离体人肠道菌群对柚皮苷的代谢动力学分析

目的:研究人肠道菌群对柚皮苷的代谢程度与速度,为该成分的新药开发提供参考。方法:采集健康志愿者新鲜粪便制备肠道菌群混悬液,与柚皮苷在厌氧环境下孵育,运用HPLC监测柚皮苷浓度变化,HPLC-MS鉴定代谢产物结构。柚皮苷HPLC色谱条件为检测波长288 nm,流动相甲醇-0.1%磷酸溶液梯度洗脱。结果:柚皮苷与人肠道菌群共同孵育15 min后,柚皮苷色谱峰后面可见1个代谢产物;孵育至120 min时,柚皮苷代谢率100%。经HPLC-MS鉴定代谢产物为柚皮素。柚皮苷代谢过程符合非线性动力学过程。HPLC监测发现柚皮素可被进一步代谢,导致柚皮素峰面积降低。结论:柚皮苷可被人肠道菌群代谢,代谢速度快,代谢产物主要为柚皮素,可能存在柚皮苷的二级代谢产物。

In Vitro Metabolism of Naringin by Human Intestinal Microflora

Objective: To investigate metabolites and metabolic dynamics of naringin by human intestinal microflora. Method: Human intestinal microflora were obtain from human feces,and incubated with naringin under anaerobic environment.HPLC was applied to monitor the concentration of naringin with mobile phase of methanol-0.1% phosphoric acid solution for gradient elution and detection wavelength at 250 nm.Metabolites were analysis by HPLC-MS. Result: Naringenin,one metabolite of naringin,was detected after incubation for 15 min,which was identified by HPLC-MS and its retention time was about 23 min in HPLC.Metabolism percentage of naringin was reached 100% after incubation for 120 min.Metabolic dynamics of naringin by human intestinal microflora was fitted with nonlinear kinetics.Naringenin could be converting to its metabolite through HPLC monitor. Conclusion: Naringin can be quickly metabolism by human intestinal microflora,its main metabolite is naringenin,secondary metabolites of naringin may be existed.