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  > 会议论文
学科主题: 物理化学
题名: Inhibitory potential of Chlormadinone acetate (CMA) on five important UDP-Glucuronosyltransferases in human liver
作者: Huang T(黄婷) ;  Fang ZZ(房中则) ;  Zhang YY(张延延) ;  Yang L(杨凌)
会议名称: 9th International Meeting of the International-Society-for-the-Study-of-Xenobiotics
会议日期: 2010-9-4
出版日期: 2010-09-04
会议地点: 土耳其
通讯作者: Ling Yang
部门归属: 十八室
主办者: 国际药物代谢学会
摘要: Chlormadinone acetate (CMA), a derivative of 17-а-hydroxyprogesterone, is used as an orally effective progestogen in hormone replacement therapy(HRT). In 1998, the combined monophasic low-dose oral contraceptive ethinyl estradiol (EE) 0.03 mg and chlormadinone acetate (CMA) 2 mg was approved in Germany. Glucuronidation catalyzed by UDP-glucuronosyltransferase (UGT) is one of the major steps responsible for the metabolism of many drugs, environmental chemicals and endogenous compounds. Pharmacokinetic behaviours of drugs could be altered by inhibition of these UGT isoforms and the search for drugs that potentially inhibit these UGT isoforms is very significant from a clinical point of view. In the present study, the inhibitory potential of five important UDP-Glucuronosyltransferases in human liver (UGT1A1, 1A3, 1A6, 1A9 and 2B7) by CMA was investigated using 4-MU as nonspecific substrate and recombinant UGT isoforms as enzyme sources. The results showed that CMA exhibited inhibitory effects towards UGT1A3 (IC50=8.6±1.4) and UGT2B7 (IC50=14.2±3.8μM), with other UGT isoforms negligibly influenced. The results obtained from Lineweaver-Burk and Dixon plots showed that CMA noncompetitively inhibited UGT1A3 and UGT2B7. The Ki value was calculated to be 36.9μM and 4.1μM for UGT1A3 and UGT2B7, respectively. Considering that UGT1A3 and UGT2B7 are involved in the metabolism of many drugs, special attentions should be paid when CMA was administered with the drugs which mainly experienced UGT1A3,2B7-mediated metabolism.
语种: 中文
Citation statistics: 
内容类型: 会议论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/114338
Appears in Collections:中国科学院大连化学物理研究所_会议论文

Files in This Item:

There are no files associated with this item.


Recommended Citation:
Huang T,Fang ZZ,Zhang YY,et al. Inhibitory potential of Chlormadinone acetate (CMA) on five important UDP-Glucuronosyltransferases in human liver[C]. 见:9th International Meeting of the International-Society-for-the-Study-of-Xenobiotics. 土耳其. 2010-9-4.
Service
 Recommend this item
 Sava as my favorate item
 Show this item's statistics
 Export Endnote File
Google Scholar
 Similar articles in Google Scholar
 [黄婷]'s Articles
 [房中则]'s Articles
 [张延延]'s Articles
CSDL cross search
 Similar articles in CSDL Cross Search
 [黄婷]‘s Articles
 [房中则]‘s Articles
 [张延延]‘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