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Title: In vitro tripanocidal effect of 1,8-dioxooctahydroxanthenes (xanthenodiones) and tetraketones and improvement of cardiac parameters in vivo.
Authors: Menezes, Ana Paula de Jesus
Silva, Milene Lopes da
Pereira, Wagner Luiz
Costa, Guilherme de Paula
Horta, Aline Luciano
Mendonça, Andréa Aparecida dos Santos
Carneiro, Ana Cláudia Alvarenga
Souza, Débora Maria Soares de
Novaes, Rômulo Dias
Teixeira, Róbson Ricardo
Silva, André Talvani Pedrosa da
Keywords: Inflammation
Heart damage
Issue Date: 2020
Citation: MENEZES, 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: <>. Acesso em: 10 jun. 2021.
Abstract: Objective: 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.
ISSN: 2213-7165
metadata.dc.rights.license: This 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.
Appears in Collections:DECBI - Artigos publicados em periódicos

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