中国科学院大连化学物理研究所机构知识库
Advanced  
DICP OpenIR  > 中国科学院大连化学物理研究所  > 期刊论文
题名: Strong inhibitory effect of medroxyprogesterone acetate (MPA) on UDP-glucuronosyltransferase (UGT) 2B7 might induce drug-drug interactions
作者: Huang, T.2;  Fang, Z. Z.4;  Yang, L.1
刊名: PHARMAZIE
发表日期: 2010-12-01
DOI: 10.1691/ph.2010.0671
卷: 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
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.
关键词[WOS]: BREAST-CANCER ;  GLUCURONIDATION ;  WOMEN
语种: 英语
WOS记录号: WOS:000285986600012
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/142187
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

Files in This Item:

There are no files associated with this item.


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

Recommended Citation:
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.
Service
 Recommend this item
 Sava as my favorate item
 Show this item's statistics
 Export Endnote File
Google Scholar
 Similar articles in Google Scholar
 [Huang, T.]'s Articles
 [Fang, Z. Z.]'s Articles
 [Yang, L.]'s Articles
CSDL cross search
 Similar articles in CSDL Cross Search
 [Huang, T.]‘s Articles
 [Fang, Z. Z.]‘s Articles
 [Yang, L.]‘s Articles
Related Copyright Policies
Null
Social Bookmarking
  Add to CiteULike  Add to Connotea  Add to Del.icio.us  Add to Digg  Add to Reddit 
所有评论 (0)
暂无评论
 
评注功能仅针对注册用户开放,请您登录
您对该条目有什么异议,请填写以下表单,管理员会尽快联系您。
内 容:
Email:  *
单位:
验证码:   刷新
您在IR的使用过程中有什么好的想法或者建议可以反馈给我们。
标 题:
 *
内 容:
Email:  *
验证码:   刷新

Items in IR are protected by copyright, with all rights reserved, unless otherwise indicated.

 

 

Valid XHTML 1.0!
Powered by CSpace