Leishmanicidal Activity of Guanidine Derivatives against Leishmania infantum

Página do item simplificado
dc.contributor.authorAlmeida, Fernanda Silva
dc.contributor.authorMoreira, Vitor Partite [UNESP]
dc.contributor.authorSilva, Edson dos Santos
dc.contributor.authorCardoso, Leonardo Lima
dc.contributor.authorde Sousa Palmeira, Pedro Henrique
dc.contributor.authorCavalcante-Silva, Luiz Henrique Agra
dc.contributor.authorAraújo, Demétrius A. M. de
dc.contributor.authorAmaral, Ian P. G. do
dc.contributor.authorGonzález, Eduardo René Pérez [UNESP]
dc.contributor.authorKeesen, Tatjana S. L.
dc.contributor.institutionFederal University of Paraiba
dc.contributor.institutionUniversidade Federal da Paraíba (UFPB)
dc.contributor.institutionUniversidade Estadual Paulista (UNESP)
dc.date.accessioned2023-07-29T16:09:34Z
dc.date.available2023-07-29T16:09:34Z
dc.date.issued2023-03-01
dc.description.abstractLeishmaniasis 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.en
dc.description.affiliationImmunology of Infectious Diseases Laboratory of Department of Cellular and Molecular Biology Federal University of Paraiba, PB
dc.description.affiliationBiotechnology Doctoral Program Rede Nordeste de Biotecnologia Universidade Federal da Paraíba, PB
dc.description.affiliationDepartment of Chemistry and Biochemistry Fine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP), SP
dc.description.affiliationDepartment of Biotechnology Universidade Federal da Paraíba, PB
dc.description.affiliationLaboratory of Biochemistry Department of Cellular and Molecular Biology Federal University of Paraiba, PB
dc.description.affiliationUnespDepartment of Chemistry and Biochemistry Fine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP), SP
dc.identifierhttp://dx.doi.org/10.3390/tropicalmed8030141
dc.identifier.citationTropical Medicine and Infectious Disease, v. 8, n. 3, 2023.
dc.identifier.doi10.3390/tropicalmed8030141
dc.identifier.issn2414-6366
dc.identifier.scopus2-s2.0-85151001512
dc.identifier.urihttp://hdl.handle.net/11449/249799
dc.language.isoeng
dc.relation.ispartofTropical Medicine and Infectious Disease
dc.sourceScopus
dc.subjectanti-leishmanial activity
dc.subjectapoptosis
dc.subjectcell death
dc.subjectguanidine compounds
dc.subjectLeishmaniasis
dc.subjectnitrite production
dc.titleLeishmanicidal Activity of Guanidine Derivatives against Leishmania infantumen
dc.typeArtigo
unesp.author.orcid0000-0003-4924-0542[4]
unesp.author.orcid0000-0002-9323-7677[5]
unesp.author.orcid0000-0002-8445-5189[6]
unesp.author.orcid0000-0003-1348-8554[9]
unesp.author.orcid0000-0003-0964-389X[10]
unesp.departmentFísica, Química e Biologia - FCTpt

Arquivos

Coleções

Presidente Prudente - FCT - Faculdade de Ciências e Tecnologia