摘要
研究瑞香素在大鼠肠壁产生的代谢产物。采用大鼠在体肠灌流模型,分别收集瑞香素0～2 h内的十二指肠、空肠、回肠和结肠灌流液,以液相色谱-四级杆飞行时间串联质谱法分析肠道灌流液中瑞香素的代谢产物。在大鼠十二指肠、空肠、回肠灌流液中共发现瑞香素原形药物和4个代谢产物,分别推测为瑞香素-7-硫酸酯、瑞香素-8-硫酸酯、瑞香素-7-葡糖醛酸结合物和瑞香素-8-葡糖醛酸结合物;而在结肠灌流液中未发现代谢产物。在瑞香素的4个代谢产物中,瑞香素-7-硫酸酯和瑞香素-8-硫酸酯(m/z 257)为首次发现的瑞香素在大鼠体内的Ⅱ相代谢产物,揭示了其在大鼠体内代谢的新途径。
In this study,daphnetin and its major metabolites in the intestinal wall of rats were identified by liquid chromatography and quatrupole-time of flight mass spectrometry.Perfusion fluid of duodenum,jejunum,ileum and colon were collected separately for 2 hours from the rat intestine following perfusion with daphnetin.The metabolites of daphnetin in the perfusion fluid of different intestine segments were analyzed by the liquid chromatography and quatrupole-time of flight mass spectrometry.It is shown that the parent drug daphnetin and four metabolites were found in the perfusion fluid of duodenum,jejunum and ileum.However,no metabolites were found in the colon.Among the four metabolites,two daphnetin sulfates（m/z 257） were first discovered as the phase II metabolites of daphnetin in rats,which revealed a new way of daphnetin metabolism in rats.
出处
《药学学报》
CAS
CSCD
北大核心
2011年第11期1366-1369,共4页
Acta Pharmaceutica Sinica
基金
教育部科学技术研究重点项目(208051)
江苏省"青蓝工程"科技创新团队支持计划
关键词
瑞香素
肠壁
代谢产物
daphnetin
intestinal wall
metabolite
