期刊
JOURNAL OF FUNCTIONAL FOODS
卷 40, 期 -, 页码 659-669出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.jff.2017.12.006
关键词
Herbacetin; Pharmacokinetics; Biotransformation; Glucuronidation; Hepatic metabolism; Colonic degradation
资金
- Program oh National Foundation of Natural Sciences of China [81573683]
The promising potential benefits of herbacetin in human entail its pharmacokinetic investigations, but the metabolic fate of this natural compound in vivo remains a field of unknown so far. The current study, for the first time, identified and quantified seven herbacetin-metabolites from rat urine, feces and bile after administration of herbacetin to rats. It was found that herbacetin was excreted primarily from rat urine in the form of glucuronide-conjugations. Subsequent in vitro enzyme kinetic studies and in vivo pharmacokinetic investigations suggested an extensive hepatic metabolism of herbacetin and the high exposure of herbacetin-glucuronides in systemic circulation. The clearance, t(1/2) and bioavailability of herbacetin in rats were determined as 16.4 +/- 1.92 ml.kg/min, 11.9 +/- 2.7 min, and 1.32%, respectively. On basis of these findings, a comprehensive metabolic pathway of herbacetin in rats was composed, which was crucial for the further assessments of herbacetin therapeutic effects and mechanism of pharmacological action.
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