Zhang Feng, Sun Mengya, Ma Shiyi, Sun Junfang, Li Yishi, Li Xianghong, Jiang Hong
Department of Pediatrics, The Affiliated Hospital of Qingdao University, Qingdao, Shandong, People's Republic of China.
Animal Experiment Center, Central Laboratory, The Affiliated Hospital of Qingdao University, Qingdao, Shandong, China.
Phytother Res. 2025 Sep;39(9):4060-4080. doi: 10.1002/ptr.70052. Epub 2025 Jul 27.
Neuronal development in newborns is often constrained by perinatal inflammation, with limited research available on the pathogenesis and treatment strategies for this condition. This study aimed to investigate the neuroprotective effects of Embelin in mitigating perinatal inflammation-induced neuronal development limitations by targeting 5-lipoxygenase (5-LOX) and reducing oxidative stress and ferroptosis. This study utilized in vivo and in vitro inflammation models to assess the therapeutic potential of Embelin, a small molecule drug from the FDA compound library. Using Autodock software and surface plasmon resonance detection technology, 5-LOX was identified as the molecular target of Embelin. Neuronal ferroptosis and oxidative stress were analyzed in rat models and PC12 cells treated with lipopolysaccharide (LPS) and Embelin. Biochemical assays, immunofluorescence staining, and western blotting were performed to quantify protein expression and oxidative stress markers. Embelin, along with the 5-LOX inhibitor Zileuton and 5-LOX mRNA silencing, significantly inhibited 5-LOX expression in neurons. Conversely, overexpressed 5-LOX promoted ferroptosis, and this effect could be inhibited by Embelin. These interventions reduced oxidative stress, suppressed ferroptosis, and promoted normal neuronal development in the cerebral cortex and hippocampus. The findings highlight Embelin's ability to specifically target and mitigate 5-LOX-induced ferroptosis, facilitating recovery from perinatal inflammation-induced neurodevelopmental deficits. Embelin demonstrates significant neuroprotective potential by inhibiting 5-LOX-mediated ferroptosis and oxidative stress, offering a promising therapeutic strategy for perinatal brain injury and related neurodevelopmental disorders.
新生儿的神经元发育常常受到围产期炎症的限制,而关于这种情况的发病机制和治疗策略的研究有限。本研究旨在探讨恩贝林通过靶向5-脂氧合酶(5-LOX)、减轻氧化应激和铁死亡来减轻围产期炎症诱导的神经元发育受限的神经保护作用。本研究利用体内和体外炎症模型来评估恩贝林(一种来自FDA化合物库的小分子药物)的治疗潜力。使用Autodock软件和表面等离子体共振检测技术,确定5-LOX为恩贝林的分子靶点。在脂多糖(LPS)和恩贝林处理的大鼠模型和PC12细胞中分析神经元铁死亡和氧化应激。进行生化测定、免疫荧光染色和蛋白质印迹以量化蛋白质表达和氧化应激标志物。恩贝林与5-LOX抑制剂齐留通以及5-LOX mRNA沉默一起,显著抑制神经元中5-LOX的表达。相反,过表达的5-LOX促进铁死亡,而这种作用可被恩贝林抑制。这些干预措施减少了氧化应激,抑制了铁死亡,并促进了大脑皮层和海马体中神经元的正常发育。这些发现突出了恩贝林特异性靶向和减轻5-LOX诱导的铁死亡的能力,有助于从围产期炎症诱导的神经发育缺陷中恢复。恩贝林通过抑制5-LOX介导的铁死亡和氧化应激显示出显著的神经保护潜力,为围产期脑损伤和相关神经发育障碍提供了一种有前景的治疗策略。