Abstract

The goal of this study is to investigate the biotransformation of ginsenoside Rg1 in vivo. A highly sensitive and specific LC-MS/MS method was developed and used for metabolite identification in rat feces and urine after oral administration of ginsenoside Rg1 . Four metabolites of Rg1 were detected in rat feces and three metabolites of Rg1 were detected in rat urine. Deglycosylation and oxygenation were found to be the major metabolic pathways of ginsenoside Rg1 after oral administration in rat. Except for the reported metabolites Rh1 and protopanaxatriol, mono-oxygenated Rg1 and mono-oxygenated protopanaxatriol were detected for the first time after oral administration of Rg1. The in vivo metabolite profiling of ginsenoside Rg1 in rat was proposed. Viewed collectively, Rg1 was metabolized to mono-oxygenated Rg1, Rh1, protopanaxatriol and the secondary metabolite mono-oxygenated protopanaxatriol in rat.

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