Simultaneous determination of imperatorin and its metabolites in vitro and in vivo by a GC-MS method: application to a bioavailability and protein binding ability study in rat plasma

Biomedical Chromatography : BMC
Gang ZhaoSicen Wang

Abstract

In this study, a simple and sensitive gas chromatography-mass spectrometry method was developed for the study of bioavailability and protein binding and the metabolism of imperatorin in rat. The results showed that the pharmacokinetics of imperatorin after intravenous and oral administration in rats exhibited linear characteristics. The absolute bioavailability of imperatorin was calculated as ~3.85, ~33.51 and ~34.76% for 6.25, 12.5 and 25 mg/kg, respectively. The low bioavailability of imperatorin may be attributed to the poor absorption or extensive metabolism. The phase I metabolites of imperatorin formed in vitro by rat liver microsomes were studied, and two metabolites were isolated and identified as xanthotoxol and heraclenin. Following oral administration of imperatorin, one metabolite (heraclenin) was detected in rat plasma, and two potential metabolites (xanthotoxol and heraclenin) were detected in rat urine. However, none of potential metabolites was detected in rat feces and bile. The results showed that the metabolites of imperatorin were excreted by kidney, and heraclenin was associated with an active component. Demethylation and oxygenization were the main metabolic pathways. In vitro plasma protein binding of im...Continue Reading

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Citations

Jan 19, 2016·Phytomedicine : International Journal of Phytotherapy and Phytopharmacology·Yi Mei ZhengWing Shing Ho
May 2, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Aneta GrabarskaAndrzej Stepulak
Sep 29, 2018·Food Science and Biotechnology·Wei-Hong LiangYuh-Chyang Charng
Dec 7, 2018·Journal of Asian Natural Products Research·Di WeiHuai-Zhen He

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