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目的 :探讨钙调蛋白的抑制剂三氟拉嗪是否具有逆转人肾癌的天然多药耐药性的作用。方法 :对经过病理证实的 36例肾透明细胞癌组织采用RT PCR方法检测mdr 1表达水平 ,高表达的为耐药组 ,无或低表达的为敏感组 ,给予阿霉素和三氟拉嗪处理 ,并采用MTT法评价细胞毒作用 ,流式细胞仪检测细胞内ADR浓度聚集。结果 :三氟拉嗪 (TFP)对肿瘤细胞无明显的细胞毒作用 ;但具有逆转肾癌对ADR的耐药 ,并且在耐药的肾癌中 ,效果更明显 (P <0 0 1)。同样三氟拉嗪(TFP)能增加化疗药物细胞内浓度 ,但未存在剂量 效应相关性 ,具有饱和性。结论 :三氟拉嗪能逆转人肾癌MDR ,可以作为肾癌化疗和辅助用药 ,其低毒副作用使其具有应用价值和可行性
Objective: To investigate whether calmodulin inhibitor trifluoperazine can reverse the natural multidrug resistance of human renal cell carcinoma. Methods: The expression of mdr 1 was detected by RT-PCR in 36 cases of renal clear cell carcinoma confirmed by pathology. The high expression of mdr 1 was the resistant group, the sensitive group without or low expression was treated with doxorubicin and trifluoperazine The MTT assay was used to evaluate the cytotoxicity and the concentration of ADR in the cells was detected by flow cytometry. Results: TFP had no obvious cytotoxic effect on tumor cells, but it could reverse the resistance of renal carcinoma to ADR and was more effective in resistant renal cell carcinoma (P <0.01). The same trifluoperazine (TFP) can increase the intracellular concentration of chemotherapy drugs, but there is no dose-response correlation, with saturation. CONCLUSION: Triflutrazine can reverse MDR of human renal cell carcinoma, which can be used as chemotherapy and adjuvant chemotherapy for renal cell carcinoma. Its low toxicity and side effects make it valuable and feasible