Effects of camptothecin, a topoisomerase I inhibitor, on Plasmodium falciparum

Currently, the treatment of falciparum malaria is seriously compromised by spreading drug resistance. We studied the effects of camptothecin, a potent and specific topoisomerase I inhibitor, on erythrocytic malaria parasites in vitro. In Plasmodium falciparum, camptothecin trapped protein-DNA comple...

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Bibliographic Details
Published in:Biochemical pharmacology 1998-03, Vol.55 (5), p.709-711
Main Authors: Bodley, Annette L., Cumming, Jared N., Shapiro, Theresa A.
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antiparasitic agents
Biological and medical sciences
camptothecin
Camptothecin - pharmacology
Enzyme Inhibitors - pharmacology
Erythrocytes - parasitology
malaria
Medical sciences
Pharmacology. Drug treatments
Plasmodium falciparum
Plasmodium falciparum - drug effects
Plasmodium falciparum - enzymology
topoisomerase
Topoisomerase I Inhibitors
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Summary:Currently, the treatment of falciparum malaria is seriously compromised by spreading drug resistance. We studied the effects of camptothecin, a potent and specific topoisomerase I inhibitor, on erythrocytic malaria parasites in vitro. In Plasmodium falciparum, camptothecin trapped protein-DNA complexes, inhibited nucleic acid biosynthesis, and was cytotoxic. These results provide proof for the concept that topoisomerase I is a vulnerable target for new antimalarial drug development.
ISSN:0006-2952
1873-2968
DOI:10.1016/S0006-2952(97)00556-X