Wilhelm Ethel A, Ferreira Ana Teresinha, Pinz Mikaela P, Reis Angélica S Dos, Vogt Ane G, Stein Andre L, Zeni Gilson, Luchese Cristiane
Centro de Ciências Químicas, Farmacêuticas e de Alimentos, Universidade Federal de Pelotas, Capão do Leão, RS, Brazil.
Departamento de Química, Centro de Ciências Naturais e Exatas, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.
An Acad Bras Cienc. 2017 May;89(1 Suppl 0):457-467. doi: 10.1590/0001-3765201720160668. Epub 2017 May 22.
The present study investigated the antioxidant effect of a new class of quinoline derivatives (a-d) on assays in vitro. Lipid peroxidation, thiol peroxidase-like and free radical scavenging activities were determined to evaluate antioxidant activity of compounds. Thiol oxidase-like and δ-aminolevulinate dehydratase activities were performed as a toxicological parameter. A second objective of this study was to evaluate the in vivo antinociceptive effect of the compound with better antioxidant effect and without toxic effects in a model of nociception induced by formalin in mice. In liver, at 100 µM, compound a reduced the lipid peroxidation to the control levels, while compounds c and d partially reduced it. In brain, only compound d partially reduced the lipid peroxidation at 50 and 100 µM. Compound b did not have an effect on the lipid peroxidation. Thiol peroxidase-like and free radical scavenging activities are not involved in the antioxidant mechanisms of these compounds. Compounds did not present thiol oxidase-like activity and effect on the δ-aminolevulinate dehydratase. In vivo experiments showed that compound a caused an inhibition of licking time in the first and second phases, and edema formation induced by formalin. In conclusion, quinoline derivative without selenium presented better in vitro antioxidant effect and in vivo antinociceptive activity.
本研究在体外试验中考察了一类新型喹啉衍生物（a - d）的抗氧化作用。通过测定脂质过氧化、硫醇过氧化物酶样活性和自由基清除活性来评估化合物的抗氧化活性。进行硫醇氧化酶样活性和δ-氨基乙酰丙酸脱水酶活性测定作为毒理学参数。本研究的第二个目的是在小鼠福尔马林诱导的伤害感受模型中，评估具有较好抗氧化作用且无毒性作用的化合物的体内抗伤害感受作用。在肝脏中，浓度为100 μM时，化合物a将脂质过氧化降低至对照水平，而化合物c和d仅部分降低了脂质过氧化。在大脑中，仅化合物d在50 μM和100 μM时部分降低了脂质过氧化。化合物b对脂质过氧化无影响。硫醇过氧化物酶样活性和自由基清除活性不参与这些化合物的抗氧化机制。化合物未表现出硫醇氧化酶样活性，对δ-氨基乙酰丙酸脱水酶也无影响。体内实验表明，化合物a在第一和第二阶段抑制了舔舐时间以及福尔马林诱导的水肿形成。总之，不含硒的喹啉衍生物在体外具有较好的抗氧化作用，在体内具有抗伤害感受活性。
