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作者以抗阿霉素（ＡＤＭ）的人肺腺癌Ａ５４９亚细胞系Ａ５４９／Ｒ１和Ａ５４９／Ｒ２为模型，对异搏定（ＶＰＬ）的体外逆转抗药性效果及其作用机理进行了初步探索。发现ＶＰＬ浓度在１０μｇ／ｍｌ以下时无直接抑癌作用；以１０μｇ／ｍｌ剂量ＶＰＬ与ＡＤＭ联合，能使Ａ５４９／Ｒ２细胞内ＡＤＭ聚积量显著增加（Ｐ＜０．０５），并能使抗药细胞的抗药指数（ＲＦ）显著下降。结果表明，ＶＰＬ在体外能有效地逆转肿瘤细胞的抗药性，此作用与ＶＰＬ同Ｐ－糖蛋白竞争性结合，阻止药物外排有关，而与其钙通道阻断作用无关。
In this study, A549 / R1 and A549 / R2 cell lines A549 / R1 and A549 / R2 against human lung adenocarcinoma of adriamycin (ADM) were used as models to investigate the reversal drug resistance and mechanism of verapamil (VPL) in vitro. It was found that VPL concentration of 10μg / ml or less no direct tumor suppressor effect; 10μg / ml dose of VPL combined with ADM can A549 / R2 intracellular ADM accumulation increased significantly (P <0.05), and can make drug resistance Cell resistance index (RF) decreased significantly. The results showed that VPL can effectively reverse the drug resistance of tumor cells in vitro. This effect is related to the competitive binding of VPL with P-glycoprotein to prevent drug efflux but not to calcium channel blockade.