染料木黄酮在雌雄大鼠肝微粒体中的代谢差异  

Gender-based differences in genistein metabolism in rat liver microsomes

作　　者：王汝涛[1] 周四元[1] 梅其炳[1] 戴兴凌[2] 冉玉华[1] 刘振国[1] 

机构地区：[1]第四军医大学药学系药理学教研室,陕西西安710033 [2]解放军第三二三医院,陕西西安710054

出　　处：《中国药理学通报》2006年第7期811-814,共4页Chinese Pharmacological Bulletin

基　　金：国家高技术研究发展计划(863计划)资助项目(No2003AA2Z347C)

摘　　要：目的研究染料木黄酮在♀、♂大鼠肝微粒体中的代谢差异。方法制备♀、♂大鼠肝微粒体,确定染料木黄酮代谢的酶动力学条件,分别用CYP1A2抗体和选择性CYP1A2抑制剂呋喃茶碱与大鼠肝微粒体和染料木黄酮共同温孵,测定染料木黄酮在♀、♂大鼠肝微粒体中的代谢速率,评价♀、♂大鼠CYP1A2的相对百分比活性。结果在CYP1A2抗体浓度为1∶400,孵育时间为30 m in条件下,♂大鼠肝微粒体代谢染料木黄酮的相对代谢率为(20.95±2.13)%,♀动物为(13.73±1.26)%。在选择性CYP1A2抑制剂呋喃茶碱浓度为3.125μmol.L-1,孵育时间为30 m in条件下,♂动物为(58.02±3.35)%,而♀大鼠肝微粒体代谢染料木黄酮的相对代谢率为(43.82±2.65)%,两者之间差异有显著性(P<0.01)。结论染料木黄酮在♂大鼠肝微粒体中代谢较♀大鼠快,提示♂大鼠肝微粒体CYP1A2酶活性高于♀大鼠。Aim To study the gender-based difference in genistein metabolism in rat liver microsomes in vitro. Methods Liver microsomes was obtained from male and female rats. The optimized system of enzyme catalytic reaction of genistein in rat liver microsomes was set up. The reaction velocity of genistein in female and male rat liver microsomes was assessed by incubating genistein with CYP1A2 antibody or specific CYP1A2 inhibitor furafylline, and the percentage of the relative metabolism of genistein of CYP1 A2 was derivated by using the data of the reaction velocity. Results The metabolism of genistein by microsomes was inhibited by CYP1 A2 antibody （ 1 ： 400 ） after incubation for 30 min. The percentage of the control metabolism of genistein of microsomes in male and female rat were 20. 95% ± 2. 13% and 13.73% ± 1.26% respectively （P 〈 0.01 ）. The percentage of the control metabolism of genistein of microsomes in male and female rat were 58.02% ± 3.35% and 43.82% ± 2.65% respectively （P 〈 0. 01 ） at the present of specific CYP1 A2 inhibitor furafylline 3. 125 μmol· L^-1. Conclusion The results indicated that the activity of male rat liver CYP1A2 was higher than that of the female rat. The gender-based differences of genistein metabolism existed in rat liver microsomes.

关 键 词：染料木黄酮 肝微粒体 CYP1A2 

分 类 号：R-332[医药卫生] R282.71