Effect of auranofin on absorptive processes in the rat small bowel.
Mucosal auranofin (AF) caused a concentration dependent inhibition of fluid, Na+, glycine and galactose transport by everted sacs of rat small intestine (IC50 = 2 X 10(-4) M). Inhibition of nutrient absorption was not due to reduced fluid uptake since a similar reduction in fluid uptake induced by a mucosal osmotic load failed to alter glycine transport. Inhibitory effects of AF were not observed when metabolism was reduced, suggesting that carrier mediated entry processes were unaltered. AF inhibited Na+, K+-ATPase activity in isolated enterocytes (IC50 = 2 X 10(-4) M), without affecting Mg2+-dependent ATPase activity. Our studies suggest that the actions of AF on small intestinal absorption may result from inhibition of the Na+ pump.
D000251:Adenosine Triphosphatases / Q000378:metabolism; D000818:Animals; D001310:Auranofin; D006051:Aurothioglucose / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000494:pharmacology; D001692:Biological Transport / Q000187:drug effects; D003967:Diarrhea / Q000139:chemically induced; D006046:Gold / Q000031:analogs & derivatives*; D007408:Intestinal Absorption / Q000187:drug effects; D007421:Intestine, Small / Q000201:enzymology / Q000378:metabolism*; D008297:Male; D051381:Rats
D006051:Aurothioglucose; D001310:Auranofin; D006046:Gold; D000251:Adenosine Triphosphatases