Evidence of Guanidines Potential against Leishmania (Viannia) braziliensis: Exploring In Vitro Effectiveness, Toxicities and of Innate Immunity Response Effects

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorFederal University of Parnaíba Delta—UFDPar-
Autor(es): dc.contributorUniversity of Vienna-
Autor(es): dc.contributorInstituto Oswaldo Cruz-
Autor(es): dc.contributorParacelsus Medical University-
Autor(es): dc.creatordos Anjos, Luana Ribeiro-
Autor(es): dc.creatorde Souza, Vanessa Maria Rodrigues-
Autor(es): dc.creatorMachado, Yasmim Alves Aires-
Autor(es): dc.creatorPartite, Vitor Moreira-
Autor(es): dc.creatorAufy, Mohammed-
Autor(es): dc.creatorDias Lopes, Geovane-
Autor(es): dc.creatorStudenik, Christian-
Autor(es): dc.creatorAlves, Carlos Roberto-
Autor(es): dc.creatorLubec, Gert-
Autor(es): dc.creatorGonzalez, Eduardo Rene Perez-
Autor(es): dc.creatorRodrigues, Klinger Antonio da Franca-
Data de aceite: dc.date.accessioned2025-08-21T16:03:03Z-
Data de disponibilização: dc.date.available2025-08-21T16:03:03Z-
Data de envio: dc.date.issued2025-04-29-
Data de envio: dc.date.issued2023-12-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.3390/biom14010026-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/308076-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/308076-
Descrição: dc.descriptionLeishmaniasis is a complex group of infectious and parasitic diseases that afflict many thousands of individuals across five continents. Leishmaniasis treatment remains a challenge because it relies on drugsknown for their high toxicity and limited efficacy, making itimperative to identify new molecules that offer greater effectiveness and safety. This study sought to explore the impact of seven synthetic guanidine derivatives (LQOF-G1, LQOF-G2, LQOF-G6, LQOF-G7, LQOF-G32, LQOF-G35 and LQOF-G36) onthe parasite Leishmania (Viannia) braziliensis and in vitro macrophage infection by this parasite, as well as cytotoxic approaches in vitro models of mammalian host cells and tissues. The synthesized compounds showed purity ≥ 99.65% and effectively inhibited parasite growth. LQOF-G1 proved the most potent, yielding the best half-maximal inhibitory concentration (IC50) values against promastigotes (4.62 μmol/L), axenic amastigotes (4.27 μmol/L), and intracellular amastigotes (3.65 μmol/L). Notably, the antileishmanial activity of LQOF-G1, LQOF-G2, and LQOF-G6 was related to immunomodulatory effects, evidenced by alterations in TNF-α, IL-12, IL-10, nitric oxide (NO), and reactive oxygen species (ROS) levels in the supernatant of culture macrophages infected with L. (V.) braziliensis and coincubated with these compounds. LQOF-G2 and LQOF-G36 compounds exhibited vasodilator and spasmolytic effects at higher concentrations (≥100 μmol/L). Generally, LQOF-G1, LQOF-G2, and LQOF-G32 compounds were found to be nontoxic to assessed organs and cells. No toxic effects were observed in human cell lines, such as HEK-293, CaCo-2 and A549, at concentrations ≥ 500 μmol/L. Collectively, data have shown unequivocal evidence of the effectiveness of these compounds against L. (V.) braziliensis parasite, one of the causative agents of Tegumentary Leishmaniasis and Mucocutaneous Leishmaniasis in America.-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionFinanciadora de Estudos e Projetos-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado do Rio de Janeiro (FAPERJ)-
Descrição: dc.descriptionFine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP)-
Descrição: dc.descriptionInfectious Disease Laboratory—LADIC Federal University of Parnaíba Delta—UFDPar, Campus Ministro Reis Velloso, Parnaíba-
Descrição: dc.descriptionDepartment of Pharmaceutical Sciences Division of Pharmacology and Toxicology University of Vienna, Josef Holaubek Platz 2, UZAII (2D 259)-
Descrição: dc.descriptionLaboratório de Biologia Molecular e Doenças Endêmicas Fundação Oswaldo Cruz Instituto Oswaldo Cruz, 4365, Manguinhos-
Descrição: dc.descriptionDepartment of Neuroproteomics Paracelsus Medical University-
Descrição: dc.descriptionFine Organic Chemistry Lab School of Sciences and Technology São Paulo State University (UNESP)-
Descrição: dc.descriptionFinanciadora de Estudos e Projetos: 01.23.0034.00 (0419/22)-
Descrição: dc.descriptionFAPESP: 2021/0595-8-
Descrição: dc.descriptionCNPq: 301744/2019-0-
Descrição: dc.descriptionCNPq: 403260/2021-3-
Descrição: dc.descriptionFAPERJ: E-26/010.000983/2019-
Descrição: dc.descriptionFAPERJ: E-26/200.799/2021-
Descrição: dc.descriptionFAPERJ: E-26/204.189/2021-
Idioma: dc.languageen-
Relação: dc.relationBiomolecules-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectguanidine derivatives-
Palavras-chave: dc.subjectimmunomodulation-
Palavras-chave: dc.subjectLeishmania (Viannia) braziliensis-
Palavras-chave: dc.subjectorgan and cell toxicity-
Título: dc.titleEvidence of Guanidines Potential against Leishmania (Viannia) braziliensis: Exploring In Vitro Effectiveness, Toxicities and of Innate Immunity Response Effects-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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