Naslov
Pesticides and their binary combinations as p-glycoprotein inhibitors in nih 3t3/mdr1 cells

Autori
Pivčević, Branka ; Žaja, Roko

Izvornik
Environmental Toxicology and Pharmacology (1382-6689) 3 (2006); 268-276

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
multidrug resistance; P-glycoprotein; pesticides; binary combinations; NIH 3T3/MDR1; calcein acetoxymethyl ester

Sažetak
The purpose of the present study was to assess do selected pesticides as well as their binary combinations acts as inhibitors of P-glycoprotein (P-gp) activity of NIH 3T3 mouse fibroblasts stable transfected with human MDR1 gene (NIH 3T3/MDR1). As a result of P-gp inhibition the increase of intracellular accumulation of a model fluorescent P-gp substrate calcein acetoxymethyl ester was measured. Pesticide and verapamil individual dose-response data were scaled and expressed as percent of maximum effect. Results showed that from 14 pure pesticides tested endosulfan, phosalone and propiconazole were nearly potent as model inhibitor verapamil (EC50=1.5 &micro ; ; ; ; M), while diazinon showed a lower potency of inhibiting P-gp transport activity (EC50=58.4 &micro ; ; ; ; M). Concentrations of pesticides which produced the same inhibiting effect (isoboles) were combined binary. Results, calculated using the isobole method, revealed that diazinon in all combinations caused synergistic effect in inhibiting P-gp transport activity.

Izvorni jezik
Engleski

Znanstvena područja
Biologija

POVEZANOST RADA