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目的 研究黄皮酰胺在大鼠体内的代谢转化途径。方法 收集ip给药后大鼠的尿液、粪便及血液进行分析 ,寻找已知的代谢产物并通过HPLC DAD和HPLC MS分析寻找未知的代谢产物 ,确定大鼠体内的主要代谢途径。并通过比较 (+ ) ,(- ) 黄皮酰胺代谢的差异 ,初步研究其代谢转化的立体选择性。结果 HPLC分析发现 ,大鼠肝微粒体中所分离得到的 6个主要代谢产物均在体内存在 ,(+ ) ,(- ) 黄皮酰胺的代谢有明显的差异 ,根据MS碎片信息确定了一个新的代谢产物的结构 ,即N 去甲黄皮酰胺。结论 手性黄皮酰胺主要在肝脏中发生羟基化代谢反应 ,并有明显的立体选择性
Objective To investigate the metabolic pathway of clausenamide in rats. Methods The urine, feces and blood of rats were collected after ip administration to find out the known metabolites. The unknown metabolites were identified through HPLC DAD and HPLC MS analysis to determine the main metabolic pathways in rats. And by comparing the (+), (-) metabolism of clausenamide, the preliminary study of its stereospecificity of metabolic transformation. Results The HPLC analysis showed that the six major metabolites isolated from rat liver microsomes were all present in the body. The metabolites of (+) and (-) clausenamide were significantly different, and a new The structure of the metabolite, ie N-desmethylamide. Conclusion Chiral yellow amide mainly in the liver hydroxylation metabolic reaction, and significant stereoselectivity