Title:Antioxidant, Antitumor and Bactericidal Activities of Ethyl Gallate Quinoxalines
VOLUME: 16 ISSUE: 6
Author(s):Rafaely N. Lima, Jaqueline R. Gonçalves, Valdenizia R. Silva, Luciano de S. Santos, Daniel P. Bezerra, Milena B.P. Soares, Andrei Leitão and André L.M. Porto*
Affiliation:Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, Av. Joao Dagnone, 1100, Ed. Quimica Ambiental, Santa Angelina, 13563-120, Sao Carlos, SP, Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, Av. Joao Dagnone, 1100, Ed. Quimica Ambiental, Santa Angelina, 13563-120, Sao Carlos, SP, Instituto Goncalo Moniz, Fundacao Oswaldo Cruz, R. Waldemar- Falcao, 121, 40296-710, Candeal, Salvador, BA, Instituto Goncalo Moniz, Fundacao Oswaldo Cruz, R. Waldemar- Falcao, 121, 40296-710, Candeal, Salvador, BA, Instituto Goncalo Moniz, Fundacao Oswaldo Cruz, R. Waldemar- Falcao, 121, 40296-710, Candeal, Salvador, BA, Instituto Goncalo Moniz, Fundacao Oswaldo Cruz, R. Waldemar- Falcao, 121, 40296-710, Candeal, Salvador, BA, Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, Av. Trabalhador Sao Carlense, 400, CP 780, 13.560-970, Sao Carlos, SP, Instituto de Quimica de Sao Carlos, Universidade de Sao Paulo, Av. Joao Dagnone, 1100, Ed. Quimica Ambiental, Santa Angelina, 13563-120, Sao Carlos, SP
Keywords:Antitumor, cytotoxicity, DPPH, disk-diffusion, gallic acid, docking study.
Abstract:
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.
Methods: We 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.