Stage-dependent effects of analogs of gramicidin A on the growth of Plasmodium falciparum in vitro

Tryptophan-N-formylated gramicidin A, a nonhemolytic derivative of the toxic peptide antibiotic gramicidin A, has previously been shown to induce potassium leakage from Plasmodium falciparum-infected erythrocytes in vitro and to inhibit the growth of the parasite. In the present study the antimalari...

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Bibliographic Details
Published in:Parasitology research (1987) 1995, Vol.81 (1), p.26-31
Main Authors: OTTEN-KUIPERS, M. A, ROELOFSEN, B, OP DEN KAMP, J. A. F
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Biological and medical sciences
Cell Division - drug effects
Dose-Response Relationship, Drug
Erythrocytes - parasitology
Gramicidin - pharmacology
Medical sciences
Pharmacology. Drug treatments
Plasmodium falciparum - drug effects
Plasmodium falciparum - growth & development
Time Factors
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Summary:Tryptophan-N-formylated gramicidin A, a nonhemolytic derivative of the toxic peptide antibiotic gramicidin A, has previously been shown to induce potassium leakage from Plasmodium falciparum-infected erythrocytes in vitro and to inhibit the growth of the parasite. In the present study the antimalarial activities of two other nonhemolytic derivatives of gramicidin A, viz., acylated gramicidin A and desformylated gramicidin A, were tested and compared with those of gramicidin A and tryptophan-N-formylated gramicidin A. The 50% growth-inhibitory concentrations (IC50 values) of the four compounds varied from 0.3 to 18.3 nM, and complete growth inhibition was detected within one parasitic growth cycle. Using highly synchronized cultures of P. falciparum, it was furthermore shown that the gramicidin analogs are inhibitory to all developmental stages of the parasite, although their efficiency in accomplishing growth inhibition was found, as expected, to be clearly stage-dependent and to increase with the age of the parasite.
ISSN:0932-0113
1432-1955
DOI:10.1007/BF00932413