Synthesis and evaluation of resveratrol derivatives as fetal hemoglobin inducers

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MetadadosDescriçãoIdioma
Autor(es): dc.contributorUniversidade Estadual Paulista (Unesp)-
Autor(es): dc.contributorUniversidade Estadual de Campinas (UNICAMP)-
Autor(es): dc.contributorWeill Cornell Medical College-
Autor(es): dc.creatorBosquesi, Priscila Longhin [UNESP]-
Autor(es): dc.creatorMelchior, Aylime Castanho Bolognesi [UNESP]-
Autor(es): dc.creatorPavan, Aline Renata [UNESP]-
Autor(es): dc.creatorLanaro, Carolina-
Autor(es): dc.creatorde Souza, Cristiane Maria-
Autor(es): dc.creatorRusinova, Radda-
Autor(es): dc.creatorChelucci, Rafael Consolin [UNESP]-
Autor(es): dc.creatorBarbieri, Karina Pereira [UNESP]-
Autor(es): dc.creatorFernandes, Guilherme Felipe dos Santos [UNESP]-
Autor(es): dc.creatorCarlos, Iracilda Zepone [UNESP]-
Autor(es): dc.creatorAndersen, Olaf Sparre-
Autor(es): dc.creatorCosta, Fernando Ferreira-
Autor(es): dc.creatorDos Santos, Jean Leandro [UNESP]-
Data de aceite: dc.date.accessioned2022-02-22T00:25:44Z-
Data de disponibilização: dc.date.available2022-02-22T00:25:44Z-
Data de envio: dc.date.issued2020-12-11-
Data de envio: dc.date.issued2020-12-11-
Data de envio: dc.date.issued2020-07-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.bioorg.2020.103948-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/198853-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/198853-
Descrição: dc.descriptionResveratrol (RVT) derivatives (10a-i) were designed, synthesized, and evaluated for their potential as gamma-globin inducers in treating Sickle Cell Disease (SCD) symptoms. All compounds were able to release NO at different levels ranging from 0 to 26.3%, while RVT did not demonstrate this effect. In vivo, the antinociceptive effect was characterized using an acetic acid-induced abdominal contortion model. All compounds exhibited different levels of protection, ranging from 5.9 to 37.3%; the compound 10a was the most potent among the series. At concentrations between 3.13 and 12.5 µM, the derivative 10a resulted in a reduction of 41.1–64.3% in the TNF-α levels in the supernatants of macrophages that were previously LPS-stimulated. This inhibitory effect was higher than that of RVT used as the control. In addition, the compound 10a and RVT induced double the production of the gamma-globin chains (γG + γA), compared to the vehicle, using CD34+ cells. Compound 10a also did not induce membrane perturbation and it was not mutagenic in the in vivo assay. Thus, compound 10a emerged as a new prototype of the gamma-globin-inducer group with additional analgesic and anti-inflammatory activities and proving to be a useful alternative to treat SCD symptoms.-
Descrição: dc.descriptionCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)-
Descrição: dc.descriptionOptical Society-
Descrição: dc.descriptionUniversidade Estadual Paulista-
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.descriptionNational Institutes of Health-
Descrição: dc.descriptionSão Paulo State University (UNESP) School of Pharmaceutical Sciences-
Descrição: dc.descriptionUniversity of Campinas (UNICAMP) Hematology and Hemotherapy Center-
Descrição: dc.descriptionWeill Cornell Medical College Department of Physiology and Biophysics-
Descrição: dc.descriptionSão Paulo State University (UNESP) School of Pharmaceutical Sciences-
Descrição: dc.descriptionFAPESP: 2012/50359-2-
Descrição: dc.descriptionFAPESP: 2014/00984-3-
Descrição: dc.descriptionCNPq: 304731/2017-0-
Descrição: dc.descriptionNational Institutes of Health: GM21342-
Idioma: dc.languageen-
Relação: dc.relationBioorganic Chemistry-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectEpigenetic-
Palavras-chave: dc.subjectFetal hemoglobin inducers-
Palavras-chave: dc.subjectGamma-globin inducers-
Palavras-chave: dc.subjectNitric oxide-
Palavras-chave: dc.subjectResveratrol-
Palavras-chave: dc.subjectSickle Cell Disease-
Título: dc.titleSynthesis and evaluation of resveratrol derivatives as fetal hemoglobin inducers-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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