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

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Autor(es): dc.creatorMenezes, Ana Paula de Jesus-
Autor(es): dc.creatorSilva, Milene Lopes da-
Autor(es): dc.creatorPereira, Wagner Luiz-
Autor(es): dc.creatorCosta, Guilherme de Paula-
Autor(es): dc.creatorHorta, Aline Luciano-
Autor(es): dc.creatorMendonça, Andréa Aparecida dos Santos-
Autor(es): dc.creatorCarneiro, Ana Cláudia Alvarenga-
Autor(es): dc.creatorSouza, Débora Maria Soares de-
Autor(es): dc.creatorNovaes, Rômulo Dias-
Autor(es): dc.creatorTeixeira, Róbson Ricardo-
Autor(es): dc.creatorSilva, André Talvani Pedrosa da-
Data de aceite: dc.date.accessioned2025-08-21T15:08:09Z-
Data de disponibilização: dc.date.available2025-08-21T15:08:09Z-
Data de envio: dc.date.issued2021-09-23-
Data de envio: dc.date.issued2021-09-23-
Data de envio: dc.date.issued2019-
Fonte completa do material: dc.identifierhttp://www.repositorio.ufop.br/jspui/handle/123456789/13792-
Fonte completa do material: dc.identifierhttps://doi.org/10.1016/j.jgar.2020.04.005-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/capes/1003168-
Descrição: dc.descriptionObjective: 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.-
Formato: dc.formatapplication/pdf-
Idioma: dc.languageen-
Direitos: dc.rightsaberto-
Direitos: dc.rightsThis 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.-
Palavras-chave: dc.subjectInflammation-
Palavras-chave: dc.subjectHeart damage-
Palavras-chave: dc.subjectBenznidazole-
Título: dc.titleIn vitro tripanocidal effect of 1,8-dioxooctahydroxanthenes (xanthenodiones) and tetraketones and improvement of cardiac parameters in vivo.-
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