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目的研究蛇床夫内酯在大鼠肝微粒体中的酶促反应动力学。方法以回芹内酯为内标,采用液质联用(LC/MS)的方法测定蛇床夫内酯在体外代谢中的代谢产物3″,8-甲氧基异欧前胡内酯(M1)和5″-羟基-8-甲氧基异欧前胡内酯(M2)。用Linewrave-Burk作图分析数据,计算酶促动力学常数。结果代谢物M1的Vmax=1.152 5μmol.(min.mg pro)-1,Km=133.156 6μmol.L-1,M2的Vmax=1.630 8μmol.(min.mg pro)-1,Km=292.857 1μmol.L-1。结论该方法简单、快速、可靠,适用于蛇床夫内酯的体外代谢研究。
Objective To study the enzymatic reaction kinetics of snakebide lactone in rat liver microsomes. Methods Metoclaurylalcohol was used as internal standard and the metabolites of snakefrolactone in vitro were determined by liquid chromatography-mass spectrometry (LC / MS) 3 “ M1) and 5 ”-hydroxy-8-methoxy iso-iso-pre-lactone (M2). Data were analyzed using Linewrave-Burk mapping to calculate enzymatic kinetic constants. Results Vmax of metabolite M1 was 1.152 5 μmol. (Min.mg pro) -1, Km = 133.156 6 μmol.L-1, Vmax of M2 was 1.630 8 μmol. (Min.mg pro) -1, Km = 292.857 1 μmol·L -1. Conclusion The method is simple, rapid and reliable and is suitable for the in vitro metabolism studies of.