The sulphonylurea glibenclamide inhibits multidrug resistance protein(MRP1)activity in human lung cancer cells

摘要

Glibenclamide, a sulphonylurea widely used for the treatment of non-insulin-dependent diabetes mellitus, has been shown to inhibit the activities of various ATP-binding cassette(ABC) transporters. In the present study, its effects towards multidrug resistance protein 1(MRP1), an ABC efflux pump conferring multidrug resistance and handling organic anions, were investigated. Intracellular accumulation of calcein, an anionic dye substrate for MRP1, was strongly increased By glibenclamide in a dose-dependent manner in MRP1-overexpressing lung tumour GLC4/Sb30 Cells through inhibition of MRP1-related calcein efflux.