Benzophenone derivatives showed dual anti-inflammatory and antiproliferative activities by inhibiting cox enzymes and promote cyclin e downregulation.

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dc.contributor.authorFolquitto, Laís Regina dos Santos
dc.contributor.authorSouza, Thiago Belarmino de
dc.contributor.authorJanuário, Jaqueline Pereira
dc.contributor.authorNascimento, Isadora M.
dc.contributor.authorBrandão, Brenda Tavares de Vasconcelos
dc.contributor.authorMoreira, Maria E. C.
dc.contributor.authorHorvath, Renato de Oliveira
dc.contributor.authorSantos, Marcelo Henrique dos
dc.contributor.authorCoelho, Luiz Felipe Leomil
dc.contributor.authorVeloso, Marcia Paranho
dc.contributor.authorSoares, Marisi Gomes
dc.contributor.authorCarvalho, Diogo Teixeira
dc.contributor.authorIonta, Marisa
dc.contributor.authorPaula, Daniela Aparecida Chagas de
dc.contributor.authorDias, Danielle Ferreira
dc.date.accessioned2022-12-07T20:10:50Z
dc.date.available2022-12-07T20:10:50Z
dc.date.issued2022pt_BR
dc.description.abstractConsidering the promising antitumor effects of compounds with dual anti-inflammatory and antiproliferative activities, thus benzophenones analogs (2-7) were evaluated on in vivo anti- inflammatory assay and molecular docking analysis. Those with the best molecular docking results were in vitro evaluated on cyclooxygenase (COX) enzymes and tested regarding antiproliferative activity. All derivatives displayed in vivo anti-inflammatory activity. Among them, the substances 2’-hydroxy-4’-benzoylphenyl-β-D-glucopyranoside (4), 4-hydroxy-4’-methoxybenzophenone (5) and 4’-(4’’-methoxybenzoyl)phenyl-β-D-glucopyranoside (7)showed the best values of Glide Score in COX-2 docking evaluation and 4 and 5 selectively inhibited COX-2 and COX-1 in vitro enzymatic assay, respectively. Thus, 4 and 5 were tested against breast cancer (MCF-7, MDA-MB-231, Hs578T) and non-small-cell-lung cancer (A549) cell lines. The estrogen-positive MCF-7 cell line was more responsive compared to other tested cell lines. They induced cell cycle arrest at G1/S transition in MCF-7 cell line once there was an increase in G0/G1 population with concomitant reduction of S population. The antiproliferative activity of these substances on MCF-7 was associated with their ability to inhibit cyclin E expression, a critical regulator of G1/S transition. Taken together, the data indicate that 4 and 5 have dual anti-inflammatory and antiproliferative activities and support further studies to evaluate their antitumor potential.pt_BR
dc.identifier.citationFOLQUITTO, L. R. dos S. et al. Benzophenone derivatives showed dual anti-inflammatory and antiproliferative activities by inhibiting cox enzymes and promote cyclin e downregulation. Journal of The Brazilian Chemical Society, v. 33, n. 4, 2022. Disponível em: <https://www.scielo.br/j/jbchs/a/vQWfZ7vcwWjt8bHCnpVSydR/>. Acesso em: 11 out. 2022.pt_BR
dc.identifier.doihttps://doi.org/10.21577/0103-5053.20210154pt_BR
dc.identifier.issn1678-4790
dc.identifier.urihttp://www.repositorio.ufop.br/jspui/handle/123456789/15877
dc.language.isoen_USpt_BR
dc.rightsabertopt_BR
dc.rights.licenseThis is an open-access article distributed under the terms of the Creative Commons Attribution License. Fonte: o PDF do artigo.pt_BR
dc.subjectMolecular dockingpt_BR
dc.subjectEar edemapt_BR
dc.subjectBreast cancerpt_BR
dc.subjectTriple-negativept_BR
dc.titleBenzophenone derivatives showed dual anti-inflammatory and antiproliferative activities by inhibiting cox enzymes and promote cyclin e downregulation.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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