目的 研究野木瓜果实总皂苷对人肝癌耐药细胞BEL-7402/5 FU多药耐药(MDR)的逆转作用,并初步探讨其耐药逆转机制.方法 采用MTT法测定5-氟尿嘧啶(5-FU)、阿霉素(ADM)、丝裂霉素(MMC)和野木瓜果实总皂苷对BEL-7402细胞、BEL-7402/5 FU细胞的毒性及野木瓜果实总皂苷逆转MDR的效果;利用蛋白质印迹法检测P-糖蛋白(P-gp)的表达情况.结果 BEL-7402/5 FU细胞对5-FU、ADM、MMC的耐药指数分别为21.71,2.73,2.11;野木瓜果实总皂苷能有效抑制BEL-7402/5 FU细胞增殖,无细胞毒性剂量为5,10 μg/mL,逆转耐药倍数分别为1.36、1.93;野木瓜果实总皂苷联合5-FU作用BEL-7402/5 FU细胞,可降低P-gp蛋白表达.结论 野木瓜果实总皂苷能部分逆转BEL-7402/5 FU细胞MDR,其机制可能是通过下调P-gp的表达而实现的.%Objective To investigate the reverse effect of total saponins from the fruit of Stauntonvine chinensis DC on the multidrug resistance (MDR) cell BEL-7402/5 FU, and explore the related mechanism.Methods The cells toxicant effect of 5-fluorouracil (5-FU), adriamycin (ADM), mitomycin (MMC) and total saponins from the fruit of Stauntonvine chinensis DC to BEL-7402 cells and BEL-7402/5 FU cells, and the reversal effect of total saponins from the fruit of Stauntonvine chinensis DC were evaluated by MTT assays.The expression of P-glycoprotein (P-gp) was detected by western blotting (WB).Results The resistance index of BEL-7402/5 FU cells to 5-FU, ADM, MMC were 21.71, 2.73 and 2.11 respectively.Total saponins from the fruit of Stauntonvine chinensis DC could significantly inhibit the proliferation of BEL-7402 and BEL-7402/5 FU cells.The available reversal concentration of total saponins from the fruit of Stauntonvine chinensis DC were 5 mg/mL and 10 mg/mL, and the reversal index were 1.36 and 1.93 respectively.After treated with total saponins from the fruit of Stauntonvine chinensis DC and 5-FU, the expression of P-gp was decreased.Conclusion The total saponins from the fruit of Stauntonvine chinensis DC could partly reverse the MDR of BEL-7402/5 FU cells, the reversal mechanisms may be due to down regulating the expression of P-gp.
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