Pharmacokinetic study on ginsenoside Rg3 and ginsenoside Rh2 in gut microbiota dysbiosis rats / 中草药

ABSTRACT

Objective: The aim of this study was to explore the pharmacokinetics of ginsenoside Rg3 and its deglycosylated metabolite, ginsenoside Rh2 in lincomycin-induced gut microbiota dysbiosis rats after ig administration of ginsenoside Rg3. Methods: An LC-MS/MS analytical method was developed and validated to detect ginsenoside Rg3 and Rh2 in plasma of rats. The method was validated by specificity, linearity, lower limits of quantification (LLOQ), precision, accuracy, matrix effect, recovery, and stability. Lincomycin (orally, 5 000 mg/kg, 7 d) was selected to induce gut microbiota dysbiosis. The fecal moisture contents and the β-D-glucosidase activity were also assessed in this study. And the plasma samples were collected and analyzed after ig administration of ginsenoside Rg3 (20 mg/kg). Results: The results indicated that this method could be used for the determination of the concentration of ginsenoside Rg3 and Rh2 in plasma of rats. The fecal moisture content in rats treated with lincomycin was significantly increased (P < 0.01) and the β-D-glucosidase activity was decreased (P < 0.01) compared with the control rats. The AUC0~∞ and Cmax in gut microbiota dysbiosis rats were increased, while the AUC0~t and Cmax of its active metabolite, ginsenoside Rh2 were significantly decreased (P < 0.01) compared with normal rats. Conclusion: The pharmacokinetic profile of ginsenoside Rg3 and Rh2 is changed in gut microbiota dysbiosis rats, which partly relates to the decreased β-D-glucosidase activity.