Leishmanicidal Activity of Guanidine Derivatives against Leishmania infantum

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorFederal University of Paraiba-
Autor(es): dc.contributorUniversidade Federal da Paraíba (UFPB)-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.creatorAlmeida, Fernanda Silva-
Autor(es): dc.creatorMoreira, Vitor Partite-
Autor(es): dc.creatorSilva, Edson dos Santos-
Autor(es): dc.creatorCardoso, Leonardo Lima-
Autor(es): dc.creatorde Sousa Palmeira, Pedro Henrique-
Autor(es): dc.creatorCavalcante-Silva, Luiz Henrique Agra-
Autor(es): dc.creatorAraújo, Demétrius A. M. de-
Autor(es): dc.creatorAmaral, Ian P. G. do-
Autor(es): dc.creatorGonzález, Eduardo René Pérez-
Autor(es): dc.creatorKeesen, Tatjana S. L.-
Data de aceite: dc.date.accessioned2025-08-21T18:03:52Z-
Data de disponibilização: dc.date.available2025-08-21T18:03:52Z-
Data de envio: dc.date.issued2023-07-29-
Data de envio: dc.date.issued2023-07-29-
Data de envio: dc.date.issued2023-03-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/tropicalmed8030141-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/249799-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/249799-
Descrição: dc.descriptionLeishmaniasis is a neglected tropical infectious disease with thousands of cases annually; it is of great concern to global health, particularly the most severe form, visceral leishmaniasis. Visceral leishmaniasis treatments are minimal and have severe adverse effects. As guanidine-bearing compounds have shown antimicrobial activity, we analyzed the cytotoxic effects of several guanidine-bearing compounds on Leishmania infantum in their promastigote and amastigote forms in vitro, their cytotoxicity in human cells, and their impact on reactive nitrogen species production. LQOFG-2, LQOFG-6, and LQOFG-7 had IC50 values of 12.7, 24.4, and 23.6 µM, respectively, in promastigotes. These compounds exhibited cytotoxicity in axenic amastigotes at 26.1, 21.1, and 18.6 µM, respectively. The compounds showed no apparent cytotoxicity in cells from healthy donors. To identify mechanisms of action, we evaluated cell death processes by annexin V and propidium iodide staining and nitrite production. Guanidine-containing compounds caused a significant percentage of death by apoptosis in amastigotes. Independent of L. infantum infection, LQOFG-7 increased nitrite production in peripheral blood mononuclear cells, which suggests a potential mechanism of action for this compound. Therefore, these data suggest that guanidine derivatives are potential anti-microbial molecules, and further research is needed to fully understand their mechanism of action, especially in anti-leishmanial studies.-
Descrição: dc.descriptionImmunology of Infectious Diseases Laboratory of Department of Cellular and Molecular Biology Federal University of Paraiba, PB-
Descrição: dc.descriptionBiotechnology Doctoral Program Rede Nordeste de Biotecnologia Universidade Federal da Paraíba, PB-
Descrição: dc.descriptionDepartment of Chemistry and Biochemistry Fine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP), SP-
Descrição: dc.descriptionDepartment of Biotechnology Universidade Federal da Paraíba, PB-
Descrição: dc.descriptionLaboratory of Biochemistry Department of Cellular and Molecular Biology Federal University of Paraiba, PB-
Descrição: dc.descriptionDepartment of Chemistry and Biochemistry Fine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP), SP-
Idioma: dc.languageen-
Relação: dc.relationTropical Medicine and Infectious Disease-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectanti-leishmanial activity-
Palavras-chave: dc.subjectapoptosis-
Palavras-chave: dc.subjectcell death-
Palavras-chave: dc.subjectguanidine compounds-
Palavras-chave: dc.subjectLeishmaniasis-
Palavras-chave: dc.subjectnitrite production-
Título: dc.titleLeishmanicidal Activity of Guanidine Derivatives against Leishmania infantum-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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