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目的:研究大鼠口服棉花皮素-8-O-β-D-葡萄糖醛酸苷后尿液中的代谢产物。方法:健康大鼠口服250mg·kg-1棉花皮素-8-O-β-D-葡萄糖醛酸苷后,收集0～48h的尿样,经HPD-600大孔吸附树脂分离纯化后采用HPLC-DAD-MSn方法对尿样中的原形药物及其代谢产物进行分析及结构推测。结果:在大鼠尿液中检测到棉花皮素-8-O-β-D-葡萄糖醛酸苷的6个主要代谢产物,根据负离子模式下电喷雾质谱的裂解规律、紫外光谱特征以及与标准品对照的方法,鉴定了其中1个代谢产物的结构,推测了其他5个代谢产物的结构,其代谢过程主要是葡萄糖醛酸化、脱葡萄糖醛酸以及甲基化等。结论:本文建立的方法快速、灵敏,可用于棉花皮素-8-O-β-D-葡萄糖醛酸苷及其体内外代谢产物的研究。
OBJECTIVE: To study the metabolites in urine of rats after oral administration of cottonseedin-8-O-β-D-glucuronide. Methods: After oral administration of 250mg · kg-1 cottonseedin-8-O-β-D-glucuronide, the urine samples of 0-48h were collected from healthy rats and purified by HPD-600 macroporous resin. -DAD-MSn method was used to analyze and structure the prototype drugs and their metabolites in urine samples. Results: Six major metabolites of cottonseedin-8-O-β-D-glucuronide were detected in the urine of rats. According to the cleavage rules of electrospray ionization mass spectrometry in negative ion mode, The structure of one of the metabolites was identified and the structures of the other five metabolites were speculated. The metabolic processes were mainly glucuronidation, glucuronic acid and methylation. Conclusion: The method established in this paper is rapid and sensitive and can be applied to the study of cottonseedin-8-O-β-D-glucuronide and its metabolites in vitro and in vivo.