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Deglycosylation of Liquiritin Strongly Enhances its Inhibitory Potential Towards UDP-Glucuronosyltransferase (UGT) Isoforms
Guo, Bin1; Fan, Xu-Ran2,3; Fang, Zhong-Ze2,3,5; Cao, Yun-Feng2,3; Hu, Cui-Min5; Yang, Julin6; Zhang, Yan-Yan2,3; He, Rong-Rong4; Zhu, Xu2,3; Yu, Zhen-Wen2,3; Sun, Xiao-Yu2,3; Hong, Mo2,3; Yang, Lu2,3
关键词Udp-glucuronosyltransferase Licorice Liquiritin Liquiritigenin
刊名PHYTOTHERAPY RESEARCH
2013-08-01
DOI10.1002/ptr.4855
27期:8页:1232-1236
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
关键词[WOS]DRUG-DRUG INTERACTIONS
英文摘要The detailed mechanisms on licorice-drug interaction remain to be unclear. The aim of the present study is to investigate the inhibition of important UGT isoforms by two important ingredients of licorice, liquiritin, and liquiritigenin. The results showed that liquiritigenin exhibited stronger inhibition towards all the tested UGT isoforms than liquiritin. Data fitting using Dixon and Lineweaver-Burk plots demonstrated the competitive inhibition of liquiritigenin towards UGT1A1 and UGT1A9-mediated 4-MU glucuronidation reaction. The inhibition kinetic parameters (K-i) were calculated to be 9.1 and 3.2M for UGT1A1 and UGT1A9, respectively. Substrate-dependent inhibition behaviour was also observed for UGT1A1 in the present study. All these results will be helpful for understanding the deep mechanism of licorice-drug interaction. However, when translating these in vitro parameters into in vivo situations, more complex factors should be considered, such as substrate-dependent inhibition of UGT isoforms, the contribution of UGT1A1 and UGT1A9 towards the metabolism of drugs, and many factors affecting the abundance of ingredients in the licorice. Copyright (c) 2012 John Wiley & Sons, Ltd.
语种英语
WOS记录号WOS:000322114900019
引用统计
被引频次:16[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/137786
专题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.Jinan Univ, Coll Pharm, Guangzhou 510632, Guangdong, Peoples R China
5.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA
6.Ningbo Coll Hlth Sci, Ningbo 315100, Zhejiang, Peoples R China
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Guo, Bin,Fan, Xu-Ran,Fang, Zhong-Ze,et al. Deglycosylation of Liquiritin Strongly Enhances its Inhibitory Potential Towards UDP-Glucuronosyltransferase (UGT) Isoforms[J]. PHYTOTHERAPY RESEARCH,2013,27(8):1232-1236.
APA Guo, Bin.,Fan, Xu-Ran.,Fang, Zhong-Ze.,Cao, Yun-Feng.,Hu, Cui-Min.,...&Yang, Lu.(2013).Deglycosylation of Liquiritin Strongly Enhances its Inhibitory Potential Towards UDP-Glucuronosyltransferase (UGT) Isoforms.PHYTOTHERAPY RESEARCH,27(8),1232-1236.
MLA Guo, Bin,et al."Deglycosylation of Liquiritin Strongly Enhances its Inhibitory Potential Towards UDP-Glucuronosyltransferase (UGT) Isoforms".PHYTOTHERAPY RESEARCH 27.8(2013):1232-1236.
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