Abstract
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.
MeSH terms
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Acetogenins
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Aminoquinolines / chemistry
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Aminoquinolines / pharmacology*
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Animals
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Antimalarials / chemistry
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Antimalarials / pharmacology*
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Drug Resistance, Microbial
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Electron Transport Complex I / antagonists & inhibitors*
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Fatty Alcohols / pharmacology*
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Humans
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Lactones / pharmacology*
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Malaria, Falciparum / drug therapy
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Malaria, Falciparum / microbiology
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Microbial Sensitivity Tests
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Mitochondrial ADP, ATP Translocases / antagonists & inhibitors
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Mitochondrial ADP, ATP Translocases / metabolism
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Plant Extracts / pharmacology*
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Plasmodium falciparum / drug effects*
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Plasmodium falciparum / enzymology*
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Plasmodium falciparum / isolation & purification
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Sensitivity and Specificity
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Structure-Activity Relationship
Substances
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Acetogenins
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Aminoquinolines
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Antimalarials
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Fatty Alcohols
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Lactones
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Plant Extracts
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Mitochondrial ADP, ATP Translocases
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Electron Transport Complex I