Zhao Xudong, Ren Zhichao, Cao Dingwen, Huang Yusen
State Key Laboratory Cultivation Base, Shandong Provincial Key Laboratory of Ophthalmology, Shandong Eye Institute, Shandong First Medical University and Shandong Academy of Medical Sciences Qingdao, Shandong, China.
Qingdao University, Qingdao Medical College Qingdao, Shandong, China.
Am J Transl Res. 2025 May 15;17(5):3307-3321. doi: 10.62347/IQUZ8416. eCollection 2025.
Herpes Simplex Keratitis (HSK) is a leading cause of infectious-related blindness, primarily driven by corneal inflammation and dysregulated immune response. Luteolin (LUT), a flavonoid with anti-inflammatory and antiviral properties, has the potential to target key signaling pathways and provide therapeutic benefits. This study aimed to investigate the mechanisms through which LUT alleviates HSK.
LUT's potential targets in HSK were identified using a systemic biology approach. Protein-Protein Interaction (PPI) analysis was performed to determine key hub genes. Molecular docking was used to assess LUT's binding affinity to PTGS2 and other key proteins. HSK mice were treated with LUT, and corneal opacity, edema, and thickness were then evaluated using slit-lamp microscopy and Optical Coherence Tomography. Inflammatory cytokine levels were quantified by quantitative Real-Time Polymerase Chain Reaction PCR (qRT-PCR), while PTGS2/NF-κB pathway activation, PTGS2 expression, and NF-κB phosphorylation levels were assessed by Western Blotting (WB).
LUT was found to regulate 30 HSK-related proteins, with AKT1, TNF, and PTGS2/NF-κB identified as key nodes. Furthermore, molecular docking confirmed a strong binding to PTGS2 (-9.7 kcal/mol). LUT treatment significantly reduced corneal opacity and edema, restoring corneal thickness to near-normal levels. RT-qPCR revealed downregulation of inflammatory cytokines, and WB analysis showed decreased PTGS2 expression and NF-κB phosphorylation, confirming LUT's role in attenuating corneal inflammation via inhibiting the PTGS2/NF-κB signaling pathway.
LUT alleviates HSK by modulating the PTGS2/NF-κB signaling pathway, reducing inflammation and corneal damage, and highlighting its therapeutic potential for ocular inflammatory diseases.
单纯疱疹病毒性角膜炎(HSK)是感染性致盲的主要原因,主要由角膜炎症和免疫反应失调所致。木犀草素(LUT)是一种具有抗炎和抗病毒特性的黄酮类化合物,有可能靶向关键信号通路并带来治疗益处。本研究旨在探究LUT减轻HSK的机制。
采用系统生物学方法确定LUT在HSK中的潜在靶点。进行蛋白质-蛋白质相互作用(PPI)分析以确定关键枢纽基因。利用分子对接评估LUT与PTGS2及其他关键蛋白的结合亲和力。用LUT治疗HSK小鼠,然后使用裂隙灯显微镜和光学相干断层扫描评估角膜混浊、水肿和厚度。通过定量实时聚合酶链反应PCR(qRT-PCR)定量炎症细胞因子水平,同时通过蛋白质印迹法(WB)评估PTGS2/NF-κB信号通路激活、PTGS2表达和NF-κB磷酸化水平。
发现LUT可调节30种与HSK相关的蛋白,其中AKT1、TNF和PTGS2/NF-κB被确定为关键节点。此外,分子对接证实LUT与PTGS2有很强的结合力(-9.7千卡/摩尔)。LUT治疗显著降低了角膜混浊和水肿,使角膜厚度恢复到接近正常水平。RT-qPCR显示炎症细胞因子下调,WB分析显示PTGS2表达和NF-κB磷酸化降低,证实LUT通过抑制PTGS2/NF-κB信号通路在减轻角膜炎症中发挥作用。
LUT通过调节PTGS2/NF-κB信号通路减轻HSK,减少炎症和角膜损伤,突出了其在眼部炎症性疾病中的治疗潜力。