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目的:研究大鼠口服芦丁后血浆、尿液、粪便和胆汁中的代谢产物。方法:按50 mg·kg~(-1)剂量对Wistar大鼠一次性灌胃芦丁,取不同时间点的血浆、尿液、粪便和胆汁,采用超高效液相色谱-四级杆-飞行时间串联质谱(UPLC-Q-TOF/MS)对各生物样品进行检测,分析样品中芦丁的代谢产物。流动相乙腈(A)-0.1%甲酸水溶液(B)梯度洗脱(0~10 min,5%~15%A;10~15 min,15%~60%A;15~18 min,60%~90%A;18~19 min,90%~5%A;19~22 min,5%A),流速0.4 m L·min~(-1),样品温度4℃;电喷雾离子源(ESI),负离子监测模式。结果:从大鼠血浆、尿液、粪便和胆汁中共鉴定出22个代谢产物,其中血浆中7个,尿液中19个,粪便中12个,胆汁中15个,代谢产物主要包括Ⅰ相的水解代谢产物和Ⅱ相的葡萄糖醛酸结合、硫酸结合及甲基化代谢产物。结论:芦丁在大鼠体内存在多种代谢途径,代谢产物主要包括去糖基化产物和苷元槲皮素进一步生物转化的代谢产物,为芦丁的体内代谢提供了重要信息。
OBJECTIVE: To study metabolites of plasma, urine, feces and bile in rats after oral administration of rutin. Methods: Routine administration of rutin at a dose of 50 mg · kg ~ (-1) for one time was carried out in Wistar rats. Plasma, urine, feces and bile were collected at different time points. The ultra high performance liquid chromatography - quadrupole - Time series tandem mass spectrometry (UPLC-Q-TOF / MS) for the detection of various biological samples, the sample of rutin metabolites. The mobile phase consisted of a gradient of acetonitrile (A) -0.1% aqueous solution of formic acid (B) (0-10 min, 5-15% A; 10-15 min, 15-60% A; 90% A; 18-19 min, 90% -5% A; 19-22 min, 5% A) at a flow rate of 0.4 m L · min -1 with a sample temperature of 4 ° C; electrospray ionization (ESI) , Negative ion monitoring mode. Results: A total of 22 metabolites were identified from plasma, urine, feces and bile in rats, including 7 in plasma, 19 in urine, 12 in feces and 15 in bile. The metabolites mainly consisted of phase Ⅰ Glucuronidation of hydrolyzed metabolites and phase II, sulfate binding and methylation metabolites. CONCLUSION: Rutin has a variety of metabolic pathways in rats. Metabolites mainly include the metabolites of deglycosylation products and quercetin biotransformation, which provide important information for the metabolism of rutin in vivo.