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目的 :观察了潘生丁对KB细胞株多药耐药的逆转作用并对其作用机制进行探讨。方法 :使用MTT法检测比较KB母细胞和耐药细胞株对长春新碱 (VCR)的药物敏感度并观察潘生丁对耐药的逆转程度 ;用3H标记的VCR检测细胞内药物浓度的变化。结果 :潘生丁作用下 ,KB母细胞和耐药细胞株的药物敏感度均有增高并呈剂量相关关系 ,有MRP表达的耐药细胞株对VCR的敏感度比母细胞株高 17倍。母细胞株和耐药细胞株细胞内的药物蓄积均有明显增加。结论 :潘生丁能通过增加细胞内的VCR蓄积 ,显著提高KB细胞对药物的敏感度 ;耐药细胞株与母细胞株相比 ,有较大程度的逆转 ,可能与MRP的表达有关 ,有待进一步探讨
Objective: To observe the reversal effect of dipyridamole on multidrug resistance in KB cell line and its mechanism of action. Methods: MTT assay was used to compare drug susceptibility of vincristine (VCR) to KB cells and drug resistant cell lines and the extent of reversal of dipyridamole resistance was observed. The change of intracellular drug concentration was detected by 3H labeled VCR. Results: Under the action of dipyridamole, the drug sensitivity of KB cells and drug-resistant cell lines were increased and dose-dependent. The MRP-expressing drug-resistant cell lines were 17 times more sensitive to VCR than the parental cell lines. There was a significant increase in the accumulation of drugs in the cell lines of both parental and drug resistant cell lines. CONCLUSION: Dipyridamole can increase the sensitivity of KB cells to drugs by increasing the accumulation of intracellular VCR. Compared with the parental cell lines, dipyridamole has a greater degree of reversal, which may be related to the expression of MRP, which needs to be further explored