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
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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
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