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Title: | Benzophenone derivatives showed dual anti-inflammatory and antiproliferative activities by inhibiting cox enzymes and promote cyclin e downregulation. |
Authors: | Folquitto, Laís Regina dos Santos Souza, Thiago Belarmino de Januário, Jaqueline Pereira Nascimento, Isadora M. Brandão, Brenda Tavares de Vasconcelos Moreira, Maria E. C. Horvath, Renato de Oliveira Santos, Marcelo Henrique dos Coelho, Luiz Felipe Leomil Veloso, Marcia Paranho Soares, Marisi Gomes Carvalho, Diogo Teixeira Ionta, Marisa Paula, Daniela Aparecida Chagas de Dias, Danielle Ferreira |
Keywords: | Molecular docking Ear edema Breast cancer Triple-negative |
Issue Date: | 2022 |
Citation: | FOLQUITTO, 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. |
Abstract: | Considering 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. |
URI: | http://www.repositorio.ufop.br/jspui/handle/123456789/15877 |
metadata.dc.identifier.doi: | https://doi.org/10.21577/0103-5053.20210154 |
ISSN: | 1678-4790 |
metadata.dc.rights.license: | This is an open-access article distributed under the terms of the Creative Commons Attribution License. Fonte: o PDF do artigo. |
Appears in Collections: | DEFAR - Artigos publicados em periódicos |
Files in This Item:
File | Description | Size | Format | |
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ARTIGO_BenzophenoneDerivativesShowed.pdf | 1,55 MB | Adobe PDF | View/Open |
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