In Vitro Investigations into the Potential Drug Interactions of Pseudoginsenoside DQ Mediated by Cytochrome P450 and Human Drug Transporters

体外研究伪人参皂苷 DQ 通过细胞色素 P450 和人体药物转运体介导的潜在药物相互作用

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作者:Zhuo Li, Cuizhu Wang, Jinping Liu, Pingya Li, Hao Feng

Abstract

Pseudoginsenoside DQ (PDQ), an ocotillol-type ginsenoside, is synthesized with protopanaxadiol through oxidative cyclization. PDQ exhibits good anti-arrhythmia activity. However, the inhibitory effect of PDQ on the cytochrome 450 (CYP450) enzymes and major drug transporters is still unclear. Inhibition of CYP450 and drug transporters may affect the efficacy of the drugs being used together with PDQ. These potential drug-drug interactions (DDIs) are essential for the clinical usage of drugs. In this study, we investigated the inhibitory effect of PDQ on seven CYP450 enzymes and seven drug transporters with in vitro models. PDQ has a significant inhibitory effect on CYP2C19 and P-glycoprotein (P-gp) with a half-inhibitory concentration (IC50) of 0.698 and 0.41 μM, respectively. The inhibition of CYP3A4 and breast cancer-resistant protein (BCRP) is less potent, with IC50 equal to 2.02-6.79 and 1.08 μM, respectively.

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