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	Inhibitory potential of Chlormadinone acetate (CMA) on five important UDP-Glucuronosyltransferases in human liver
	Huang T(黄婷) ; Fang ZZ(房中则) ; Zhang YY(张延延) ; Yang L(杨凌)
	2010-09-04
会议名称	9th international meeting of the international-society-for-the-study-of-xenobiotics
会议日期	2010-9-4
会议地点	土耳其
页码	147/2
通讯作者	ling yang
中文摘要	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.
会议主办者	国际药物代谢学会
学科主题	物理化学
语种	中文
WOS记录号	WOS:000281147700256
内容类型	会议论文
源URL	[http://159.226.238.44/handle/321008/114338]
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
推荐引用方式 GB/T 7714	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.

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