LAUSR

Moscatilin, a bioactive ingredient isolated from Dendrobium moscatum, has been demonstrated to have excellent anti-cancer activity. The goals of the present study were to investigate the metabolic profiles of moscatilin and to identify and characterize its metabolites. In vitro studies were performed by incubating moscatilin (10 μM) with rat, dog, monkey and human liver microsomes (0.5 mg protein/mL) to generate the metabolites. An analytical method of liquid chromatography combined with hybrid quadrupole orbitrap high resolution mass spectrometry in full mass/data-dependent MS/MS scan was utilized to separate and identify the metabolites in accordance with their accurate masses, formulas and MS/MS fragment ions determination. A total of six phase I metabolites were detected and structurally characterized. The phase I metabolic pathways of moscatilin were hydroxylation, demethylation and dehydrogenation. In glutathione-supplemented liver microsomes, nine glutathione conjugates were detected and identified. Our results demonstrated that moscatilin was susceptible to bioactivation with the result of ortho quinone and quinone-methide intermediates. The present study provided an overview on the in vitro metabolic profiles of moscatilin, which will aid in the understanding of the efficacy and safety of this active compound. This article is protected by copyright. All rights reserved.