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Type: Artigo de periódico
Title: Anti-African trypanocidal and antimalarial activity of natural flavonoids, dibenzoylmethanes and synthetic analogues
Author: dos Santos, DAP
Braga, PAD
da Silva, MFDF
Fernandes, JB
Vieira, PC
Magalhaes, AF
Magalhaes, EG
Marsaioli, AJ
Moraes, VRD
Rattray, L
Croft, SL
Abstract: Objectives The known anti-protozoal activity of flavonoids has stimulated the testing of other derivatives from natural and synthetic sources. Methods As part. of our efforts to find potential lead compounds, a number of flavonoids isolated from Neoraputia paraensis, N. magnifica, Murraya paniculata, (Rutaceae), Lonchocarpus montanus, L. latifolius, L. subglaucescens, L. atropurpureus, L. campestris, Deguelia hatschbachii (Leguminosae), dibenzoylmethanes front L. subglaucescens and synthetic analogues were tested for in-vitro activity against chloroquine-sensitive Plasmodium falciparum and Trypanosoma brucei rhodesiense bloodstream form trypomastigotes. An assay with KB cells has been developed in order to compare in-vitro cytotoxicity of flavonoids with a selective action on the parasites. Key findings Thirteen of the compounds tested had IC50 values ranging from 4.6 to 9.9 mu M against T brucei rhodesiense. In contrast, a small number of compounds showed significant activity against P. falciparum; seven of those tested had IC50 values ranging From. 2.7 to 9.5 mu M. Among the flavones only one had IC50 < 10 mu m (7.6 mu m), whereas against T. brucei rhodesiense seven had IC50 < 10 mu m. Synthetic dibenzoylmethanes were the! most active in terms of number (Five) of compounds and the IC50 values (2.7-9.5 mu M) against P. falciparum. Conclusions Dibenzoylmethanes represent a novel class of compounds tested for the first time as antimalarial and trypanocidal agents.
Subject: antimalarial
trypanocidal agent
Country: EUA
Editor: Wiley-blackwell
Rights: fechado
Identifier DOI: 10.1211/jpp/61.02.0017
Date Issue: 2009
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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