大鼠肝肠不同微粒体药物代谢酶对黄芩素葡糖醛酸酸化代谢物的影响研究

Effects of Various Microsomal Drug-metabolizing Enzymes on Specific Glucuronidation of Baicalein in Rats' Liver and Intestine

目的:探讨肝肠器官对黄芩素代谢的影响。方法:采用体外微粒体药物代谢酶孵育法,在不同孵育时间和不同浓度下,运用高效液相色谱(HPLC)法测定黄芩素及其葡糖醛酸酸化代谢物的含量。探讨大鼠肝肠不同微粒体对黄芩素葡糖醛酸酸化代谢产物生成速率的影响。结果:不同微粒体药物代谢酶对黄芩素均有代谢作用,且随孵育时间延长代谢作用增加,呈较好的时间和剂量依赖关系,其中十二指肠微粒体代谢作用最强,肝脏代谢作用最弱。结论:黄芩素在肝肠器官有较强的代谢,主要代谢部位是肠道。

OBJECTIVE： To investigate the effect of rat liver and intestine on the metabolism of Baicalein.METHODS： The microsomal drug metabolizing enzyme incubation method was employed, and the contents of bacicalein and its glucuronidation metabolite at different incubation time were determiend by HPLC. The effects of various microsomes on the glucuronidation rates of Baicalein were studied.RESULTS： Different microsomal drugmetabolizing enzymes contributed to the metabolism of Baicalein in time - and concentration dependent manner, with Jejunum microsome the strongest while the colon microsome the weakest in efficacy.CONCLUSION： Baicalein had a strong metabolism in liver and intestine especially in the intestine.