染料木黄酮在大鼠肝微粒体代谢的酶动力学  

Enzyme kinetics of genistein metabolism in rat liver microsomes

作　　者：王汝涛[1] 周四元[1] 梅其炳[1] 杨志福[1] 刘振国[1] 刘琳娜[1] 

机构地区：[1]第四军医大学基础部药理学教研室

出　　处：《中国临床药理学与治疗学》2005年第3期294-297,共4页Chinese Journal of Clinical Pharmacology and Therapeutics

摘　　要：目的:体外研究大鼠肝微粒体中染料木黄酮代谢的酶动力学,及选择性细胞色素(CYP)酶抑制剂对其代谢的影响。方法:用大鼠肝微粒体研究染料木黄酮代谢的酶动力学,探讨CYP酶的选择性抑制剂对其代谢的影响及参与其代谢的CYP酶。结果:CYP1A2抑制剂呋喃茶碱可以显著地抑制染料木黄酮代谢,使染料木黄酮的代谢速率下降。而其它CYP特异性抑制剂对染料木黄酮代谢没有明显的影响。结论:CYP1A2参与了染料木黄酮的代谢,CYP1A2的抑制剂可能会与染料木黄酮发生代谢相互作用,从而降低染料木黄酮的代谢速率。AIM: To study the enzyme kinetics of genistein metabolism and the effects of selective CYP450 inhibitors on the metabolism of genistein in rat liver microsomes. METHODS: Rat liver microsome was used to perform enzyme kinetic studies. Various selective CYP inhibitors were used to investigate their inhibitory effects on the metabolism of genistein and the principal CYP isoform involved in genistein metabolicly ring. RESULTS: The metabolism of genistein was significantly inhibited by furafylline while quinidine, sulfaphenazole, tranylcypromine diethyldithiocarbamate and ketoconazole showed little inhibitory effect on the metabolism of genistein. CONCLUSION: CYP1A2 is involved in genistein metabolism. CYP1A2 inhibitors and genistein may interact metabolicly, thereby reduced the rate of genistein metabolism.

关 键 词：染料木黄酮 微粒体 药代动力学 酶动力学 细胞色素酶 植物雌激素 

分 类 号：R965.2[医药卫生—药理学]