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Chinese Academy of Sciences Institutional Repositories Grid
Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7

文献类型:期刊论文

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
刊名phytotherapy research
出版日期2013-09-01
卷号27期号:9页码:1358-1361
关键词licorice glycyrrhizic acid glycyrrhetinic acid UDP-glucuronosyltransferases (UGTs) herb-drug interaction
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.
WOS标题词science & technology ; life sciences & biomedicine
类目[WOS]chemistry, medicinal ; pharmacology & pharmacy
研究领域[WOS]pharmacology & pharmacy
关键词[WOS]drug-drug interactions ; human liver ; glucuronidation ; polymorphism ; cells
收录类别SCI
语种英语
WOS记录号WOS:000324024000016
公开日期2015-11-10
源URL[http://159.226.238.44/handle/321008/137736]  
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.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
推荐引用方式
GB/T 7714
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.
APA Huang, Yin-Peng.,Cao, Yun-Feng.,Fang, Zhong-Ze.,Zhang, Yan-Yan.,Hu, Cui-Min.,...&Sun, Hong-Zhi.(2013).Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7.phytotherapy research,27(9),1358-1361.
MLA Huang, Yin-Peng,et al."Glycyrrhetinic Acid Exhibits Strong Inhibitory Effects Towards UDP-Glucuronosyltransferase (UGT) 1A3 and 2B7".phytotherapy research 27.9(2013):1358-1361.

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来源:大连化学物理研究所

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