染料木黄酮在大鼠肝微粒体代谢的酶动力学

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。

Enzyme kinetics of genistein metabolism in rat liver microsomes

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.