An effective diaryl derivative against Leishmania amazonensis and its influence on the parasite X macrophage interaction

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Abstract

The activity of several diarylheptanoid derivatives (curcuminoids) was previously evaluated against Leishmania amazonensis promastigotes and among them the most active compound was 5-hydroxy-7- (4-hydroxy-3-methoxyphenyl)-1-(4-methoxyphenyl)-1,4,6-heptatrien-3-one. This study was carried out to investigate the influence of this diaryl derivative on the infective promastigotes and Balb/c mice peritoneal macrophage interaction. The potential in vitro toxicity was also evaluated. Promastigotes pretreated for 24 hours with the compound had their infective capacity significantly decreased. When the infection of Balb/c macrophage by L.amazonensis promastigotes was already installed, addition of the drug resulted in a diminishing of the infection rate. It was demonstrated that the compound was not toxic to the host macrophage in a concentration equivalent to the LD50/24 h from the previous in vitro experiment. © 2004 Taylor & Francis Ltd.

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Alves, L. V., Cysne-Finkelstein, L., Temporal, R. M., Genestra, M. S., & Leon, L. L. (2004). An effective diaryl derivative against Leishmania amazonensis and its influence on the parasite X macrophage interaction. Journal of Enzyme Inhibition and Medicinal Chemistry, 19(5), 437–439. https://doi.org/10.1080/1475636042000198789

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