Homologous acetylenic acetogenins from Porcelia macrocarpa R.E. (Fries) displayed potent activity against amastigotes from Trypanosoma cruzi

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorFederal University of ABC-
Autor(es): dc.contributorButantan Institute-
Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorMackenzie Presbyterian University-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.creatorBrito, Ivanildo A.-
Autor(es): dc.creatorCastro Levatti, Erica V.-
Autor(es): dc.creatorRegasini, Luis O.-
Autor(es): dc.creatorFerreira, Edgard A.-
Autor(es): dc.creatorLopes, Flavia B.-
Autor(es): dc.creatorFernandes, João Paulo S.-
Autor(es): dc.creatorBatista, João M.-
Autor(es): dc.creatorTempone, Andre G.-
Autor(es): dc.creatorLago, João Henrique G.-
Data de aceite: dc.date.accessioned2025-08-21T23:22:20Z-
Data de disponibilização: dc.date.available2025-08-21T23:22:20Z-
Data de envio: dc.date.issued2025-04-29-
Data de envio: dc.date.issued2025-03-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.phytochem.2024.114360-
Fonte completa do material: dc.identifierhttps://hdl.handle.net/11449/297585-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/297585-
Descrição: dc.descriptionAs part of our continuous study on the Annonaceae species Porcelia macrocarpa, in the present work, eight chemically related 2-alkyl-3-hydroxy-4-methyl-γ-lactones (1–8) were isolated. Their structures were characterised by NMR, MS, and VCD. Their antitrypanosomal activity was evaluated in vitro against intracellular amastigotes with EC50 values ranged from 13.9 to 1.1 μM for compounds 1–3 and 6–8, while compounds 4 and 5 were inactive (EC50 > 100 μM). Compounds 1–8 did not exert toxicity against NCTC cells at the highest tested concentration (CC50 > 200 μM). Compared with the standard drug benznidazole (EC50 = 3.6 μM and SI > 54.6), compound 8 proved to be the most potent γ-lactone with an EC50 of 1.1 μM and an SI of >181.8. Finally, the structure–activity relationship analysis suggested that flexibility and length of side chain of the related γ-lactones 1–8 play an important role in the activity against amastigotes. The results contribute to the discovery of new molecular prototypes that can be used as scaffolds for developing drugs to treat Chagas disease.-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionConselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionUniversidade Estadual Paulista-
Descrição: dc.descriptionCentre for Natural and Human Sciences Federal University of ABC, Santo Andre, SP-
Descrição: dc.descriptionCentre for Pathophysiology Butantan Institute, SP-
Descrição: dc.descriptionInstitute of Biosciences Humanities and Exact Sciences São Paulo State University, SP-
Descrição: dc.descriptionSchool of Engineering Mackenzie Presbyterian University, SP-
Descrição: dc.descriptionDepartment of Medicine Federal University of São Paulo, SP-
Descrição: dc.descriptionDepartment of Pharmaceutical Sciences Federal University of São Paulo, SP-
Descrição: dc.descriptionInstitute of Science and Technology Federal University of São Paulo, SP-
Descrição: dc.descriptionInstitute of Biosciences Humanities and Exact Sciences São Paulo State University, SP-
Idioma: dc.languageen-
Relação: dc.relationPhytochemistry-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectAcetogenins-
Palavras-chave: dc.subjectAnnonaceae-
Palavras-chave: dc.subjectChagas disease-
Palavras-chave: dc.subjectPorcelia macrocarpa-
Palavras-chave: dc.subjectSAR-
Palavras-chave: dc.subjectTrypanosoma cruzi-
Título: dc.titleHomologous acetylenic acetogenins from Porcelia macrocarpa R.E. (Fries) displayed potent activity against amastigotes from Trypanosoma cruzi-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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