Deglycosylation Process of Ginsenosides does not Affect the Toxicity of Irinotecan

Herb-drug interaction between ginseng and irinotecan was investigated in the present study through determining the inhibition potential of ginsenosides towards the glucuronidation of SN-38 which has been widely accepted as the active metabolite to induce the toxicity. Human liver microsomes (HLMs)-catalyzed SN-38 incubation system was used. The results showed that ginsenosides Rg(3) and Rh-2 exhibited competitive inhibition towards the glucuronidation of SN-38. The similar IC50 values were found for the inhibition of ginsenosides Rg(3) and Rh-2 towards the glucuronidation of SN-38, indicating no effects of deglycosylation process of ginsenosides Rg(3) towards the inhibition capability towards SN-38 glucuronidation. In conclusion, the competitive inhibition of ginsenosides Rg(3) and Rh-2 towards SN-38 glucuronidation was demonstrated in the present study, indicating the potential herb-drug interaction between ginseng and irinotecan. Additionaly, the deglycosylation of Rg(3) to form Rh-2 did not alter the inhibition potential towards SN-38 glucuronidation.