[Studies on the mechanism of antifungal action of ciclopiroxolamine/Inhibition of transmembrane transport of amino acid, K+ and phosphate in Candida albicans cells (author's transl)].
6-Cyclohexyl-1-hydroxy-4-methyl-2(1H)-pyridone, 2-aminoethanol salt (ciclopiroxolamine, Cic, Hoe 296, Batrafen) was fungicidal to growing cultures of Candida albicans, although this effect was apparent after a certain period of cell proliferation, depending upon the drug concentration. Glucose-dependent uptake of all the amino acids tested, K+ and phosphate in starved C. albicans cells was significantly but to a considerably varying extent inhibited by the drug at levels around MIC. Accumulation of amino acid in the cellular pool was more profoundly inhibited than over-all amino acid incorporation into proteins. Cic did not affect the permeability barriers of C. albicans protoplasts or lecithin liposomes. It is presumed from these results that Cic-mediated growth inhibition or death of fungal cells is primarily caused by intracellular depletion of some essential substrates and/or ions, and that such effects are brought about through blockage of their uptake from the medium.
D000596:Amino Acids / Q000378:metabolism*; D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects / Q000378:metabolism*; D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D000077768:Ciclopirox; D008081:Liposomes / Q000378:metabolism; D010710:Phosphates / Q000378:metabolism*; D011188:Potassium / Q000378:metabolism*; D011728:Pyridones / Q000494:pharmacology*; D013997:Time Factors
D000596:Amino Acids; D000935:Antifungal Agents; D008081:Liposomes; D010710:Phosphates; D011728:Pyridones; D000077768:Ciclopirox; D011188:Potassium
Studien zum Mechanismus der antimyzetischen Wirkung von Ciclopiroxolamin. Hemmung des Transports von Aminosäuren, K+ und Phosphaten durch die Zellmembran von Candida albicans.