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Strong inhibitory effect of medroxyprogesterone acetate (MPA) on UDP-glucuronosyltransferase (UGT) 2B7 might induce drug-drug interactions
Huang, T.2; Fang, Z. Z.4; Yang, L.1
刊名PHARMAZIE
2010-12-01
DOI10.1691/ph.2010.0671
65期:12页:919-921
收录类别SCI
文章类型Article
WOS标题词Science & Technology ; Life Sciences & Biomedicine ; Physical Sciences
类目[WOS]Chemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
研究领域[WOS]Pharmacology & Pharmacy ; Chemistry
关键词[WOS]BREAST-CANCER ; GLUCURONIDATION ; WOMEN
英文摘要The aim of the present study was to investigate the inhibitory effects of medroxyprogesterone acetate (MPA) on four important UGT isoforms (UGT1A1, 1A6, 1A9 and 2B7). 4-methylumbelliferone (4-MU) was used as a nonselective substrate, and recombinant UGT isoforms were utilized as an enzyme source. The results showed that MPA exhibited inhibitory effects on UGT2B7 (IC(50) = 29.3 +/- 1.5 mu M), with a negligible influence on other UGT isoforms. The results obtained from Lineweaver-Burk and Dixon plots showed that MPA competitively inhibited UGT2B7. The K(i) value was calculated to be 7.2 mu M. Based on the concentration of MPA in human liver, the magnitude of in vivo drug-drug interaction (DDI) was predicted. The [1]/K(i) value was calculated to be 0.31, which suggested that DDIs might occur when MPA was co-administered with drugs which mainly undergo UGT2B7-mediated metabolism.
语种英语
WOS记录号WOS:000285986600012
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文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/142187
专题中国科学院大连化学物理研究所
作者单位1.Chinese Acad Sci, Dalian Inst Chem Phys, Lab Pharmaceut Resource Discovery, Dalian 116023, Peoples R China
2.Shanghai Inst Planned Parenthood Res, Natl Populat & Family Planning Key Lab Contracept, Shanghai, Peoples R China
3.Chinese Acad Sci, Inst Chem Phys, Dalian 116023, Peoples R China
4.Chinese Acad Sci, Grad Sch, Beijing, Peoples R China
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Huang, T.,Fang, Z. Z.,Yang, L.. Strong inhibitory effect of medroxyprogesterone acetate (MPA) on UDP-glucuronosyltransferase (UGT) 2B7 might induce drug-drug interactions[J]. PHARMAZIE,2010,65(12):919-921.
APA Huang, T.,Fang, Z. Z.,&Yang, L..(2010).Strong inhibitory effect of medroxyprogesterone acetate (MPA) on UDP-glucuronosyltransferase (UGT) 2B7 might induce drug-drug interactions.PHARMAZIE,65(12),919-921.
MLA Huang, T.,et al."Strong inhibitory effect of medroxyprogesterone acetate (MPA) on UDP-glucuronosyltransferase (UGT) 2B7 might induce drug-drug interactions".PHARMAZIE 65.12(2010):919-921.
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