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目的建立测定大鼠肝微粒体中有机锡抗癌化合物DBDCT的方法并研究其相应的酶促动力学。方法采用HPLC测定DBDCT在体外代谢系统中的酶促动力学,用Eadie-Hofstee法分析数据,求算酶促动力学参数Km和Vmax以及肝代谢速率Clin。结果在体外代谢系统中,DBDCT代谢酶促动力学参数Km=159.07μmol·L-1,Vmax=2.813μmol·(min·mg)-1以及肝清除率Clin=Vmax/Km=0.017L·(min·mg)-1。结论此分析方法符合方法学验证要求且简单准确,可满足DBDCT体外代谢的研究。
Objective To establish a method for the determination of organotin anticancer compound DBDCT in rat liver microsomes and to study its corresponding enzymatic kinetics. Methods The enzymatic kinetics of DBDCT in the in vitro metabolic system was determined by HPLC. The data were analyzed by Eadie-Hofstee method to calculate the kinetic parameters Km and Vmax and the liver metabolic rate Clin. Results In in vitro metabolic system, the kinetic parameters of DBDCT metabolism were Km = 159.07μmol·L-1, Vmax = 2.813μmol · (min · mg) -1 and hepatic clearance rate Clin = Vmax / Km = 0.017L · min · Mg) -1. Conclusion This method meets the verification requirements of methodology and is simple and accurate to meet the in vitro metabolism of DBDCT.