Mendonça, Débora Vasconcelos CostaTavares, Grasiele de Sousa VieiraLage, Daniela PagliaraSoyer, Tauane GonçalvesCarvalho, Lívia MendesDias, Daniel SilvaRibeiro, Patrícia Aparecida FernandesOttoni, Flaviano MeloAntinarelli, Luciana Maria RibeiroVale, Danniele LucianaRibeiro, Fernanda LudolfDuarte, Mariana CostaCoimbra, Elaine SoaresChávez Fumagalli, Miguel AngelRoatt, Bruno MendesSouza, Daniel MenezesBarichello, José MarioAlves, Ricardo JoséCoelho, Eduardo Antônio Ferraz2019-04-032019-04-032019MENDONÇA, D. V. C. et al. In vivo antileishmanial efficacy of a naphthoquinone derivate incorporated into a Pluronic® F127-based polymeric micelle system against Leishmania amazonensis infection. Biomedicine & Pharmacotherapy, v. 109, p. 779-787, jan. 2019. Disponível em: <https://www.sciencedirect.com/science/article/pii/S0753332218367878>. Acesso em: 22 fev. 2019.07533322http://www.repositorio.ufop.br/handle/123456789/10927New therapeutic strategies against leishmaniasis are desirable, since the treatment against disease presents problems, such as the toxicity, high cost and/or parasite resistance. As consequence, new antileishmanial compounds are necessary to be identified, as presenting high activity against Leishmania parasites, but low toxicity in mammalian hosts. Flau-A is a naphthoquinone derivative recently showed to presents an in vitro effective action against Leishmania amazonensis and L. infantum species. In the present work, the in vivo efficacy of Flau-A, which was incorporated into a Poloxamer 407-based micelle system, was evaluated in a murine model against L. amazonensis infection. Amphotericin B (AmB) and Ambisome® were used as controls. The animals were infected and later treated with the compounds. Thirty days after the treatment, parasitological and immunological parameters were evaluated. Results showed that AmB, Ambisome® , Flau-A or Flau-A/M-treated animals presented significantly lower average lesion diameter and parasite burden in tissue and organs evaluated, when compared to the control (saline and micelle) groups. Flau-A or Flau-A/M-treated mice were those presenting the most significant reductions in the parasite burden, when compared to the others. These animals developed also a more polarized antileishmanial Th1 immune response, which was based on significantly higher levels of IFN-γ, IL-12, TNF-α, GM-CSF, and parasite-specific IgG2a isotype; associated with low levels of IL-4, IL10, and IgG1 antibody. The absence of toxicity was found in these animals, although mice receiving AmB have showed high levels of renal and hepatic damage markers. In conclusion, results suggested that the Flau-A/M compound may be considered as a possible therapeutic target to be evaluated against human leishmaniasis.en-USabertoChemotherapyAmphotericin BTegumentary leishmaniasisToxicityArtigo publicado em periodicoThis is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/BY-NC-ND/4.0/). Fonte: o próprio artigo.