Gao Jimeng, Liu Yu, Li Ruicheng, Liu Yuecen, Qi Zhongquan, Zhang Zhengmian
Medical College of Guangxi University, Da-Xue-Dong Road No.100, Nanning, Guangxi, 530004, China.
Institute of Regulatory Science for Medical Devices, SCU, 610065, China.
Eur J Pharmacol. 2025 Sep 5;1002:177816. doi: 10.1016/j.ejphar.2025.177816. Epub 2025 Jun 7.
Spinal cord injury (SCI) is a highly disabling condition affecting the central nervous system (CNS). In the context of secondary SCI, microglial pyroptosis exerts a profound influence on neurological recovery. A novel lipophilic unsaturated fatty acid derivative from Isatis indigotica, DCAAA, has been synthesized and its structure and toxicity were evaluated. Through extensive in vivo and in vitro studies, this study explored the therapeutic potential and underlying molecular mechanisms of DCAAA. Treatment with DCAAA markedly attenuated oxidative stress following SCI and suppressed the expression of pyroptosis-associated proteins NLRP3, GSDMD, ASC, and Caspase-1, along with pro-inflammatory cytokines IL-1β and IL-18. Histological analyses, including HE, Nissl, and Masson staining, alongside Basso-Beattie-Bresnahan (BBB) scoring and footprint analysis, demonstrated that DCAAA facilitated axonal regeneration and improved motor function post-SCI. In vitro experiments, simulating pyroptosis through lipopolysaccharide (LPS) and adenosine triphosphate (ATP) exposure, yielded findings consistent with those observed in vivo. DCAAA significantly mitigated BV2 cell activation and oxidative stress following stimulation, while inhibiting the expression of pyroptosis-related proteins and pro-inflammatory cytokines. In conclusion, DCAAA reduces microglial pyroptosis following SCI by targeting the PI3K/AKT/NF-κB and NLRP3/caspase-1/GSDMD pathways, thereby promoting axonal regeneration and enhancing motor function recovery.
脊髓损伤(SCI)是一种影响中枢神经系统(CNS)的高度致残性疾病。在继发性SCI的背景下,小胶质细胞焦亡对神经功能恢复产生深远影响。已合成了一种来自菘蓝的新型亲脂性不饱和脂肪酸衍生物DCAAA,并对其结构和毒性进行了评估。通过广泛的体内和体外研究,本研究探讨了DCAAA的治疗潜力和潜在分子机制。DCAAA治疗显著减轻了SCI后的氧化应激,并抑制了焦亡相关蛋白NLRP3、GSDMD、ASC和Caspase-1以及促炎细胞因子IL-1β和IL-18的表达。包括苏木精-伊红(HE)、尼氏和Masson染色在内的组织学分析,以及Basso-Beattie-Bresnahan(BBB)评分和足迹分析表明,DCAAA促进了SCI后轴突再生并改善了运动功能。在体外实验中,通过暴露于脂多糖(LPS)和三磷酸腺苷(ATP)模拟焦亡,得到的结果与体内观察到的结果一致。DCAAA显著减轻了刺激后BV2细胞的活化和氧化应激,同时抑制了焦亡相关蛋白和促炎细胞因子的表达。总之,DCAAA通过靶向PI3K/AKT/NF-κB和NLRP3/caspase-1/GSDMD途径减少SCI后的小胶质细胞焦亡,从而促进轴突再生并增强运动功能恢复。