Abstract
BackgroundThe 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.MethodsWe 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.ResultsThe 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.ConclusionsThe 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.
Highlights
The in vitro activity against Leishmania spp. of a novel group of compounds, phenalenone derivatives, is described in this study
Mitochondrial effects We observed that incubation with phenalenone F134 induced a highly significant decrease of the ATP level of L. amazonensis promastigotes (F(6, 20) = 10.504, P = 0.002)
In the present study we examined the mitochondrial membrane potential alterations in L. donovani, and the results showed that the membrane potential decreased when incubated with the IC90 of the phenalenones F20 and F40 (Fig. 3) (F(6, 20) = 15.083, P < 0.001 and F(6, 20) = 15.083, P = 0.008, respectively)
Summary
The in vitro activity against Leishmania spp. of a novel group of compounds, phenalenone derivatives, is described in this study. According to the World Health Organization (WHO), leishmaniasis is one of the seven most important tropical diseases and it represents a serious world health problem that presents a broad spectrum of clinical manifestations with a potentially fatal outcome [2, 3]. It is found in all Pentavalent antimony-based medicines for leishmaniasis have been in clinical practice from 1947 [5] but they cause side effects. In the absence of an effective vaccine, there is an urgent need for new and more
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