Du Li-da, Fang Cheng, Wang Yue-Qing, Feng Zi-Ying, Abiola Ogunleye Femi, Gao Zhao-Lin, Huang Ju-Yang, Ma Yin-Zhong
Institute of Molecular Medicine & Innovative Pharmaceutics, Qingdao University, Qingdao, 266071, China.
Provincial Laboratory of Polymorphic Medicine, Tengzhou, 277599, China.
Acta Pharmacol Sin. 2025 Mar 11. doi: 10.1038/s41401-025-01505-x.
The acute phase of ischemic stroke is marked by a surge in matrix metalloproteinase-9 (MMP-9) activity. While integral to natural repair processes, MMP-9 exacerbates injury by breaking down the blood-brain barrier (BBB) and promoting edema and inflammation. MMP-9 is predominantly secreted by inflammatory cells such as neutrophils, macrophages and microglia soon after stroke onset. In this study we investigated the effects of MMP-9 inhibition via SB-3CT on astrocytic lipid metabolism, and its potential to enhance neuronal survival and recovery following ischemic stroke. Mice were subjected to transient middle cerebral artery occlusion (tMCAO) for 60 min, mice then were injected with SB-3CT (25 mg/kg, i.v.). On D3 post tMCAO, neurological outcomes were assessed, and whole brains were collected for analysis. Lipidomic analysis of brain tissue showed that SB-3CT treatment significantly restrained astrocytic cholesterol metabolism by modulating the sphingolipid and glycerophospholipid pathways. Specifically, SB-3CT reduced ceramide accumulation and promoted an increase in neuroprotective hexosylceramides, leading to enhanced neuronal survival and synaptic integrity. In addition, SB-3CT treatment reduced astrocytic and microglial reactivity, thereby mitigating neuroinflammation. In order to optimize the timing and dosage of MMP-9 inhibition to maximize the therapeutic efficacy, tMCAO mice were given three injections of SB-3CT on D0, D2 and D4 within 7 days after modeling. We found that prolonged MMP-9 inhibition alleviated astrogliosis, concurrently impaired neurological recovery and inhibited angiogenesis. These results demonstrate the critical role of lipid metabolism in MMP-9-mediated brain injury and the potential of SB-3CT as a therapeutic strategy for ischemic stroke by targeting astrocytic lipid metabolism.
缺血性中风的急性期以基质金属蛋白酶-9(MMP-9)活性激增为特征。虽然MMP-9是自然修复过程所必需的,但它通过破坏血脑屏障(BBB)以及促进水肿和炎症反应而加重损伤。中风发作后不久,MMP-9主要由炎症细胞如中性粒细胞、巨噬细胞和小胶质细胞分泌。在本研究中,我们研究了通过SB-3CT抑制MMP-9对星形胶质细胞脂质代谢的影响,以及其增强缺血性中风后神经元存活和恢复的潜力。将小鼠进行短暂性大脑中动脉闭塞(tMCAO)60分钟,然后给小鼠注射SB-3CT(25mg/kg,静脉注射)。在tMCAO后第3天,评估神经功能结果,并收集全脑进行分析。脑组织的脂质组学分析表明,SB-3CT治疗通过调节鞘脂和甘油磷脂途径显著抑制星形胶质细胞胆固醇代谢。具体而言,SB-3CT减少了神经酰胺的积累,并促进了具有神经保护作用的己糖神经酰胺增加,从而提高了神经元的存活率和突触完整性。此外,SB-3CT治疗降低了星形胶质细胞和小胶质细胞的反应性,从而减轻了神经炎症。为了优化MMP-9抑制的时间和剂量以最大化治疗效果,在建模后7天内于第0、2和4天给tMCAO小鼠注射三次SB-3CT。我们发现,延长MMP-9抑制可减轻星形胶质细胞增生,同时损害神经功能恢复并抑制血管生成。这些结果证明了脂质代谢在MMP-9介导的脑损伤中的关键作用,以及SB-3CT作为通过靶向星形胶质细胞脂质代谢治疗缺血性中风的潜在策略。