Antioxidant, Antitumor and Bactericidal Activities of Ethyl Gallate Quinoxalines

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Author(s): Rafaely N. Lima*, Jaqueline R. Gonçalves, Valdenizia R. Silva, Luciano de S. Santos, Daniel P. Bezerra, Milena B. P. Soares, Andrei Leitão, André L. M. Porto*.

Journal Name: Current Bioactive Compounds

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Background: Quinoxaline, a fused heterocycle of benzene and pyrazine rings are becoming recognized as a potent class of anti-cancer compounds, such as, in a wide array of pharmacological activities.

Objectives: The objective of this study was evaluate the three gallate quinoxalines (G-A1, G-A2, and G-A3) as c-Met kinase inhibitors using a docking study, in vitro anticancer potential measurements, antioxidant and bactericidal activities.

Results: The docking study showed hydrogen bond linkage of quinoxalines with amino acids at active site of c-Met kinase structures, indicating a possible cancer inhibition cell proliferation. Therefore, the three quinoxalines were analyzed against four in vitro cancer cell lines, and G-A1 demonstrated cytotoxicity against HL-60 and HCT116 cell lines (IC50= 9.55 and IC50= 16.67 μmol L-1, respectively). In HepG2 and MCF-7 cells, the IC50 were 22.48 and 33.42 μmol L-1, respectively. For G-A2 and G-A3, cytotoxic activity ranged from 61.22 to >101.21 μmol L-1. Potent antioxidant activities were also obtained for G-A2>G-A1>G-A3 (IC50= 4.5-8.4 μmol L-1 and AAI= 8.8-17.8). Six different Bacillius strains showed growth inhibition (11.33 to 13.33 mm) in the presence of quinoxaline G-A1 (500 µg).

Conclusion: The present work showed the biological potential of quinoxalines G-A1, G-A2 and G-A3 in inhibiting four cancer cells proliferation, in addition to a very strong antioxidant activity.

Keywords: Antitumor, Cytotoxicity, DPPH, disk-diffusion, gallic acid, docking studAntitumor, docking study

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(E-pub Ahead of Print)
DOI: 10.2174/1573407215666190318144105
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