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为了研究葛根素单体和葛根提取物中的葛根素在大鼠肝微粒体中的代谢是否存在差异,建立微粒体孵育体系。采用高效液相色谱法测定葛根素在肝微粒体代谢系统中的含量,并应用GraphPad Prism 5.0软件分析数据,计算酶促反应动力学参数。在体外代谢系统中,葛根素单体的酶促反应动力学参数K_m为(0.93±0.17)μmol/L,V_(max)为(93.59±2.82) nmol/min·mg,CL_(int)(V_(max)/K_m)为(100.6±1.07) mL/min·mg;葛根提取物中葛根素的相应的动力学参数分别为(1.02±0.09)μmol/L,(22.48±1.53) nmol/min·mg和(22.04±1.72) mL/min·mg。葛根素单体和葛根提取物中的葛根素在大鼠肝微粒体的代谢存在明显的差异,葛根素单体的代谢速度快于葛根提取物中的葛根素的代谢速度。结果提示中药提取物中的其它成分可影响有效成分单体的代谢过程。
In order to study whether the puerarin in puerarin and Pueraria lobata extract had different metabolism in rat liver microsomes, a microsomal incubation system was established. The content of puerarin in the microsomes of liver microsomes was determined by high performance liquid chromatography (HPLC), and the data were analyzed by GraphPad Prism 5.0 software to calculate the enzymatic kinetic parameters. In the in vitro metabolic system, the kinetic parameters Kp of puerarin were (0.93 ± 0.17) μmol / L, V max (93.59 ± 2.82) nmol / min · mg and CL_ (int) (100.6 ± 1.07) mL / min · mg. The corresponding kinetic parameters of puerarin in Pueraria lobata extract were (1.02 ± 0.09) μmol / L and (22.48 ± 1.53) nmol / min · mg and (22.04 ± 1.72) mL / min · mg. The metabolism of puerarin in puerarin and Pueraria lobata extract in rat liver microsomes was significantly different. The metabolism of puerarin monomer was faster than the puerarin in pueraria extract. The results suggest that other components of traditional Chinese medicine extract can affect the metabolism of the active ingredient monomer.