Laboratory of Cell Biology, Federal University of Alagoas, 57072-900, Maceió, Brazil.
Laboratory of Bioinformatics and Computational Chemistry, State University of Southwest of Bahia, 45700-000, Bahia, Brazil.
Eur J Pharmacol. 2021 Apr 15;897:173929. doi: 10.1016/j.ejphar.2021.173929. Epub 2021 Feb 6.
Acute lung injury (ALI) remains to cause a high rate of mortality in critically ill patients. It is known that inflammation is a key factor in the pathogenesis of lipopolysaccharide (LPS)-induced ALI, which makes it a relevant approach to the treatment of ALI. In this study, we evaluated the potential of nasally instilled p-coumaric acid to prevent LPS-induced ALI in mice, by evaluating its effects on cellular and molecular targets involved in inflammatory response via in vitro and in silico approaches. Our results demonstrated that p-coumaric acid reduced both neutrophil accumulation and pro-inflammatory cytokine abundance, and simultaneously increased IL-10 production at the site of inflammation, potentially contributing to protection against LPS-induced ALI in mice. In the in vitro experiments, we observed inhibitory effects of p-coumaric acid against IL-6 and IL-8 production in stimulated A549 cells, as well as reactive oxygen species generation by neutrophils. In addition, p-coumaric acid treatment decreased neutrophil adhesion on the TNF-α-stimulated endothelial cells. According to the in silico predictions, p-coumaric acid reached stable interactions with both the ATP-binding site of IKKβ as well as the regions within LFA-1, critical for interaction with ICAM-1, thereby suppressing the production of proinflammatory mediators and hindering the neutrophil infiltration, respectively. Collectively, these findings indicate that p-coumaric acid is a promising anti-inflammatory agent that can be used for developing a pharmaceutical drug for the treatment of ALI and other inflammatory disorders.
急性肺损伤(ALI)仍然是导致危重病患者死亡率高的原因。已知炎症是脂多糖(LPS)诱导的 ALI 发病机制中的关键因素,这使得它成为治疗 ALI 的一种相关方法。在这项研究中,我们通过体外和计算方法评估了鼻内滴注对羟基肉桂酸(p-coumaric acid)预防 LPS 诱导的 ALI 的潜力,评估其对炎症反应中涉及的细胞和分子靶标。我们的结果表明,对羟基肉桂酸可减少中性粒细胞的积累和促炎细胞因子的丰度,同时增加炎症部位的 IL-10 产生,这可能有助于预防 LPS 诱导的小鼠 ALI。在体外实验中,我们观察到对羟基肉桂酸对刺激的 A549 细胞中 IL-6 和 IL-8 产生以及中性粒细胞产生的活性氧具有抑制作用。此外,对羟基肉桂酸处理可减少 TNF-α 刺激的内皮细胞上的中性粒细胞粘附。根据计算预测,对羟基肉桂酸与 IKKβ 的 ATP 结合位点以及与 ICAM-1 相互作用的关键区域 LFA-1 内都达到了稳定的相互作用,从而抑制了促炎介质的产生并阻碍了中性粒细胞的浸润。总之,这些发现表明对羟基肉桂酸是一种有前途的抗炎剂,可用于开发治疗 ALI 和其他炎症性疾病的药物。