槲皮素作为抗炎抗氧化剂的分子对接分析。
and Molecular Docking Analysis of Quercetin as an Anti-inflammatory and Antioxidant.
机构信息
Department of Clinical Biochemistry, Faculty of Medicine, Bushehr University of Medical Sciences, Bushehr, Iran.
Clinical Research Development Center, "The Persian Gulf Martyrs" Hospital, Bushehr University of Medical Sciences, Bushehr, Iran.
出版信息
Curr Pharm Des. 2023;29(11):883-891. doi: 10.2174/1381612829666230330084043.
INTRODUCTION
Quercetin (3,3',4',5,7-pentahydroxyflavone) is a dietary flavonoid with good antioxidant and anti-inflammatory properties.
AIMS
The present study aims to determine these effects in peripheral blood mononuclear cells (PBMCs) evoked by lipopolysaccharides (LPS).
METHODS
The mRNA expression and protein secretion of inflammatory mediators were evaluated by enzyme- linked immunosorbent assay (ELISA) and quantitative real-time polymerase chain reaction (PCR), respectively. Western blotting was utilized for assessing p65-NF-κB phosphorylation. Ransod kits evaluated the glutathione peroxidase (GPx) and superoxide dismutase (SOD) activity in the cell lysates. Ultimately, the molecular docking approach was performed to investigate the biological activity of Quercetin against NF-κB pathway proteins and antioxidant enzymes.
RESULTS
The findings revealed that quercetin significantly attenuated the expression and secretion of inflammatory mediators and p65-NF-κB phosphorylation in LPS-induced PBMCs. Additionally, quercetin dose-dependently improved the activities of SOD and GPx enzymes and decreased LPS-mediated oxidative stress in PBMCs. Moreover, quercetin has a considerable binding affinity to IκKb, the core element of the NF-κB pathway and the antioxidant enzyme SOD.
CONCLUSION
The data show that quercetin plays a vital role in ameliorating inflammation and oxidative stress caused by LPS in PBMCs.
简介
槲皮素（3,3',4',5,7-五羟基黄酮）是一种具有良好抗氧化和抗炎特性的膳食类黄酮。
目的
本研究旨在确定其对脂多糖（LPS）诱导的外周血单个核细胞（PBMC）的这些作用。
方法
通过酶联免疫吸附试验（ELISA）和实时定量聚合酶链反应（PCR）分别评估炎症介质的 mRNA 表达和蛋白分泌。采用 Western blot 法评估 p65-NF-κB 磷酸化。Ransod 试剂盒评估细胞裂解物中谷胱甘肽过氧化物酶（GPx）和超氧化物歧化酶（SOD）的活性。最终，采用分子对接方法研究槲皮素对 NF-κB 通路蛋白和抗氧化酶的生物学活性。
结果
结果表明，槲皮素可显著抑制 LPS 诱导的 PBMC 中炎症介质的表达和分泌以及 p65-NF-κB 磷酸化。此外，槲皮素呈剂量依赖性地提高了 SOD 和 GPx 酶的活性，并降低了 LPS 介导的 PBMC 中的氧化应激。此外，槲皮素与 NF-κB 通路的核心元件 IκKb 和抗氧化酶 SOD 具有相当大的结合亲和力。
结论
数据表明，槲皮素在改善 LPS 诱导的 PBMC 炎症和氧化应激中起着重要作用。
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