摘要
目的:探索秦皮乙素和秦皮甲素在大鼠尿液中的代谢物,以期阐明这2种药物在体内作用的化学基础。方法:单次灌胃给药秦皮乙素和秦皮甲素后收集48 h内大鼠尿液,经固相萃取法处理,采用HPLC-MS^n检测代谢产物,色谱条件为流动相甲醇-0.2%甲酸(12∶88),流速1.0 m L·min^(-1),进样量5μL,柱温35℃,检测波长339 nm;质谱条件为电喷雾离子化方式,正离子扫描模式,喷雾电压3.0 k V,碰撞气流量0.16 m L·min^(-1),洗脱溶剂温度350℃,离子源温度450℃。结果:从大鼠尿液中发现并初步鉴定了5个代谢产物的化学结构,主要为秦皮乙素的水解产物、还原产物、甲基化产物及硫酸化产物。结论:推测秦皮甲素在体内先水解为秦皮乙素,再进行水解、还原、甲基化及硫酸化反应。
Objective: To investigate the metabolites of aesculin and aesculetin in rat urine. Method:After single oral administration of aesculin and aesculetin to rats,urine was collected within 48 h and pretreated by solid-phase extraction method. Metabolites were determined by a HPLC-MS^n method. Result: Five major metabolites were found and their chemical structures were elucidated as hydrolysate, reduzate, methylated metabolite and sulfated product, respectively. Conclusion: According to the rule of metabolism, aesculin is hydrolyzed as aesculetin which were further metabolized in vivo. The method can be used to identify the structures of active components responsible for pharmacological effects.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2016年第11期93-96,共4页
Chinese Journal of Experimental Traditional Medical Formulae
基金
国家自然科学基金项目(30960526
81560688)