体外研究细胞色素 P450 和人药物转运体介导的伪人参皂苷 DQ 的潜在药物相互作用。
In Vitro Investigations into the Potential Drug Interactions of Pseudoginsenoside DQ Mediated by Cytochrome P450 and Human Drug Transporters.
机构信息
School of Pharmaceutical Sciences, Jilin University, 126 Xinmin Street, Changchun 130021, China.
Department of Human Anatomy, College of Basic Medical Sciences, Jilin University, 126 Xinmin Street, Changchun 130021, China.
出版信息
Molecules. 2024 May 24;29(11):2482. doi: 10.3390/molecules29112482.
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 (IC) of 0.698 and 0.41 μM, respectively. The inhibition of CYP3A4 and breast cancer-resistant protein (BCRP) is less potent, with IC equal to 2.02-6.79 and 1.08 μM, respectively.
拟人参皂苷 DQ（PDQ）是一种通过氧化环化作用由原人参二醇合成的奥克梯隆型人参皂苷，具有良好的抗心律失常活性。然而，PDQ 对细胞色素 450（CYP450）酶和主要药物转运体的抑制作用尚不清楚。CYP450 和药物转运体的抑制可能会影响与 PDQ 同时使用的药物的疗效。这些潜在的药物相互作用（DDI）对于药物的临床应用至关重要。在这项研究中，我们使用体外模型研究了 PDQ 对七种 CYP450 酶和七种药物转运体的抑制作用。PDQ 对 CYP2C19 和 P 糖蛋白（P-gp）具有显著的抑制作用，半抑制浓度（IC）分别为 0.698 和 0.41 μM。对 CYP3A4 和乳腺癌耐药蛋白（BCRP）的抑制作用较弱，IC 值分别为 2.02-6.79 和 1.08 μM。
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