E. Chieli et al., ASSESSMENT OF P-GLYCOPROTEIN-DEPENDENT DRUG TRANSPORT IN ISOLATED RATHEPATOCYTES USING RHODAMINE-123, Cell biology and toxicology, 9(3), 1993, pp. 235-241
To test the activity of P-170 glycoprotein in isolated hepatocytes, a
method has been developed employing the fluorescent dye rhodamine 123
(R-123). The uptake of R-123 by both freshly isolated and 4-hr-plated
hepatocytes depends on dye concentration, time of incubation, and cell
number. The efflux of R-123 from cells is inhibited by sodium azide a
nd by verapamil. In standard conditions the efficiency of efflux of R-
123 from cells correlates with the relative amount of immunoblottable
glycoprotein. The method has been applied to detection of P-170 activi
ty in hepatocytes from animals of different ages as well as from carci
nogen-treated animals. The proposed assay appears a simple and adequat
e tool for the functional assessment of multidrug transporter in liver
.