2种重组人源化葡糖醛酸化转移酶对染料木素代谢的作用研究  

Effects of Two Recombinant Human Glucuronyltransferases Enzymes on the Metabolism of Genistein

作　　者：于红宇 廖景光 陈历雄 唐南[2] 叶玲[2] 刘中秋[2] 

机构地区：[1]广州市番禺区何贤纪念医院药剂科,广州市511400 [2]南方医科大学药学院,广州市510515

出　　处：《中国药房》2009年第13期976-978,共3页China Pharmacy

基　　金：国家"十五"支撑计划课题(2006BAI11B08-04)

摘　　要：目的:比较研究2种重组人源化葡糖醛酸化转移酶UGT1A9和UGT1A10(分别主要存在于肝脏和肠道)对异黄酮类化合物染料木素的代谢作用,预测染料木素的主要代谢途径和机制。方法:采用体外微粒体药物代谢酶孵育法,高效液相色谱法检测染料木素在3个不同浓度(2.5、10、35μmol.L-1)下被2种代谢酶转化为葡糖醛酸结合物的代谢速率。结果:UGT1A9和UGT1A10都对染料木素有显著代谢作用,且随着浓度的增加,代谢速率加快,呈较好的浓度依赖关系,但以UGT1A9代谢速率更快。结论:UGT1A9对染料木素的代谢作用大于UGT1A10,提示染料木素的主要代谢部位在肝脏,但肠道也有部分代谢。OBJECTIVE： To evaluate the effects of two recombinant human glucuronyltransferases UGT1A9 and UGT1A10 （existing in the liver and intestine） on the metabolism of genistein （isoflavones）, and to predicate the chief metabolic channel and its action mechanism. METHODS： By in vitro microsomal drug- metabolizing enzyme incubation method, and the metabolic rate of genistein at different concentrations （2.5, 10, 35μmol·L^-1） converted to glucuronide conjugate by two metabolic enzymes was determined by HPLC. RESULTS： Both UGT1A9 and UGT1A10 exhibited remarkable effects on the metabolism of genistein in concentration-dependent manner, with UGT1A9 showing higher potency. CONCLUSION： The better efficacy of UGTIA9 than that of UGT1A10 for genistein metabolism suggests that the metabolizing of genistein occurred mainly in liver and partially in intestine.

关 键 词：染料木素 UGT1A9 UGT1A10 代谢 

分 类 号：R969.1[医药卫生—药理学]