Universidade Estadual Paulista (UNESP), Faculdade de Ciências Farmacêuticas, Araraquara, Departamento de Alimentos e Nutrição, Rodovia Araraquara-Jau, km 1, Araraquara, SP 14802-901, Brazil.
U.S. Horticultural Research Laboratory, Agricultural Research Service, USDA, 2001 South Rock Road, Port Fierce, Florida 34945, United States.
J Agric Food Chem. 2021 Feb 17;69(6):1796-1805. doi: 10.1021/acs.jafc.0c04553. Epub 2021 Feb 3.
Eriocitrin plays a role in the reduction of oxidative stress and inflammation linked to the development of diabetes and atherosclerosis. We investigated the pharmacokinetics and distribution of eriocitrin metabolites in rats orally administered with eriocitrin. Plasma, urine, and organs were collected at 12 different time points from 0 to 24 h and analyzed by HPLC-PDA-MS. For the first time, the metabolism and distribution of orally administered eriocitrin were shown. Nine metabolites of eriocitrin were identified in rat urine, and seven in various tissues (eriodictyol, homoeriodictyol, hesperetin, and glucuronidated metabolites), and preliminary identifications of these metabolites are suggested. Overall, eriocitrin metabolites were widely distributed in the rat tissues, where homoeriodictyol and homoeriodictyol-7--glucuronide were the major metabolites. The half-lives of the metabolites in plasma were between 3 and 3.2 h, and the total bioavailability of eriocitrin was less than 1%.
橙皮苷元在降低与糖尿病和动脉粥样硬化发展相关的氧化应激和炎症方面发挥作用。我们研究了橙皮苷元在大鼠口服给药后的代谢物的药代动力学和分布。在 0 到 24 小时的 12 个不同时间点收集血浆、尿液和器官,并通过 HPLC-PDA-MS 进行分析。首次显示了口服给予的橙皮苷元的代谢和分布。在大鼠尿液中鉴定出 9 种橙皮苷元的代谢物,在各种组织中鉴定出 7 种(橙皮素、高圣草酚、桔皮素和葡萄糖醛酸化代谢物),并对这些代谢物进行了初步鉴定。总的来说,橙皮苷元代谢物在大鼠组织中广泛分布,其中高圣草酚和高圣草酚-7-O-葡萄糖醛酸苷是主要代谢物。代谢物在血浆中的半衰期在 3 到 3.2 小时之间,橙皮苷元的总生物利用度小于 1%。