RESUMO
ABSTRACT Purpose: Bioactive molecules are relevant to fight cancer and associated conditions. Quinoxaline is a privileged N-heterocycle, notably as anticancer agents. Herein, we report the evaluation of the quinoxaline derivatives DEQX and OAQX as anticancer agents, as well as in function of their anti-inflammatory and analgesic activities. Methods: Quinoxalines were synthesized and tested as anticancer agents based on cell viability and Annexin V-FITC apoptosis. Anti-inflammatory activity was evaluated from mouse carrageenan peritonitis and levels of interleukin (IL)-1β and tumor necrosis factor (TNF)-alfa for enzyme-linked immunosorbent assay. Hot-plate and acetic acid-induced writing test were employed to investigate analgesia. Results: Both reduced the Ht-29 cell viability in a dependent-concentration manner (p < 0.001). Total apoptosis was detected for cells treated with 12.5 and 25 µg/mL of both the compounds for 24 and 48 h (all doses, p < 0.0001). DEQX (all doses, p < 0.01) and OAQX (all doses, p < 0.001) acted in leukocyte migration and decreased the IL-1β and TNF-β levels (p < 0.05). DEQX (all doses, p < 0.05) and OAQX (5mg/kg, p < 0.001) showed peripheral analgesic effect. Conclusions: In-vitro and in-vivo results suggest that these quinoxalines are promising for application in pharmacological area due to their anticancer, anti-inflammatory, and peripheric analgesia.
RESUMO
OBJETIVO: Comparar o efeito hipotensor a curto prazo das três formulações de colírio de tartarato de brimonidina, Alphagan®, Alphagan® P e Alphagan® Z em olhos normais. MÉTODO: Estudo prospectivo, randomizado, duplo-cego que contou com 60 voluntários, os quais foram submetidos a exame oftalmológico inicial e aferição da pressão intraocular (PIO). Os participantes foram distribuídos em três grupos: 1 tartarato de brimonidina 0,15%, 2 tartarato de brimonidina 0,2% e 3 tartarato de brimonidina 0,1%, aleatoriamente, cada um recebeu uma gota de colírio em cada olho e a pressão intraocular foi aferida após 30 minutos, 1 hora e 2 horas. RESULTADOS: Observou-se que todas as concentrações de tartarato de reduziram significativamente a pressão intraocular durante o tempo estudado, com p<0,05. Ao ser analisada a diferença percentual do efeito hipotensor de cada grupo, verificou-se que não há diferença significativa entre os colírios estudados: (1) -13,50%, (2) -11,50%, (3) -11,90% após 30 minutos (p=0,650); (1) -24,30%, (2) -18,60%, (3) -18,30% após 1 hora (p=0,324); (1) -29,14% (2) -21,20%, (3) -25,60% após 2 horas (p=0,068). CONCLUSÃO: Não há diferença estatisticamente significativa para redução da pressão intraocular (no período de pico) entre as três formulações de brimonidina.
PURPOSE: To compare the hypotensive effect in normal eyes of three formulations with different concentrations of brimonidine tartrate: 0.2%; 0.15% and 0.1%. METHODS: Prospective, randomized, double-blind study included 60 volunteers, who underwent initial ophthalmologic examination and measurement of intraocular pressure (IOP). Individuals were divided into three groups: (1) brimonidine tartrate 0.15%, (2) brimonidine tartrate 0.2% and (3) brimonidine tartrate 0.1% and randomly received one drop each of drops in each eye. The IOP was measured after 30 minutes, 1 hour and 2 hours. RESULTS: We found that all concentrations of brimonidine tartrate significantly reduced intraocular pressure during the study period, with p<0.05. When analyzing the percentage difference of the hypotensive effect of each group, we found no significant difference between the studied groups: (1) -13.50%, (2) -11.50%, (3) -11.90% after 30 minutes (p=0.650); (1) -24.30%, (2) -18.60%, (3) -18.30% after 1 hour (p=0.324); (1) -29.14%, (2) -21.20%, (3) -25.60% after 2 hours (p=0.068). CONCLUSION: There is no statistically significant difference in intraocular pressure reduction (peak period) between the three formulations of brimonidine.