Antiplasmodial activity of acetogenins and inhibitory effect on Plasmodium falciparum adenylate translocase.
Three Annonaceous acetogenins exhibited in vitro antimalarial activities on a chloroquine-resistant Plasmodium falciparum strain, with IC50s ranging from 5 to 10 microM. Structure-activity relationships showed that maximal antimalarial activity occurred in the presence of at least one tetrahydrofuran moiety and a synergistic action with chloroquine was observed. These acetogenins partially inhibited the P. falciparum adenylate translocase.
Rakotomanga
M
M
USM 504 Laboratoire de biologie fonctionnelle des protozoaires, Museum National d' Histoire Naturelle, 75005 Paris, France.
Razakantoanina
V
V
Raynaud
S
S
Loiseau
P M
PM
Hocquemiller
R
R
Jaureguiberry
G
G
D054378:Acetogenins; D000634:Aminoquinolines / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D042967:Electron Transport Complex I / Q000037:antagonists & inhibitors*; D005233:Fatty Alcohols / Q000494:pharmacology*; D006801:Humans; D007783:Lactones / Q000494:pharmacology*; D016778:Malaria, Falciparum / Q000188:drug therapy / Q000382:microbiology; D008826:Microbial Sensitivity Tests; D000226:Mitochondrial ADP, ATP Translocases / Q000037:antagonists & inhibitors / Q000378:metabolism; D010936:Plant Extracts / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology* / Q000302:isolation & purification; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
D054378:Acetogenins; D000634:Aminoquinolines; D000962:Antimalarials; D005233:Fatty Alcohols; D007783:Lactones; D010936:Plant Extracts; D000226:Mitochondrial ADP, ATP Translocases; D042967:Electron Transport Complex I