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Synthesis and biological activities of a nitro-shiff base compound as a potential anti-inflammatory agent.
European Journal of Pharmaceutical Sciences ( IF 4.6 ) Pub Date : 2020-03-08 , DOI: 10.1016/j.ejps.2020.105300
Beatriz Cardoso Roriz 1 , Danieli Fernanda Buccini 2 , Beatriz Fuzinato Dos Santos 3 , Suellen Rolon de Sousa Silva 2 , Nelson Luís de Campos Domingues 3 , Susana Elisa Moreno 2
Affiliation  

In order to discover a new compound having anti-inflammatory activity, a nitro-Schiff base was evaluated. The compound was synthesized and characterized by 1H NMR and 13C 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.

中文翻译:

硝基席夫碱化合物作为潜在的消炎药的合成和生物活性。

为了发现具有抗炎活性的新化合物,对硝基席夫碱进行了评价。合成该化合物,并通过1 H NMR和13 C NMR进行表征。通过溶血和MTT细胞活力测定在体外评价细胞毒性活性。为了评估遗传毒性,在体内进行了微核分析。使用诸如中性粒细胞迁移测定,爪水肿和渗出测定之类的体内炎症模型检查化合物的抗炎作用。还估计了体内和体外NO的产生。数据显示该化合物在所有测试浓度下均未诱导溶血。类似地,该化合物不诱导对细胞的细胞毒性和遗传毒性。中性粒细胞迁移测定表明,在所有测试浓度下,该化合物均减少了募集至腹膜腔的中性粒细胞数量约60%。在渗出测定中,该化合物显示出渗出减少了24%。爪水肿模型在所有评估的时间点均显示爪体积明显减少。在体外和体内NO的产生均降低。这些结果表明,硝基席夫碱化合物可有效抑制炎症,可能是治疗炎症相关疾病的良好候选者。爪水肿模型在所有评估的时间点均显示爪体积明显减少。在体外和体内NO的产生均降低。这些结果表明,硝基席夫碱化合物可有效抑制炎症,并且可能是治疗炎症相关病症的良好候选者。爪水肿模型在所有评估的时间点均显示爪体积明显减少。在体外和体内NO的产生均降低。这些结果表明,硝基席夫碱化合物可有效抑制炎症,并且可能是治疗炎症相关病症的良好候选者。
更新日期:2020-03-09
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