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目的:分析大鼠灌胃毛橘红醇提物后血浆中柚皮苷、柚皮素及其代谢产物。方法:健康雄性SD大鼠按50 g.kg-1剂量经口给予毛橘红醇提物,1.0 h后采集眼眶静脉血液制备血浆,采用UPLC-Q-TOF的MSE功能与M etabolynxTM软件联合的方法分析。结果:在大鼠血浆中检测到柚皮苷(M1)、柚皮素(M2)、柚皮苷5-O-葡萄糖醛酸苷(M3)、柚皮苷4′-O-葡萄糖醛酸苷(M4)、柚皮素葡萄糖醛酸苷(M5)、柚皮苷4′-O-硫酸酯(M6)、羟基化柚皮素甲醚(M7)、柚皮素葡萄糖醛酸基和硫酸酯基共价结合物(M8)、羟基化柚皮素葡萄糖醛酸苷(M9)。其中M3,M4,M6为首次报道的柚皮苷代谢物,M7,M9为首次报道的柚皮素代谢物。结论:柚皮苷、柚皮素在大鼠体内以葡萄糖醛酸化、硫酸化的形式被代谢,柚皮素还以氧甲基化、羟化葡萄糖醛酸化的形式被代谢。
OBJECTIVE: To analyze the contents of naringin, naringenin and their metabolites in rats after intragastric administration of the extract of Mao orange red. METHODS: Healthy male Sprague-Dawley rats were orally administered the extract of Mao orange red by 50 g.kg-1 dose, and the orbital venous blood was collected 1.0 h later. The plasma was prepared by MSE function of UPLC-Q-TOF and M etabolynx TM software analysis. Results: Naringin (M1), naringenin (M2), naringin 5-O-glucuronide (M3), naringin 4’-O-glucuronide (M4), naringenin glucuronide (M5), naringin 4’-O-sulfate (M6), hydroxylated naringenin (M7), naringenin glucuronic acid and sulfate Covalent conjugate (M8), hydroxylated naringenin glucuronide (M9). Among them, M3, M4 and M6 were the first reported naringin metabolites, and M7 and M9 were the first reported naringenin metabolites. CONCLUSION: Naringin and naringenin are metabolized by glucuronidation and sulfation in rats. Naringenin is also metabolized by oxymethylated and hydroxylated glucuronidation.