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Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
pharmacology, toxicology and pharmaceutics
Cytotoxicity and DNA binding properties of the plant alkaloid burasaine
European Journal of Pharmaceutical Sciences, Volume 20, No. 4-5, Year 2003
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Description
Burasaine is a plant alkaloid isolated from the roots of several species of the Burasaia genus endemic to Madagascar. It exhibits in vitro antiplasmodial activities but the molecular basis of this biological activity is not known. The strong structural similarity with the alkaloid berberine prompted us to postulate that burasaine could interact with DNA. To test this hypothesis, we investigated the mode of binding of burasaine to DNA and tested its cytotoxic potential toward human HL-60 leukemia cells. Its inhibitory activity toward topoisomerases I and II was also studied. Absorption and melting temperature measurements attested that burasaine forms stable complexes with DNA. The results of electric linear dichroism (ELD) spectroscopy may be interpreted either by an intercalation or by an external stacking parallel to the base pairs. The affinity of burasaine for DNA is slightly lower than that of berberine and this translates at the cellular level by a reduced cytotoxicity. Burasaine does not promote DNA cleavage by human topoisomerases I or II and this likely accounts for its very weak cytotoxic potential and its very modest effects on the cell cycle progression observed at high concentrations. The study identifies DNA as a potential bioreceptor for burasaine and contributes to a better understanding of the mechanism of action of benzoquinolizine alkaloids. © 2003 Elsevier B.V. All rights reserved.
Authors & Co-Authors
Kluza, Jérome
France, Paris
Inserm
Baldeyrou, Brigitte
France, Paris
Inserm
Colson, Pierre
Belgium, Liege
Université de Liège
Rasoanaivo, Philippe
Madagascar, Antananarivo
Institut Malgache de Recherches Appliquees Antananarivo
Mambu, Lengo
France, Paris
Museum National D'histoire Naturelle
Frappier, François
France, Paris
Museum National D'histoire Naturelle
Bailly, Christian
France, Paris
Inserm
Statistics
Citations: 49
Authors: 7
Affiliations: 4
Identifiers
Doi:
10.1016/j.ejps.2003.08.007
ISSN:
09280987
Research Areas
Genetics And Genomics
Study Locations
Madagascar