Image-based in vitro screening reveals the trypanostatic activity of hydroxymethylnitrofurazone against trypanosoma cruzi

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorLondon School of Hygiene and Tropical Medicine-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorUnion of the Colleges of the Great Lakes (UNILAGO)-
Autor(es): dc.creatorScarim, Cauê Benito-
Autor(es): dc.creatorOlmo, Francisco-
Autor(es): dc.creatorFerreira, Elizabeth Igne-
Autor(es): dc.creatorChin, Chung Man-
Autor(es): dc.creatorKelly, John M.-
Autor(es): dc.creatorFortes Francisco, Amanda-
Data de aceite: dc.date.accessioned2025-08-21T18:01:48Z-
Data de disponibilização: dc.date.available2025-08-21T18:01:48Z-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2021-07-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/ijms22136930-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/231466-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/231466-
Descrição: dc.descriptionHydroxymethylnitrofurazone (NFOH) is a therapeutic candidate for Chagas disease (CD). It has negligible hepatotoxicity in a murine model compared to the front-line drug benznidazole (BZN). Here, using Trypanosoma cruzi strains that express bioluminescent and/or fluorescent reporter proteins, we further investigated the in vitro and in vivo activity of NFOH to define whether the compound is trypanocidal or trypanostatic. The in vitro activity was assessed by exploiting the fluorescent reporter strain using wash-out assays and real-time microscopy. For animal experi-mentation, BALB/c mice were inoculated with the bioluminescent reporter strain and assessed by highly sensitive in vivo and ex vivo imaging. Cyclophosphamide treatment was used to promote parasite relapse in the chronic stage of infection. Our data show that NFOH acts by a trypanostatic mechanism, and that it is more active than BZN in vitro against the infectious trypomastigote form of Trypanosoma cruzi. We also found that it is more effective at curing experimental infections in the chronic stage, compared with the acute stage, a feature that it shares with BZN. Therefore, given its reduced toxicity, enhanced anti-trypomastigote activity, and curative properties, NFOH can be considered as a potential therapeutic option for Chagas disease, perhaps in combination with other trypanocidal agents.-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences Sao Paulo State University (UNESP)-
Descrição: dc.descriptionDepartment of Infection Biology Faculty of Infectious and Tropical Diseases London School of Hygiene and Tropical Medicine, Keppel Street-
Descrição: dc.descriptionLAPEN—Laboratory of Design and Synthesis of Chemotherapeutic Agents Potentially Active on Neglected Diseases Department of Pharmacy School of Pharmaceutical Sciences University of Sao Paulo (USP)-
Descrição: dc.descriptionAdvanced Research Center in Medicine School of Medicine Union of the Colleges of the Great Lakes (UNILAGO)-
Descrição: dc.descriptionSchool of Pharmaceutical Sciences Sao Paulo State University (UNESP)-
Descrição: dc.descriptionFAPESP: 2016/10847-9-
Idioma: dc.languageen-
Relação: dc.relationInternational Journal of Molecular Sciences-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectBenznidazole-
Palavras-chave: dc.subjectBioluminescence imaging-
Palavras-chave: dc.subjectChagas disease-
Palavras-chave: dc.subjectHydroxymethylnitrofura-zone-
Palavras-chave: dc.subjectTrypanosoma cruzi-
Palavras-chave: dc.subjectTrypanostatic effect-
Título: dc.titleImage-based in vitro screening reveals the trypanostatic activity of hydroxymethylnitrofurazone against trypanosoma cruzi-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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