Abstract
Platonia insignis Mart., popularly known as “bacurizeiro,” is used in traditional medical practices based on its diverse biological properties. This study was aimed at evaluating the antileishmanial effects of the ethanol extract (EtOH-Ext), hexane fraction (Hex-F), and its main isolated Lupeol obtained from stem barks of P. insignis against Leishmania (Leishmania) amazonensis, as well as their cytotoxicity and possible mechanisms of action. The EtOH-Ext, Hex-F, and Lupeol inhibited the growth of L. amazonensis promastigote forms at IC50 of 174.24, 45.23, and 39.06 µg/mL, respectively, as well as L. amazonensis axenic amastigote forms at IC50 of 40.58, 35.87, and 44.10 µg/mL, respectively. The mean cytotoxic concentrations for macrophages (CC50) were higher than those for amastigotes (341.95, 71.65, and 144.0 µg/mL, resp.), indicating a selective cytotoxicity towards the parasite rather than the macrophages. Interestingly, all treatments promoted antileishmanial effect against macrophage-internalized amastigotes at concentrations lower than CC50. Furthermore, increases of lysosomal volume of macrophages treated with EtOH-Ext, Hex-F, and Lupeol were observed. On the other hand, only Lupeol stimulated increase of phagocytic capability of macrophages, suggesting this compound might be characterized as the biomarker for the antileishmanial effect of P. insignis stem bark, as well as the involvement of immunomodulatory mechanisms in this effect.
Highlights
Leishmaniasis are parasitic diseases caused by protozoa from Leishmania genus
According to the World Health Organization (WHO), approximately 556 million people were in areas at risk of contamination of visceral leishmaniasis and 399 million for cutaneous leishmaniasis in 2014 [2]
This work aimed to assess the potential antileishmanial activity, cytotoxicity, and immunomodulatory effect of ethanol extract (EtOH-Ext), its hexanic fraction (Hex-F), and the main constituent Lupeol obtained from the stem bark of P. insignis
Summary
Leishmaniasis are parasitic diseases caused by protozoa from Leishmania genus. Humans are infected by the sting of sand flies which live in forest areas, caves, or rodent dens. This pathology is widely distributed throughout the world and occurs in Asia, Europe, Africa, and the Americas. Leishmaniasis is capable of affecting both man and animals, affecting more than 12 million people worldwide, with 2 to 3 million of new cases each year [2, 3]. According to the World Health Organization (WHO), approximately 556 million people were in areas at risk of contamination of visceral leishmaniasis and 399 million for cutaneous leishmaniasis in 2014 [2]
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