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首页> 外文期刊>Journal of biochemical and molecular toxicology >Discovery of novel pyrazole derivatives as a potent anti-inflammatory agent in RAW264.7 cells via inhibition of NF-kappaB for possible benefit against SARS-CoV-2
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Discovery of novel pyrazole derivatives as a potent anti-inflammatory agent in RAW264.7 cells via inhibition of NF-kappaB for possible benefit against SARS-CoV-2

机译：通过抑制NF-Kappab对SARS-COV-2可能益处的NF-Kappab，将新型吡唑衍生物作为Raw264.7细胞中的有效抗炎剂的发现

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摘要

Due to unavailability of a specific drug/vaccine to attenuate severe acute respiratory syndrome coronavirus 2, the current strategy to combat the infection has been largely dependent upon the use of anti-inflammatory drugs to control cytokines storm responsible for respiratory depression. Thus, in this study, we discovered novel pyrazole analogs as a potent nuclear factor kappa B (NF-kappaB) inhibitor. The compounds were assessed for NF-kappaB transcriptional inhibitory activity in RAW264.7 cells after stimulation with lipopolysaccharides (LPS), revealing Compound 6c as the most potent analog among the tested series. The effect of Compound 6c was further investigated on the levels of interleukin-1beta, tumor necrosis factor-alpha, and interleukin-6 in LPS-stimulated RAW267.4 cells by enzyme immunoassay, where it causes a significant reduction in the level of these cytokines. In Western blot analysis, Compound 6c also causes the inhibition of inhibitor kappa B-alpha and NF-kappaB. It was found to be snugly fitted into the inner grove of the active site of NF-kappaB by forming H-bonds and a nonbonded interaction with Asn28 in a docking analysis.
机译：由于缺乏一种特定的药物/疫苗来减弱严重急性呼吸综合征冠状病毒2型，目前对抗这种感染的策略在很大程度上依赖于使用抗炎药来控制导致呼吸抑制的细胞因子。因此，在这项研究中，我们发现新型吡唑类似物是一种有效的核因子-κB（NF-κB）抑制剂。评估这些化合物在RAW264中的NF-κB转录抑制活性。用脂多糖（LPS）刺激7个细胞后，发现化合物6c是测试系列中最有效的类似物。进一步研究了化合物6c对LPS刺激的RAW267中白细胞介素-1β、肿瘤坏死因子α和白细胞介素-6水平的影响。4.通过酶免疫分析检测细胞，使这些细胞因子的水平显著降低。在Western blot分析中，化合物6c也会抑制抑制剂κB-α和NF-κB。在对接分析中，通过形成氢键和与Asn28的非键相互作用，发现它紧密贴合在NF-κB活性位点的内凹槽中。

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