  Hu, Cui-Min4;  Sun, Xiao-Yu2, 3;  Yu, Zhen-Wen2, 3;  Zhu, Xu2, 3;  Hong, Mo2, 3;  Yang, Lu2, 3;  Sun, Hong-Zhi1, 2, 3
关键词: licorice ;  glycyrrhizic acid ;  glycyrrhetinic acid ;  UDP-glucuronosyltransferases (UGTs) ;  herb-drug interaction
刊名: PHYTOTHERAPY RESEARCH
发表日期: 2013-09-01
DOI: 10.1002/ptr.4875
卷: 27, 期:9, 页:1358-1361
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: The aim of the present study is to evaluate the inhibitory effects of liver UDP-glucuronosyltransferases (UGTs) by glycyrrhizic acid and glycyrrhetinic acid, which are the bioactive ingredients isolated from licorice. The results showed that glycyrrhetinic acid exhibited stronger inhibition towards all the tested UGT isoforms, indicating that the deglycosylation process played an important role in the inhibitory potential towards UGT isoforms. Furthermore, the inhibition kinetic type and parameters were determined for the inhibition of glycyrrhetinic acid towards UGT1A3 and UGT2B7. Data fitting using Dixon and Lineweaver-Burk plots demonstrated that the inhibition of UGT1A3 and UGT2B7 by glycyrrhetinic acid was best fit to competitive and noncompetitive type, respectively. The second plot using the slopes from Lineweaver-Burk plots versus glycyrrhetinic acid concentrations was employed to calculate the inhibition kinetic parameters (K-i), and the values were calculated to be 0.2 and 1.7M for UGT1A3 and UGT2B7, respectively. All these results remind us the possibility of UGT inhibition-based herb-drug interaction. However, the explanation of these in vitro parameters should be paid more caution due to complicated factors, including the probe substrate-dependent UGT inhibition behaviour, environmental factors affecting the abundance of herbs' ingredients, and individual difference of pharmacokinetic factors. Copyright (c) 2012 John Wiley & Sons, Ltd.
关键词[WOS]: DRUG-DRUG INTERACTIONS ;  HUMAN LIVER ;  GLUCURONIDATION ;  POLYMORPHISM ;  CELLS
语种: 英语
WOS记录号: WOS:000324024000016
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/137736
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.Liaoning Med Univ, Affiliated Hosp 1, Jinzhou 121001, Peoples R China
2.Chinese Acad Sci, Dalian Inst Chem Phys, Joint Ctr Translat Med, Dalian 116023, Peoples R China
3.Liaoning Med Univ, Affiliated Hosp 1, Dalian 116023, Peoples R China
4.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA

Recommended Citation:
Huang, Yin-Peng,Cao, Yun-Feng,Fang, Zhong-Ze,et al. Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7[J]. PHYTOTHERAPY RESEARCH,2013,27(9):1358-1361.
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