Journal of Antimicrobial Chemotherapy (1996) 37, 511-518
© 1996 The British Society for Antimicrobial Chemotherapy
research-article |
Activity of pyronaridine and mepacrine against twelve strains of Plasmodium falciparum in vitro
Department of Medical Parasitology, London School of Hygiene and Tropical Medicine London WC1E 7HT, UK
Received 7 June 1995; returned 2 August 1995; accepted 11 October 1995
*Corresponding author
Pyronaridine, an acndine derivative, has been found effective in China for the treatment of drug-resistant falciparum malaria. The activities of pyronaridine and mepacrine were compared with those of standard antimalarial drugs in vitro against chloroquine-sensitive (CS) and chloroquine-resistant (CR) Plasmodium falciparum isolates to investigate cross resistance. The 50% inhibitory concentrations (IC50) against the resistant isolates were 2.8-fold higher than the sensitive isolates for pyronaridine (CS = 7.3 nM; CR = 20.5 nM) and 3.2-fold higher for mepacrine (CS = 13.3 nM; CR = 42.6 nM). These same isolates showed an 11-fold difference in sensitivity to chloroquine with mean 1C50 values of 21 nM for sensitive and 239 nM for resistant parasites. A significant correlation was observed between parasite sensitivity (IC50) to pyronaridine and the drugs, mepacrine, amodiaquine and chloroquine. However, the high level of activity seen with pyronaridine, even against the CR isolates, should encourage further field trials with this drug.
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