SYNTHESIS OF (-)-6,6'-DINITROHINOKININ FROM HINOKININ NATURAL PRODUCT AND in silico AND in vitro TRYPANOCIDAL ACTIVITY ASSESSMENT

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Autor(es): dc.contributorUniversidade de Franca-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversidade Federal do Espírito Santo (UFES)-
Autor(es): dc.contributorUniversidade Federal de Santa Catarina (UFSC)-
Autor(es): dc.creatorCardoso, Suziene Caroline Silva-
Autor(es): dc.creatorCunha, Wilson R.-
Autor(es): dc.creatorCavallari, Pedro S. Dos S. R.-
Autor(es): dc.creatorAlmeida, Samarah Gomes DE-
Autor(es): dc.creatorJanuário, Ana Helena-
Autor(es): dc.creatorPauletti, Patrícia Mendonça-
Autor(es): dc.creatorSantos, Fernanda Amorim-
Autor(es): dc.creatorLaurentiz, Rosângela da Silva-
Autor(es): dc.creatorMiranda, Giulia Stavrakas-
Autor(es): dc.creatorAndrade, João Victor-
Autor(es): dc.creatorOrenha, Renato Pereira-
Autor(es): dc.creatorParreira, Renato Luis Tame-
Autor(es): dc.creatorAndrade E Silva, Márcio Luís-
Autor(es): dc.creatorSantos, Mario F. C.-
Autor(es): dc.creatorEsperandim, Viviane-
Data de aceite: dc.date.accessioned2025-08-21T22:31:53Z-
Data de disponibilização: dc.date.available2025-08-21T22:31:53Z-
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/10.14393/BJ-v40n0a2024-69502-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/301489-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/301489-
Descrição: dc.descriptionChagas disease is a public health problem affecting approximately seven million people worldwide. Thus, there is a need to discover drugs for the adequate treatment of this disease because currently available drugs have serious side effects. Therefore, this study aimed to evaluate the in vitro trypanocidal activity of (-)-6,6'-dinitrohinokinin, obtained from the partial synthesis of (-)-hinokinin, on the trypomastigotes and amastigotes forms. For the trypomastigote assay, blood was collected from mice infected with Trypanosoma cruzi through cardiac puncture at the parasitemic peak. The results show that (-)-6,6'-dinitrohinokinin was effective against the trypomastigote forms, presenting an IC50 of 19.83 µM and lysis percentage values of 78.4% and 69.4% at concentrations of 200 and 100 µM, respectively. Molecular docking calculations indicate that (-)-6,6'-dinitrohinokinin favorably interacts with the amino acids present in the active site of the protein trypanothione reductase, a typical target for anti-trypanosomal drug development. According to the results, the (-)-6,6'-dinitrohinokinin showed more significant trypanocidal activity with IC50 of 1.83 µM than benzonidazole positive control with IC50 of 53.2 µM, showing to be a prototype molecule promising for the development of a new antiparasitic drug.-
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.descriptionResearch Center in Exact and Technological Sciences Universidade de Franca, São Paulo-
Descrição: dc.descriptionScience graduate program Research Center in Exact and Technological Sciences Universidade de Franca, São Paulo-
Descrição: dc.descriptionDepartment of Physics and Chemistry Faculty of Engineering of Ilha Solteira Universidade Estadual Paulista, São Paulo-
Descrição: dc.descriptionBiological sciences graduation Universidade Federal do Espírito Santo, Espírito Santo-
Descrição: dc.descriptionChemistry and Physics Department Exact Natural and Health Sciences Center Universidade Federal do Espírito Santo, Espírito Santo-
Descrição: dc.descriptionChemistry graduation Universidade Federal do Espírito Santo Alto Universitário, Espírito Santo-
Descrição: dc.descriptionDepartment of Chemistry Universidade Federal de Santa Catarina, Campus Universitário Trindade, Santa Catarina-
Descrição: dc.descriptionDepartment of Physics and Chemistry Faculty of Engineering of Ilha Solteira Universidade Estadual Paulista, São Paulo-
Descrição: dc.descriptionCNPq: 150704/2022–4-
Descrição: dc.descriptionCNPq: 311122/2021–3-
Descrição: dc.descriptionCNPq: t 2011/07623–8-
Idioma: dc.languageen-
Relação: dc.relationBioscience Journal-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectMolecular docking-
Palavras-chave: dc.subjectNatural products-
Palavras-chave: dc.subjectTrypanocide-
Palavras-chave: dc.subjectTrypanosoma cruzi-
Título: dc.titleSYNTHESIS OF (-)-6,6'-DINITROHINOKININ FROM HINOKININ NATURAL PRODUCT AND in silico AND in vitro TRYPANOCIDAL ACTIVITY ASSESSMENT-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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