肉豆蔻木脂素的体外代谢初步研究

In vitro metabolism of myrislignan in the seeds of Myristica fragrans

目的:建立诱导的大鼠肝微粒体药物代谢酶体外转化模型,评价肉豆蔻木脂素的体外代谢情况,为规模化制备肉豆蔻木脂素的代谢产物提供方法。方法:将肉豆蔻木脂素与苯巴比妥诱导的大鼠肝微粒体药物代谢酶共温孵,用高效液相色谱法检测肉豆蔻木脂素及其代谢产物。结果:肉豆蔻木脂素在苯巴比妥诱导的大鼠肝微粒体药物代谢酶作用下,可以被代谢,并且发现了7个代谢产物。结论:建立的肝微粒体药物代谢酶模型可靠有效,可用于肉豆蔻中肉豆蔻木脂素的体外代谢研究。

Objective ： To study the metabolism of myrislignan isolated from the seed of Myristica fragrans Houtt. using in vitro drug-metabolizing enzymes prepared from the phenobarbital-induced rat liver microsomes, and to establish a method to cosmically prepare metabolites of myrislignan. Methods： After incubation of myrislignan with drug-metabolizing enzymes prepared from the phenobarbital-induced rat liver microsomes at 37℃ in vitro, the high-performance liquid chromatography （HPLC） method was applied to analyze myrislignan and its metabolites. Results ： Myrislignan was metabolized by drug-metabolizing enzymes in rat liver microsomes to produce 7 metabolites. Conclusion ： The established drug-metabolizing enzyme model is valid to study the metabolism of myrislignan in vitro.