Abstract
Gossypol, a disesquiterpene extracted from cotton seeds, is known to inhibit strongly the Plasmodium falciparum lactate dehydrogenase, but its high toxicity has stopped any antimalarial drug development. A series of Schiff's bases was synthesized from gossypol by modification of the aldehyde groups responsible for its toxicity. A total of 13 compounds showing low cytotoxicity were then selected and were compared with gossypol for activity against 2 chloroquine-resistant strains of P. falciparum (PFB, FCB1). These in vitro activities were evaluated using an isotope-based drug-susceptibility semiautomated microdilution test followed by determination of IC50 values (50% inhibitory concentration). In all, 12 of the 13 compounds tested were active; 3 of them displayed antimalarial activity comparable with that of gossypol itself.
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Received: 27 November 1999 / Accepted: 28 January 2000
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Razakantoanina, V., Phung, N. & Jaureguiberry, G. Antimalarial activity of new gossypol derivatives. Parasitol Res 86, 665–668 (2000). https://doi.org/10.1007/PL00008549
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DOI: https://doi.org/10.1007/PL00008549