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题名: Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation
作者: Lu, Hang1;  Fang, Zhong-Ze2, 3, 5;  Cao, Yun-Feng2, 3, 4;  Hu, Cui-Min5;  Hong, Mo2, 3;  Sun, Xiao-Yu2, 3;  Li, Hua1;  Liu, Yan1;  Fu, Xiaoguang1;  Sun, Hongzhi1
关键词: Isoliquiritigenin ;  UDP-glucuronosyltransferase (UGT) ;  Enzyme inhibition
刊名: FITOTERAPIA
发表日期: 2013
DOI: 10.1016/j.fitote.2012.12.002
卷: 84, 页:208-212
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: Isoliquiritigenin, a herbal ingredient with chalcone structure, has been speculated to be able to inhibit one of the most drug-metabolizing enzymes (DMEs) UDP-glucuronosyltransferase (UGT). Therefore, the aim of the present study was to investigate the inhibition of isoliquiritigenin towards important UGT isoforms in the liver and intestine, including UGT1A1, 1A3, 1A6, 1A7, 1A8, 1A9 and 1A10. The recombinant UGT-catalyzed 4-methylumbelliferone (4-MU) glucuronidation was used as probe reactions. The results showed that 100 mu M of isoliquiritigenin inhibited the activity of UGT1A1, UGT1A3, UGT1A6, UGT1A7, UGT1A8, UGT1A9, and UGT1A10 by 95.2%, 76.1%, 78.9%, 87.2%, 67.2%, 94.8%, and 91.7%, respectively. The data fitting using Dixon plot and Lineweaver-Burk plot showed that the inhibition of UGT1A1, UGT1A9 and UGT1A10 by isoliquiritigenin was all best fit to the competitive inhibition, and the second plot using the slopes from the Lineweaver-Burk plot versus isoliquiritigenin concentrations was used to calculate the inhibition kinetic parameter (K-i) to be 0.7 mu M, 0.3 mu M, and 18.3 mu M for UGT1A1, UGT1A9, and UGT1A10, respectively. All these results indicated the risk of clinical application of isoliquiritigenin on the drug-drug interaction and other possible diseases induced by the inhibition of isoliquiritigenin towards these UGT isoforms. (c) 2012 Published by Elsevier B.V.
关键词[WOS]: DALBERGIA-ODORIFERA ;  DRUG-INTERACTIONS ;  GILBERT-SYNDROME ;  CANCER ;  IDENTIFICATION ;  METABOLISM ;  CELLS ;  POLYMORPHISM ;  EXPRESSION ;  INDUCTION
语种: 英语
WOS记录号: WOS:000316531400029
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/137925
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.Shanghai Inst Planned Parenthood Res, Shanghai Engineer & Technol Res Ctr Reprod Hlth D, Key Lab Contracept & Devices Res NPFPC, Shanghai 200032, Peoples R China
5.NCI, Lab Metab, Ctr Canc Res, Bethesda, MD 20892 USA

Recommended Citation:
Lu, Hang,Fang, Zhong-Ze,Cao, Yun-Feng,et al. Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation[J]. FITOTERAPIA,2013,84:208-212.
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