Antiplasmodial activity of acetogenins and inhibitory effect on Plasmodium falciparum adenylate translocase

J Chemother. 2004 Aug;16(4):350-6. doi: 10.1179/joc.2004.16.4.350.

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.

Publication types

  • Comparative Study

MeSH terms

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

Substances

  • Acetogenins
  • Aminoquinolines
  • Antimalarials
  • Fatty Alcohols
  • Lactones
  • Plant Extracts
  • Mitochondrial ADP, ATP Translocases
  • Electron Transport Complex I