Institute of Organic Chemistry and Biochemistry, AS CR, Prague, Czech Republic.
Université Lille, INSERM, CHU Lille, UMR - S 1172 - Jean Pierre Aubert Research Centre, Alzheimer and Tauopathies, Lille, France.
J Alzheimers Dis. 2019;67(4):1187-1200. doi: 10.3233/JAD-180837.
Alzheimer's disease (AD) is one of the most prevalent neurodegenerative diseases, characterized by the accumulation of extracellular amyloid plaques and intraneuronal neurofibrillary tangles. These tangles mainly consist of hyperphosphorylated tau protein. As it induces tau hyperphosphorylation in vitro and in vivo, hypothermia is a useful tool for screening potential neuroprotective compounds that ameliorate tau pathology. In this study, we examined the effect of prolactin-releasing peptide (PrRP), its lipidized analog palm11-PrRP31 and glucagon-like-peptide-1 agonist liraglutide, substances with anorexigenic and antidiabetic properties, on tau phosphorylation and on the main kinases and phosphatases involved in AD development. Our study was conducted in a neuroblastoma cell line SH-SY5Y and rat primary neuronal cultures under normothermic and hypothermic conditions. Hypothermia induced a significant increase in tau phosphorylation at the pThr212 and pSer396/pSer404 epitopes. The palmitoylated analogs liraglutide and palm11-PrRP31 attenuated tau hyperphosphorylation, suggesting their potential use in the treatment of neurodegenerative diseases.
阿尔茨海默病(AD)是最常见的神经退行性疾病之一,其特征是细胞外淀粉样斑块和神经元内神经原纤维缠结的积累。这些缠结主要由过度磷酸化的 tau 蛋白组成。由于低温在体外和体内诱导 tau 过度磷酸化,因此它是筛选潜在神经保护化合物以改善 tau 病理学的有用工具。在这项研究中,我们研究了促泌乳素释放肽(PrRP)、其脂质化类似物棕榈酰化 11-PrRP31 和胰高血糖素样肽-1 激动剂利拉鲁肽对 tau 磷酸化以及 AD 发展中涉及的主要激酶和磷酸酶的影响,这些物质具有厌食和抗糖尿病的特性。我们的研究在正常温度和低温条件下在神经母细胞瘤细胞系 SH-SY5Y 和大鼠原代神经元培养物中进行。低温诱导 tau 在 pThr212 和 pSer396/pSer404 表位的磷酸化显著增加。棕榈酰化类似物利拉鲁肽和棕榈酰化 11-PrRP31 减轻了 tau 的过度磷酸化,表明它们在治疗神经退行性疾病方面具有潜在的用途。