Barik Anirban, Bhoga Dipakkumar, Dhingra Tannu, Karmarkar Gautam, Ghosh Bijoyani, Malik Nikita, Parmar Krupanshu, Datta Aishika, Borah Anupom, Bhattacharya Pallab
Department of Pharmacology and Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Gandhinagar-382355, Ahmedabad, Gujarat, India.
Cellular and Molecular Neurobiology Laboratory, Department of Life Science and Bioinformatics, Assam University, Silchar, 788011, Assam, India.
Neurochem Res. 2025 Apr 25;50(3):151. doi: 10.1007/s11064-025-04403-0.
The progressive brain damage following ischemic stroke is primarily due to oxidative stress and activation of inflammatory pathways. Post-stroke neurodegeneration can lead to the loss of neurons and glial cells, including oligodendrocytes, contributing to demyelination. Following ischemic stroke, reperfusion results in increased intracellular calcium, generation of free radicals, and inflammation culminating in accumulation of misfolded proteins in the endoplasmic reticulum (ER) lumen augmenting the ER stress. ER stress has been shown to aggravate post-stroke neurodegeneration by triggering neuronal apoptosis and also contributing towards demyelination of neurons. To address the limitations of current stroke therapies, repurposing of drugs as future adjunctive therapy may be promising. Clemastine, an antihistaminic drug, improves post stroke outcome as evident in the present study. Male Sprague Dawley (SD) rats were treated with clemastine following ischemic stroke. Harvested brain tissues were subjected to different biochemical assays, molecular assays, and histopathological analysis. Clemastine was able to reduce infarct size, alleviate oxidative stress, improve neuronal count, and functional outcomes. Clemastine downregulated genes and proteins responsible for ER stress, apoptosis and demyelination as shown by the western blot and qPCR results. Our study suggests that clemastine may alleviate endoplasmic reticulum stress-mediated demyelination by modulating PERK/ATF4/CHOP axis, and may be used as one of the adjunctive therapies for stroke in future.
缺血性中风后进行性脑损伤主要归因于氧化应激和炎症通路的激活。中风后神经退行性变可导致神经元和神经胶质细胞(包括少突胶质细胞)的丢失,从而导致脱髓鞘。缺血性中风后,再灌注导致细胞内钙增加、自由基生成和炎症,最终导致内质网(ER)腔内错误折叠蛋白的积累,加剧内质网应激。内质网应激已被证明可通过触发神经元凋亡以及导致神经元脱髓鞘来加重中风后神经退行性变。为了解决当前中风治疗的局限性,将药物重新用作未来的辅助治疗可能很有前景。如本研究所示,抗组胺药氯马斯汀可改善中风后的预后。雄性Sprague Dawley(SD)大鼠在缺血性中风后接受氯马斯汀治疗。对收获的脑组织进行不同的生化分析、分子分析和组织病理学分析。氯马斯汀能够减小梗死面积、减轻氧化应激、改善神经元数量和功能结局。蛋白质免疫印迹和定量聚合酶链反应结果显示,氯马斯汀下调了负责内质网应激、细胞凋亡和脱髓鞘的基因和蛋白质。我们的研究表明,氯马斯汀可能通过调节PERK/ATF4/CHOP轴来减轻内质网应激介导的脱髓鞘,未来可用作中风的辅助治疗方法之一。