DICP OpenIR
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
Source PublicationPHARMAZIE
2010-12-01
DOI10.1691/ph.2010.0671
Volume65Issue:12Pages:919-921
Indexed BySCI
SubtypeArticle
WOS HeadingsScience & Technology ; Life Sciences & Biomedicine ; Physical Sciences
WOS SubjectChemistry, Medicinal ; Chemistry, Multidisciplinary ; Pharmacology & Pharmacy
WOS Research AreaPharmacology & Pharmacy ; Chemistry
WOS KeywordBREAST-CANCER ; GLUCURONIDATION ; WOMEN
AbstractThe 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.
Language英语
WOS IDWOS:000285986600012
Citation statistics
Cited Times:22[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://cas-ir.dicp.ac.cn/handle/321008/142187
Collection中国科学院大连化学物理研究所
Affiliation1.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
Recommended Citation
GB/T 7714
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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