Correlation of the efficiency of fatty acid derivatives in suppressing Plasmodium falciparum growth in culture with their inhibitory effect on acyl-CoA synthetase activity.
The intraerythrocytic malaria parasite depends on the surrounding medium for a supply of phospholipid precursors. Efficient inhibition (IC50 7-90 microM) of Plasmodium falciparum growth in vitro was achieved using modified fatty acids. The fatty acid analogues most effective in suppressing P. falciparum growth in culture were also the most active inhibitors of acyl-CoA synthetase from the monkey parasite P. knowlesi.
Beaumelle
B D
BD
UA 530 CNRS, INSERM U 58, Montpellier, France.
Vial
H J
HJ
D000818:Animals; D002478:Cells, Cultured; D003066:Coenzyme A Ligases / Q000037:antagonists & inhibitors*; D003497:Cyclic N-Oxides / Q000494:pharmacology; D004912:Erythrocytes / Q000469:parasitology; D005227:Fatty Acids / Q000494:pharmacology*; D006801:Humans; D010168:Palmitates / Q000494:pharmacology; D010169:Palmitic Acids / Q000494:pharmacology*; D010961:Plasmodium / Q000201:enzymology*; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development*; D012277:Ricinoleic Acids / Q000494:pharmacology
D003497:Cyclic N-Oxides; D005227:Fatty Acids; D010168:Palmitates; D010169:Palmitic Acids; D012277:Ricinoleic Acids; C022776:2-bromopalmitate; C005072:5-doxylstearic acid; C032363:16-nitroxystearic acid; C024707:2-hydroxyhexadecanoic acid; D003066:Coenzyme A Ligases; C030521:ricinoleic acid