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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。
Objective: To study the metabolism and speed of naringin in human intestinal flora, and to provide a reference for the new drug development of this component. Methods: The fresh faeces of healthy volunteers were collected to prepare intestinal flora suspension. The suspension was incubated with naringin in anaerobic environment. The concentration of naringin was monitored by HPLC. The structure of metabolites was identified by HPLC-MS. Naringin HPLC chromatographic conditions for the detection wavelength of 288 nm, mobile phase methanol -0.1% phosphoric acid gradient elution. Results: Naringin incubated with human intestinal flora for 15 min showed one metabolite after the naringin peak. At 120 min, the naringin metabolic rate was 100%. The metabolites identified by HPLC-MS as naringenin. Naringin metabolic process in line with the nonlinear kinetic process. HPLC monitoring found that naringenin can be further metabolized, leading to reduced naringin peak area. CONCLUSION: Naringin can be metabolized by human intestinal flora, the metabolism speed is fast, the main metabolites are naringenin, and there may be secondary metabolites of naringin.