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目的 研究红霉素 (ERY)对BEL 740 2细胞 (人肝癌细胞 )多药耐药性的逆转作用。方法 将BEL 740 2细胞连续培养在含阿霉素 (ADM )的培养液中诱导耐药细胞株BEL 740 2 /ADM ,用cell ELASA法检测细胞膜表面P gp的表达 ,细胞毒试验采用MTT法 ,用荧光分光光度法测定细胞内ADM浓度。结果 BEL 740 2 /ADM细胞表面P gp高度表达 ,除对ADM耐药外 ,对长春新碱 (VCR)和丝裂霉素(MMC)也有不同程度的交叉耐药 ;ERY可增强ADM、VCR、MMC对BEL 740 2 /ADM细胞的增殖抑制作用 ,可增加BEL 740 2 /ADM细胞内ADM的浓度而对细胞膜表面P gp的表达没有影响。结论 ERY通过竞争性地饱和BEL 740 2 /ADM细胞表面P gp通道 ,使细胞内药物外排减少、浓度增加 ,从而发挥对BEL 740 2 /ADM细胞多药耐药性的逆转作用
Objective To investigate the reversal effect of erythromycin (ERY) on the multidrug resistance of BEL 7402 cells (human hepatoma cells). Methods BEL 7402 cells were cultured in adriamycin (ADM) -containing medium to induce drug-resistant cell line BEL 740 2 / ADM. The expression of P gp on the surface of cell membrane was detected by cell ELASA. The cytotoxicity assay was performed by MTT method. Intracellular ADM concentration was determined by fluorescence spectrophotometry. RESULTS: The expression of P gp was highly expressed on BEL 740 2 / ADM cells. In addition to its resistance to ADM, VEL and MMC also showed different degrees of resistance to cross-resistance. ERY enhanced ADM, VCR, The inhibitory effect of MMC on the proliferation of BEL 7402 / ADM cells increased the concentration of ADM in BEL 7402 / ADM cells but had no effect on the expression of P gp on the cell membrane. Conclusion ERY can reverse the multidrug resistance of BEL 740 2 / ADM cells by competitively saturating the P gp channel on the surface of BEL 740 2 / ADM cells.