In vitro activity of 1H-phenalen-1-one derivatives against Leishmania spp. and evidence of programmed cell death

1H-phenalen-1-one 衍生物对利什曼原虫的体外活性和程序性细胞死亡的证据

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作者:Atteneri López-Arencibia, María Reyes-Batlle, Mónica B Freijo, Ines Sifaoui, Carlos J Bethencourt-Estrella, Aitor Rizo-Liendo, Olfa Chiboub, Grant McNaughton-Smith, Jacob Lorenzo-Morales, Teresa Abad-Grillo, José E Piñero

Background

The in vitro activity against Leishmania spp. of a novel group of compounds, phenalenone derivatives, is described in this study. Previous studies have shown that some phenalenones present leishmanicidal activity, and induce a decrease in the mitochondrial membrane potential in L. amazonensis parasites, so in order to elucidate the evidence of programmed cell death occurring inside the promastigote stage, different assays were performed in two different species of Leishmania.

Conclusions

The present results highlight the potential use of phenalenone derivatives against Leishmania species and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

Methods

We focused on the determination of the programmed cell death evidence by detecting the characteristic features of the apoptosis-like process, such as phosphatidylserine exposure, mitochondrial membrane potential, and chromatin condensation among others.

Results

The results showed that four molecules activated the apoptosis-like process in the parasite. All the signals observed were indicative of the death process that the parasites were undergoing. Conclusions: The present results highlight the potential use of phenalenone derivatives against Leishmania species and further studies should be undertaken to establish them as novel leishmanicidal therapeutic agents.

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