目的：研究蛇葡萄素与阿霉素合用对人白血病多药耐药细胞株K562/ADR增殖的抑制作用及其机制。方法：MTT法测定蛇葡萄素与阿霉素合用对K562/ADR细胞的细胞毒作用，应用金正均公式进行联合用药效果分析；藻红蛋白标记抗体检测蛇葡萄素对K562/ADR细胞膜表面P 糖蛋白表达的影响；流式细胞术测定蛇葡萄素对K562/ADR细胞内阿霉素累积的影响。结果：125～5 mg·L-1的蛇葡萄素能够明显逆转K562/ADR细胞对阿霉素的耐药性。125 mg·L-1蛇葡萄素与低浓度阿霉素合用可表现出拮抗效应，而浓度在25 mg·L-1以上的蛇葡萄素与阿霉素合用可表现出相加至协同效应。蛇葡萄素能够浓度依赖性减少K562/ADR细胞膜P 糖蛋白表达，增加细胞内阿霉素的浓度。结论：蛇葡萄素能通过抑制P 糖蛋白外排药物，促进抗癌药物在细胞内的累积，增强抗癌药物对耐药细胞的细胞毒作用，逆转肿瘤多药耐药。
Objective: To investigate the inhibitory effect of ampelopsin (AMP) combined with adriamycin (ADR) on growth of human leukemia multidrug resistant cell line K562/ADR. Method: MTT assay was used to detect the effect of AMP on the cytotoxicity of ADR. Jin‘s formula was used to analyze the effect of combined drug therapy. The expression of P glycoprotein (P gp) on cell membrane of K562/ADR was detected using PE labeled antibody. Flow cytometry was used to determine the influence of AMP on the intracellular accumulation of ADR. Result: AMP at the concentration of 125 to 5 mg·L-1 could significantly reverse the multidrug resistance (MDR) to ADR in K562/ADR cells. Co administration of 125 mg·L-1 AMP and low concentrations of ADR showed an antagonistic effect, while there was an additional to synergistic effect when the concentration of AMP was above 25 mg·L-1. AMP could decrease the expression of P gp in a concentration dependent manner and increase the intracellular accumulation of ADR in K562/ADR cells. Conclusion: AMP could increased the cytotoxicity and the intracellular accumulation of chemotherapeutic drugs in MDR associated tumor cells through inhibiting the efflux of drugs by P gp. AMP may be a promising MDR modulator.