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目的:以超高效液相质谱联用法鉴定了乔松素在大鼠体内外的代谢产物。方法:分析乔松素经大鼠肝微粒体体外代谢和大鼠口服给药后的胆汁、尿液、粪便中的代谢产物,以超高效液相质谱联用法分离鉴定代谢产物。结果:在大鼠肝微粒体和胆汁、尿液、粪便中共检测到5个代谢产物,根据裂解规律及与标准品对照,鉴定了其中3个代谢产物的结构,推测了另外2个代谢产物的结构。结论:通过大鼠体内外代谢产物的比较,发现乔松素的代谢途径主要是羟基化和葡萄糖醛酸化。其原型和柚皮素是在体内的主要作用形式,在胃肠道及肝脏中的葡萄糖醛酸化是其代谢失活的主要途径。
OBJECTIVE: To identify the metabolites of Qiao Song Su in vivo and in vitro by ultra-high performance liquid chromatography-mass spectrometry. Methods: The metabolites of Qiao-Suo-Su in bile, urine and feces of rat liver microsomes after in vitro metabolism and rat oral administration were analyzed. The metabolites were isolated and identified by ultra-high performance liquid chromatography-mass spectrometry. Results: Five metabolites were detected in liver microsome, bile, urine and feces of rats, and the structures of three metabolites were identified according to the law of cleavage and comparison with standard samples. It was speculated that the other two metabolites structure. CONCLUSION: The metabolic pathway of Qiao Song Su is mainly hydroxylated and glucuronidated through the comparison of metabolites in vivo and in vitro. Its prototype and naringenin are the major forms of action in the body, and glucuronidation in the gastrointestinal tract and liver is the main pathway for their metabolic inactivation.