Cutaneous leishmaniasis is caused by spp., and its treatment is limited. The β-carbolines have shown activity against kinetoplastids. To evaluate the activity and effects of the β-carbolines, N-{2-[(4,6-bis(isopropylamino)-1,3,5-triazin-2-yl)amino]ethyl}-1-(4-methoxyphenyl)-β-carboline-3-carboxamide ( and N-benzyl-1-(4-methoxy)phenyl-9H-beta-carboline-3-carboxamide , against intracellular amastigotes and to suggest their mechanism of action. We analyzed the activity and cytotoxicity of β-carbolines and the morphological alterations by electron microscopy. Mitochondrial membrane potential, production nitric oxide, reactive oxygen species, lipidic bodies, autophagic vacuoles and ATP were also evaluated. The results showed that and are active against intracellular amastigotes and were able to induce oxidative stress and ultrastructural alterations such as accumulation of lipid bodies and autophagic vacuoles, leading to parasite death.
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http://dx.doi.org/10.2217/fmb-2020-0263 | DOI Listing |
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