目的 研究柚皮素在大鼠体内的代谢途径，为柚皮素的进一步研究开发提供参考依据。方法 大鼠ig给予柚皮素，收集不同时间段胆汁、尿液、粪便和血浆，应用液相色谱-三重四级杆-线性离子阱串联质谱（LC-QTRAP-MS）寻找和解析柚皮素在大鼠体内各生物基质中的可能代谢产物。通过对柚皮素裂解规律的研究，解析柚皮素在大鼠体内的可能代谢途径。结果 在ig给予柚皮素后大鼠的胆汁、尿、粪和血浆中共检测出14个可能的代谢产物，其主要代谢途径包括氧化、甲基化以及葡糖醛酸化和硫酸化。结论 柚皮素在大鼠体内经历了广泛的Ⅰ相和Ⅱ相代谢，代谢产物以Ⅱ相的葡萄糖醛酸和硫酸结合型代谢产物为主，通过尿排泄的代谢产物与原型相当，胆汁中以结合型代谢产物为主，在粪便中转化为原型排泄。

Objective To study the in vivo metabolic pathway of naringenin in rats, which would provide reference for its further research and development. Methods A liquid chromatography with hybrid quadruple-linear ion trap mass spectrometer (LC-QTRAP-MS) was applied to identify the metabolites of naringenin in bile, urine, feces and plasma after ig administration to rats. The fragmentation patterns of naringenin were also used to analyze possible metabolic pathways in the study. Results There were altogether 14 metabolites detected. The possible metabolic pathways of naringenin were oxidation, methylation, glucuronidation and sulfation in rats. Conclusion In vivo metabolism studies show that naringenin undergoes extensive metabolism, including phase Ⅰ and phase Ⅱ biotransformation, and the phase Ⅱ glucuronide and sulfate conjugates are primary metabolites. The relative quantitative amounts of metabolites excreted from urine are almost equivalent to that of the parent naringenin, while a large majority of metabolites are conjugated ones in bile, which are subsequently transformed to the parent in intestinal tract and appeared in feces.

国家自然科学基金重点项目（81430096，81302870）；国家科技重大专项（2012ZX09506001-006）；中国医学科学院医学与健康科技创新工程协和创新团队（2016-I2M-3-022）