中国科学院机构知识库网格
Chinese Academy of Sciences Institutional Repositories Grid
Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation

文献类型:期刊论文

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
刊名fitoterapia
出版日期2013
卷号84页码:208-212
关键词Isoliquiritigenin UDP-glucuronosyltransferase (UGT) Enzyme inhibition
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.
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]dalbergia-odorifera ; drug-interactions ; gilbert-syndrome ; cancer ; identification ; metabolism ; cells ; polymorphism ; expression ; induction
收录类别SCI
语种英语
WOS记录号WOS:000316531400029
公开日期2015-11-10
源URL[http://159.226.238.44/handle/321008/137925]  
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.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
推荐引用方式
GB/T 7714
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.
APA Lu, Hang.,Fang, Zhong-Ze.,Cao, Yun-Feng.,Hu, Cui-Min.,Hong, Mo.,...&Sun, Hongzhi.(2013).Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation.fitoterapia,84,208-212.
MLA Lu, Hang,et al."Isoliquiritigenin showed strong inhibitory effects towards multiple UDP-glucuronosyltransferase (UGT) isoform-catalyzed 4-methylumbelliferone (4-MU) glucuronidation".fitoterapia 84(2013):208-212.

入库方式: OAI收割

来源:大连化学物理研究所

浏览0
下载0
收藏0
其他版本

除非特别说明,本系统中所有内容都受版权保护,并保留所有权利。