Programa de Pós-Graduação em Biotecnologia e Biodiversidade, Universidade Federal de Mato Grosso do Sul, Cidade Universitária, Avenida Costa e Silva - Pioneiros, Campo Grande, MS, 79070-900, Brazil.
Programa de Pós-Graduação em Biotecnologia, Universidade Católica Dom Bosco, Avenida Tamandaré, 6000 - Jardim seminário, Campo Grande, MS, 79117-010, Brazil.
Eur J Pharm Sci. 2020 May 30;148:105300. doi: 10.1016/j.ejps.2020.105300. Epub 2020 Mar 8.
In order to discover a new compound having anti-inflammatory activity, a nitro-Schiff base was evaluated. The compound was synthesized and characterized by H NMR and C NMR. The cytotoxic activity was evaluated in vitro by hemolysis and MTT cell viability assay. To evaluate genotoxicity, the micronucleus assay was performed in vivo. The anti-inflammatory effects of the compound were examined using in vivo models of inflammation such as neutrophil migration assay, paw edema, and exudation assay. The production of NO was also estimated in vivo and in vitro. The data showed that the compound did not induce hemolysis at all the tested concentrations. Similarly, the compound did not induce cytotoxicity and genotoxicity to the cells. The neutrophil migration assay showed that the compound reduced the number of neutrophils recruited to the peritoneal cavity by approximately 60% at all the tested concentrations. In the exudation assay, the compound showed a reduction in extravasation by 24%. The paw edema model demonstrated a significant reduction in the paw volume at all the evaluated time points. The production of NO was decreased both in vitro and in vivo. These results suggest that the nitro-Schiff base compound efficiently inhibited inflammation and might be a good candidate for the treatment of inflammatory-associated conditions.
为了发现具有抗炎活性的新化合物，评估了硝基席夫碱。通过 H NMR 和 C NMR 对化合物进行了合成和表征。通过溶血和 MTT 细胞活力测定评估体外细胞毒性。为了评估遗传毒性，在体内进行了微核试验。在体内炎症模型如中性粒细胞迁移试验、足肿胀和渗出试验中研究了化合物的抗炎作用。还在体内和体外估计了 NO 的产生。数据表明，该化合物在所有测试浓度下均未引起溶血。同样，该化合物对细胞没有诱导细胞毒性和遗传毒性。中性粒细胞迁移试验表明，该化合物在所有测试浓度下将募集到腹腔的中性粒细胞数量减少了约 60%。在渗出试验中，化合物的渗出减少了 24%。足肿胀模型在所有评估的时间点均显示出显著的足肿胀体积减少。NO 的产生无论是在体外还是体内都有所减少。这些结果表明，硝基席夫碱化合物能有效抑制炎症，可能是治疗炎症相关疾病的良好候选药物。
