Discovery of (E)-4-styrylphenoxy-propanamide: A dual PPARα/γ partial agonist that regulates high-density lipoprotein-cholesterol levels, modulates adipogenesis, and improves glucose tolerance in diet-induced obese mice

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorCampos Univ. Darcy Ribeiro s/n – Asa Norte-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorRua Vergueiro 235/249 – Liberdade-
Autor(es): dc.creatorDutra, Luiz A.-
Autor(es): dc.creatorLacerda, Mariella G.-
Autor(es): dc.creatorDestro Inácio, Maiara-
Autor(es): dc.creatorMartins, Johnny W.L.-
Autor(es): dc.creatorLopes Silva, Ana C.-
Autor(es): dc.creatorBento da Silva, Patricia-
Autor(es): dc.creatorChorilli, Marlus-
Autor(es): dc.creatorAmato, Angélica A.-
Autor(es): dc.creatorBaviera, Amanda M.-
Autor(es): dc.creatorPassarelli, Marisa-
Autor(es): dc.creatorGuido, Rafael V.C.-
Autor(es): dc.creatorDos Santos, Jean L.-
Data de aceite: dc.date.accessioned2025-08-21T16:30:06Z-
Data de disponibilização: dc.date.available2025-08-21T16:30:06Z-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2022-04-29-
Data de envio: dc.date.issued2022-03-01-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1016/j.bioorg.2022.105600-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/231602-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/231602-
Descrição: dc.descriptionPeroxisome proliferator-activated receptors are promising therapeutic targets for metabolic diseases, including obesity, diabetes, and dyslipidemia. This study describes the design, synthesis and pharmacological evaluation of stilbene-based compounds as dual PPARα/γ partial agonists with potency in the nanomolar range. In vitro and in vivo assays revealed that the lead compound (E)-4-styrylphenoxy-propanamide (5b) removed 14C-cholesterol from the foam cells through apolipoprotein A-I and High-Density Lipoprotein-2. In the high-fat diet-induced obesity mouse model, the oral administration of compound 5b increased HDL levels, paraoxonase-1 activity, and insulin sensitivity, and decreased glucose levels. Moreover, the adipogenesis pathway and triglyceride accumulation slightly changed in the adipocyte cells upon treatment with compound 5b, without affecting the body weight and adipose tissue in obese mice. Compound 5b did not affect the plasma levels of hepatic and renal injury biomarkers. Thus, stilbene-based compound 5b is a promising prototype for developing novel candidates to treat dyslipidemia and diabetes.-
Descrição: dc.descriptionSchool of Pharmaceutical Science São Paulo State University (UNESP) Rodovia Araraquara Jaú Km 01 – s/n-
Descrição: dc.descriptionLaboratory of Molecular Pharmacology Faculty of Health Sciences University of Brasilia Campos Univ. Darcy Ribeiro s/n – Asa Norte-
Descrição: dc.descriptionLaboratório de Lípides (LIM 10) Hospital das Clínicas (HCFMUSP) da Faculdade de Medicina da Universidade de São Paulo, Av. Dr. Arnaldo 455 – Cerqueira César-
Descrição: dc.descriptionPrograma de Pós-Graduação em Medicina da Universidade Nove de Julho – UNINOVE Rua Vergueiro 235/249 – Liberdade-
Descrição: dc.descriptionSão Carlos Institute of Physics University of Sao Paulo, Av. João Dagnone 1100 – São Carlos-SP-
Descrição: dc.descriptionSchool of Pharmaceutical Science São Paulo State University (UNESP) Rodovia Araraquara Jaú Km 01 – s/n-
Idioma: dc.languageen-
Relação: dc.relationBioorganic Chemistry-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectAdipogenesis-
Palavras-chave: dc.subjectGlucose homeostasis-
Palavras-chave: dc.subjectHDL-C-
Palavras-chave: dc.subjectPON1-
Palavras-chave: dc.subjectPPARs-
Palavras-chave: dc.subjectStilbene-
Título: dc.titleDiscovery of (E)-4-styrylphenoxy-propanamide: A dual PPARα/γ partial agonist that regulates high-density lipoprotein-cholesterol levels, modulates adipogenesis, and improves glucose tolerance in diet-induced obese mice-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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