ISSN:
1432-1955
Source:
Springer Online Journal Archives 1860-2000
Topics:
Biology
,
Medicine
Notes:
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.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/PL00008549
