In vitro tripanocidal effect of 1,8-dioxooctahydroxanthenes (xanthenodiones) and tetraketones and improvement of cardiac parameters in vivo.

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dc.contributor.authorMenezes, Ana Paula de Jesus
dc.contributor.authorSilva, Milene Lopes da
dc.contributor.authorPereira, Wagner Luiz
dc.contributor.authorCosta, Guilherme de Paula
dc.contributor.authorHorta, Aline Luciano
dc.contributor.authorMendonça, Andréa Aparecida dos Santos
dc.contributor.authorCarneiro, Ana Cláudia Alvarenga
dc.contributor.authorSouza, Débora Maria Soares de
dc.contributor.authorNovaes, Rômulo Dias
dc.contributor.authorTeixeira, Róbson Ricardo
dc.contributor.authorSilva, André Talvani Pedrosa da
dc.date.accessioned2021-09-23T16:15:33Z
dc.date.available2021-09-23T16:15:33Z
dc.date.issued2020pt_BR
dc.description.abstractObjective: Trypanosoma cruzi infection affects millions of people worldwide, and the drugs available for its treatment have limited efficacy. 1,8-Dioxooctahydroxanthenes and tetraketones are compounds with important biological applications. The aim of this study was to assess the trypanocidal and inflammatory activities of nine 1,8-dioxooctahydroxanthenes (1–9) and three tetraketones (10–12). Methods and results: By in vitro killing assay, three compounds were able to eliminate CL TdTomato expressing strain of T. cruzi, 9 (IC50 = 30.65mM), 10 (IC50 = 14.11mM), and 11 (IC50 = 26.43mM). However, only 9 was not toxic to Vero cells. Next, to evaluate the in vivo antitrypanosomal and immunological efficacy of 9, Swiss mice were infected with the Y and CL strains of T. cruzi and treated for 10 days with 50 mg/kg of 9. This compound reduced the cardiac inflammatory infiltration in animals infected with both strains. Rank's ligand (RankL), CCL2, and interferon (IFN)-g were measured in the cardiac tissue homogenate of the Y-strain-infected animals, and no interference of 9 was observed. However, compound 9 increased the RankL and interleukin (IL)-10 levels in CL-infected mice. No hepatic and renal toxicity was observed. Conclusion: Our findings showed that 1,8-dioxooctahydroxanthene has antiparasitic effect and ameliorates the cardiac inflammatory parameters related to T. cruzi infection.pt_BR
dc.identifier.citationMENEZES, A. P. de J. et al. In vitro tripanocidal effect of 1,8-dioxooctahydroxanthenes (xanthenodiones) and tetraketones and improvement of cardiac parameters in vivo. Journal of Global Antimicrobial Resistance, v. 22, p. 466-476, 2020. Disponível em: <https://www.sciencedirect.com/science/article/pii/S2213716520300977>. Acesso em: 10 jun. 2021.pt_BR
dc.identifier.doihttps://doi.org/10.1016/j.jgar.2020.04.005pt_BR
dc.identifier.issn2213-7165
dc.identifier.urihttp://www.repositorio.ufop.br/jspui/handle/123456789/13792
dc.language.isoen_USpt_BR
dc.rightsabertopt_BR
dc.rights.licenseThis is an open access article under the CC BY-NC-ND license (http://creativecommons. org/licenses/by-nc-nd/4.0/). Fonte: o PDF do artigo.pt_BR
dc.subjectInflammationpt_BR
dc.subjectHeart damagept_BR
dc.subjectBenznidazolept_BR
dc.titleIn vitro tripanocidal effect of 1,8-dioxooctahydroxanthenes (xanthenodiones) and tetraketones and improvement of cardiac parameters in vivo.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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