Fu Xin-Xin, Duan Rui, Wang Si-Yu, Zhang Qiao-Quan, Wei Bin, Huang Ting, Gong Peng-Yu, Jiang Teng, Zhang Ying-Dong
School of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing, Jiangsu Province, China.
Department of Neurology, Nanjing First Hospital, Nanjing Medical University, Nanjing, Jiangsu Province, China.
Neural Regen Res. 2023 Jan;18(1):189-193. doi: 10.4103/1673-5374.343888.
Lamotrigine (LTG) is a widely used drug for the treatment of epilepsy. Emerging clinical evidence suggests that LTG may improve cognitive function in patients with Alzheimer's disease. However, the underlying molecular mechanisms remain unclear. In this study, amyloid precursor protein/presenilin 1 (APP/PS1) double transgenic mice were used as a model of Alzheimer's disease. Five-month-old APP/PS1 mice were intragastrically administered 30 mg/kg LTG or vehicle once per day for 3 successive months. The cognitive functions of animals were assessed using Morris water maze. Hyperphosphorylated tau and markers of synapse and glial cells were detected by western blot assay. The cell damage in the brain was investigated using hematoxylin and eosin staining. The levels of amyloid-β and the concentrations of interleukin-1β, interleukin-6 and tumor necrosis factor-α in the brain were measured using enzyme-linked immunosorbent assay. Differentially expressed genes in the brain after LTG treatment were analyzed by high-throughput RNA sequencing and real-time polymerase chain reaction. We found that LTG substantially improved spatial cognitive deficits of APP/PS1 mice; alleviated damage to synapses and nerve cells in the brain; and reduced amyloid-β levels, tau protein hyperphosphorylation, and inflammatory responses. High-throughput RNA sequencing revealed that the beneficial effects of LTG on Alzheimer's disease-related neuropathologies may have been mediated by the regulation of Ptgds, Cd74, Map3k1, Fosb, and Spp1 expression in the brain. These findings revealed potential molecular mechanisms by which LTG treatment improved Alzheimer's disease. Furthermore, these data indicate that LTG may be a promising therapeutic drug for Alzheimer's disease.
拉莫三嗪(LTG)是一种广泛用于治疗癫痫的药物。新出现的临床证据表明,LTG可能改善阿尔茨海默病患者的认知功能。然而,其潜在的分子机制仍不清楚。在本研究中,淀粉样前体蛋白/早老素1(APP/PS1)双转基因小鼠被用作阿尔茨海默病模型。对5月龄的APP/PS1小鼠连续3个月每天灌胃给予30 mg/kg LTG或赋形剂。使用莫里斯水迷宫评估动物的认知功能。通过蛋白质免疫印迹法检测过度磷酸化的tau蛋白以及突触和神经胶质细胞标志物。使用苏木精-伊红染色研究脑内细胞损伤。使用酶联免疫吸附测定法测量脑内β淀粉样蛋白水平以及白细胞介素-1β、白细胞介素-6和肿瘤坏死因子-α的浓度。通过高通量RNA测序和实时聚合酶链反应分析LTG治疗后脑中差异表达的基因。我们发现,LTG显著改善了APP/PS1小鼠的空间认知缺陷;减轻了脑内突触和神经细胞的损伤;并降低了β淀粉样蛋白水平、tau蛋白过度磷酸化和炎症反应。高通量RNA测序显示,LTG对阿尔茨海默病相关神经病理学的有益作用可能是通过调节脑中Ptgds、Cd74、Map3k1、Fosb和Spp1的表达来介导的。这些发现揭示了LTG治疗改善阿尔茨海默病的潜在分子机制。此外,这些数据表明LTG可能是一种有前景的阿尔茨海默病治疗药物。