Ginseng Disrupts the Metabolism of Cerebrovascular Treatment Drug Clopidogrel

Clopidogrel is a clinical drug used to treat cerebrovascular diseases, and ginsenosides are the active ingredients to show efficient therapeutic role towards cerebrovascular diseases. The present-study aims to determine potential drug-drug interaction between ginsenosides and clopidogrel. In vitro incubation mixture was used to investigate the inhibition of ginsenosides on the metabolism of clopidogrel catalyzed by human liver microsomes (HLMs). HLMs-catalyzed hydrolysis of 2-(2'-Benzoyl-3'-methoxyphenyl) benzothiazole (BMBT) was used to phenotype the activity of CES1; 100 mu M of ginsenosides were used to initially screen the inhibition on the hydrolysis of clopidogrel, and 15, 25.4, 50.4, 633, 43.2, and 71% activity of clopidogrel hydrolysis was inhibited. Given the most significant inhibition of ginsenoside Rg3 on the activity of clopidogrel hydrolysis, the inhibition of ginsenoside Rg3 on the activity of CES1 was furtherly investigated using BMBT as the probe substrate. Ginsenoside Rg3 significantly inhibited the activity of CES1. The present study broad our understanding of the inhibition of herbal components towards the activity of CES1. Additionally, CES1 inhibition-based ginsenosides-clopidogrel interaction was demonstrated.