Bjorkli Christiana, Hemler Mary, Julian Joshua B, Sandvig Axel, Sandvig Ioanna
Department of Neuromedicine and Movement Science, Faculty of Medicine and Health Sciences, Norwegian University of Science and Technology, Trondheim, Norway.
Department of Neurology, St. Olav's Hospital, Trondheim, Norway.
Front Pharmacol. 2022 Aug 16;13:913971. doi: 10.3389/fphar.2022.913971. eCollection 2022.
All drug trials completed to date have fallen short of meeting the clinical endpoint of significantly slowing cognitive decline in Alzheimer's disease (AD) patients. In this study, we repurposed two FDA-approved drugs, Fasudil and Lonafarnib, targeting synaptic formation (i.e., Wnt signaling) and cellular clearance (i.e., autophagic) pathways respectively, to test their therapeutic potential for attenuating AD-related pathology. We characterized our 3xTg AD mouse colony to select timepoints for separate and combinatorial treatment of both drugs while collecting cerebrospinal fluid (CSF) using an optimized microdialysis method. We found that treatment with Fasudil reduced Aβ at early and later stages of AD, whereas administration of Lonafarnib had no effect on Aβ, but did reduce tau, at early stages of the disease. Induction of autophagy led to increased size of amyloid plaques when administered at late phases of the disease. We show that combinatorial treatment with both drugs was effective at reducing intraneuronal Aβ and led to improved cognitive performance in mice. These findings lend support to regulating Wnt and autophagic pathways in order to attenuate AD-related pathology.
迄今为止完成的所有药物试验均未达到显著减缓阿尔茨海默病(AD)患者认知衰退这一临床终点。在本研究中,我们对两种已获美国食品药品监督管理局(FDA)批准的药物进行了重新利用,分别是法舒地尔和洛那法尼,它们分别靶向突触形成(即Wnt信号通路)和细胞清除(即自噬)途径,以测试它们减轻AD相关病理的治疗潜力。我们对我们的3xTg AD小鼠群体进行了特征分析,以选择两种药物单独和联合治疗的时间点,同时使用优化的微透析方法收集脑脊液(CSF)。我们发现,法舒地尔治疗在AD的早期和晚期均能降低Aβ水平,而洛那法尼给药对Aβ无影响,但在疾病早期确实能降低tau水平。在疾病晚期给予自噬诱导剂会导致淀粉样斑块尺寸增大。我们表明,两种药物联合治疗在降低神经元内Aβ方面有效,并能改善小鼠的认知表现。这些发现为调节Wnt和自噬途径以减轻AD相关病理提供了支持。