Benzophenone derivatives showed dual anti-inflammatory and antiproliferative activities by inhibiting cox enzymes and promote cyclin e downregulation.
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2022
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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.
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Molecular docking, Ear edema, Breast cancer, Triple-negative
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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.