Rapid in vitro prescreen for chelators as potential trypanocides based on growth of Crithidia fasciculata.
A rapid in vitro prescreen for Fe-binding chelators has been developed with growth of Crithidia fasciculata and the sparing of its heme requirement in a defined medium as a test system. The prescreen functions as an index of chelator-mediated Fe transport and as an index of growth inhibition, presumably by the interference with Fe and/or heme metabolism at intracellular chelatable sites. Of 161 chelators examined, 84 were active heme-sparers; 32 of these inhibited growth at low chelator concentrations. Twenty-eight other chelators inhibited growth and another 49 were inactive. Such chelating activity directed at Fe and heme targets in hemoflagellates may provide leads for chemotherapy.
D000818:Animals; D002614:Chelating Agents / Q000145:classification / Q000494:pharmacology*; D055598:Chemical Phenomena; D002621:Chemistry; D003421:Crithidia / Q000187:drug effects / Q000254:growth & development; D004353:Drug Evaluation, Preclinical; D006418:Heme / Q000378:metabolism; D007501:Iron / Q000378:metabolism; D014344:Trypanocidal Agents / Q000494:pharmacology*
D002614:Chelating Agents; D014344:Trypanocidal Agents; D006418:Heme; D007501:Iron