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目的:研究乌头碱(AC)在豚鼠和小鼠体外肝微粒体中代谢产物的差异。方法:优化2个种属肝微粒体与AC的P450反应体系,应用高效液相色谱-高分辨质谱联用(HPLC-HRMS)和超高相液相色谱-多级质谱(UPLC-MS/MS)法测定AC在2种肝微粒体中的细胞色素氧化酶(CYP)代谢产物。结果:AC在2种肝微粒体中均代谢产生8种代谢产物,其中6种为CYP代谢产物;脱甲基、脱乙基、脱氢和氧化反应是其主要代谢特征。结论:乌头碱在豚鼠和小鼠体外肝微粒体中的CYP主要代谢途径相同。
Objective: To investigate the differences of metabolites of aconitine (AC) in liver microsomes of guinea pigs and mice in vitro. Methods: The P450 reaction system between two microspheres and AC was optimized. The compounds were characterized by high performance liquid chromatography-high performance liquid chromatography-high performance liquid chromatography-tandem mass spectrometry (HPLC-HRMS) and ultra-high performance liquid chromatography-mass spectrometry ) Assay for cytochrome oxidase (CYP) metabolites of AC in two liver microsomes. Results: AC was metabolized in two kinds of liver microsomes to produce eight metabolites, of which six were CYP metabolites. Demethylation, de-ethylation, dehydrogenation and oxidation were the main metabolic characteristics of AC. Conclusion: The main metabolic pathway of aconitine in liver microsomes of guinea pigs and mice is the same.