LAUSR

Graphical abstract Figure. No Caption available. HighlightsPharmacokinetic study of quassinoid glycoside was performed for the first time.Bruceoside A could serve as the precursor of the potent anticancer brusatol in vivo, rather than its direct deglycosylated metabolite bruceosin.Quassinoid glycosides were proposed to be potential contributors to the anticancer properties of Fructus Bruceae. Abstract Bruceoside A, an abundant quassinoid glycoside in Fructus Bruceae, was chosen for the pharmacokinetic study. It is the first case report on the pharmacokinetic study of quassinoid glycosides so far. A sensitive, accurate, and repeatable UHPLC–MS/MS method was developed for the determination of bruceoside A and its major metabolite. The results showed bruceoside A could be transformed into the potent anticancer component brusatol in vivo, rather than its direct deglycosylated metabolite bruceosin. And the intestinal bacteria were proposed to take a potential role during such transformation. Based on the present study, it could be concluded that the quassinoid glycosides possessing weak activities in vitro could do contribution to the anticancer properties of Fructus Bruceae in vivo via transforming into more active metabolites.