LAUSR

HighlightsThe metabolic profile of corilagin in vivo and in vitro were investigated for the first time.Twenty‐four metabolites of corilagin in rat biological samples (urine, feces, plasma and tissues) were firstly reported.The phase II conjugate metabolites (except mono‐methylate conjugated metabolites) of pure Ellagitannin in vivo was firstly reported.The metabolic path ways of corilagin in rats were shown to involve hydrolysis, methylation, glycosylation, reduction, glucuronidation and sulfation.The reasons underlying poor circulating levels of corilagin were explained. Abstract Corilagin is an Ellagitannin with favorable pharmacological activities. But there was no report regarding the metabolism of corilagin in vitro or in vivo. In this study, the metabolic profile of corilagin in rats as well as in rat intestinal bacteria and liver microsomes incubation system in vitro were investigated comprehensively for the first time. Consequently, with the aid of sensitive HPLC‐Q‐TOF‐MS/MS, corilagin and its twenty‐four metabolites (fourteen phase II conjugate metabolites of corilagin, three hydrolyzed metabolites EA, GA, M3 and their seven derived metabolites) were absolutely or tentatively identified in rat biological samples (urine, feces, plasma and tissues) after oral administration of corilagin. In vitro, the three hydrolyzed metabolites were identified in rat intestinal microflora and liver microsomes. These results demonstrated that corilagin itself not only could underwent extensive phase II metabolism in rats, but also could underwent hydrolysis reaction in rats as well as in rat intestinal bacteria and liver microsomes in vitro. This study is first report to identify phase II conjugate metabolites (except mono‐methylate conjugated metabolites) of pure Ellagitannin and distribution of these metabolites in vivo. In addition, clear, detailed metabolic pathways of corilagin were shown to involve hydrolysis, methylation, glycosylation, reduction, glucuronidation and sulfation.