Costa, Rafaella RodriguesSilva, João Augusto Oliveira daReis, Thiago Alves Rosa dosTavares, Grasiele de Sousa VieiraMendonça, Débora Vasconcelos CostaFreitas, Camila Simões deLage, Daniela PagliaraMartins, Vívian TamiettiAntinarelli, Luciana Maria RibeiroMachado, Amanda SanchezBandeira, Raquel SoaresRibeiro, Fernanda LudolfSantos, Thaís Teodoro de OliveiraBrito, Rory Cristiane Fortes deHumbert, Maria VictoriaSouza, Daniel MenezesDuarte, Mariana CostaChávez Fumagalli, Miguel AngelRoatt, Bruno MendesCoimbra, Elaine SoaresCoelho, Eduardo Antônio Ferraz2021-09-302021-09-302020COSTA, R. R. et al. Acarbose presents in vitro and in vivo antileishmanial activity against Leishmania infantum and is a promising therapeutic candidate against visceral leishmaniasis. Medical Microbiology and Immunology, v. 210, p. 133-147, abr. 2021. Disponível em: <https://link.springer.com/article/10.1007%2Fs00430-021-00707-4>. Acesso em: 10 jun. 2021.1432-1831http://www.repositorio.ufop.br/jspui/handle/123456789/13833Treatment against visceral leishmaniasis (VL) is mainly hampered by drug toxicity, long treatment regimens and/or high costs. Thus, the identifcation of novel and low-cost antileishmanial agents is urgent. Acarbose (ACA) is a specifc inhibitor of glucosidase-like proteins, which has been used for treating diabetes. In the present study, we show that this molecule also presents in vitro and in vivo specifc antileishmanial activity against Leishmania infantum. Results showed an in vitro direct action against L. infantum promastigotes and amastigotes, and low toxicity to mammalian cells. In addition, in vivo experiments performed using free ACA or incorporated in a Pluronic® F127-based polymeric micelle system called ACA/ Mic proved efective for the treatment of L. infantum-infected BALB/c mice. Treated animals presented signifcant reductions in the parasite load in their spleens, livers, bone marrows and draining lymph nodes when compared to the controls, as well as the development of antileishmanial Th1-type humoral and cellular responses based on high levels of IFN-γ, IL-12, TNF-α, GM-CSF, nitrite and IgG2a isotype antibodies. In addition, ACA or ACA-treated animals sufered from low organ toxicity. Treatment with ACA/Mic outperformed treatments using either Miltefosine or free ACA based on parasitological and immunological evaluations performed one and 15 days post-therapy. In conclusion, data suggest that the ACA/Mic is a potential therapeutic agent against L. infantum and merits further consideration for VL treatment.en-USrestritoTreatmentDrug repositioningMiltefosineAcarbose presents in vitro and in vivo antileishmanial activity against Leishmania infantum and is a promising therapeutic candidate against visceral leishmaniasis.Artigo publicado em periodicohttps://link.springer.com/article/10.1007%2Fs00430-021-00707-4https://doi.org/10.1007/s00430-021-00707-4