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- W2379776476 abstract "Objective Previously,we had shown that sildenafil and vardenafil could reverse P-gp-mediated multidrug resistance(MDR) in vitro.This study was designed to determine whether PDE5 inhibitors have the potential to reverse MRP7-mediated chemotherapeutic drug resistance.Methods The MTT assay was used to access cytotoxicity.The intracellular accumulation of -paclitaxel was measured in liquid scintillation analyzer.Western blotting was used to determine the MRP7 protein expression.Results Sildenafil,vardenafil and tadalafil at 5 μmol/L significantly increased the sensitivity of HEK-MRP7 cells to paclitaxel by 9.8-,10.7-and 1.8-fold,respectively.Consistent with the cytotoxicity results,the drug accumulation data indicated sildenafil,vardenafil and tadalafil at 5 μmol/L significantly enhanced the intracellular accumulation of -paclitaxel in HEK-MRP7 cells by 3.0-,3.3-and 1.8-fold,respectively.The reversal efficacy of tadalafil was weaker than that of sildenafil and vardenafil.Western blot analysis indicated that sildenafil and vardenafil did not alter the expression of MRP7.Conclusion Sildenafil and vardenafil significantly enhanced the cytotoxicity of paclitaxel to HEK-MRP7 cells through inhibition of the drug efflux function of MRP7 rather than alteration of the expression of MRP7." @default.
- W2379776476 created "2016-06-24" @default.
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- W2379776476 date "2012-01-01" @default.
- W2379776476 modified "2023-09-25" @default.
- W2379776476 title "Sildenafil and vardenafil reverse MRP7-mediated drug resistance to paclitaxel" @default.
- W2379776476 hasPublicationYear "2012" @default.
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