A highly sensitive and specific LC-MS/MS method was developed to investigate the in vivo bio-transformation of oleuropein in rat. Rat feces and urine samples collected after oral administration were determined by liquid chromatography coupled to tandem mass spectrometry with electrospray ionization in the negative-ion mode. The assay procedure involves a simple liquid-liquid extraction of parent oleuropein and the metabolite from rat feces and urine with ethyl acetate. Chromatographic separation was operated with 0.1% formic acid aqueous and methanol in gradient program at a flow rate of 0.50 mL/min on an RP-C18 column with a total run time of 31 min. This method was successfully applied to simultaneous determination of oleuropein and its metabolites in rat feces and urine. De-glucosylation, hydrolysis, oxygenation and methylation were found to comprise the major metabolic pathway of oleuropein in rat gastrointestinal tract and three metabolites were absorbed into the blood circulatory system within 24 h after oral administration.
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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