Center for Translational Medicine, Department of Pharmacology, Temple University School of Medicine, Philadelphia, PA 19140, USA.
Aging Cell. 2013 Aug;12(4):706-11. doi: 10.1111/acel.12096. Epub 2013 Jun 11.
Emerging evidence suggests that dysregulation stress hormones, such as glucocorticoids, in aged persons put them at a higher risk to develop Alzheimer's disease (AD). However, the mechanisms underlying such vulnerability remain to be unraveled. Pharmacologic inhibition of 5-lipoxygenase (5LO), an active player in AD pathogenesis whose protein level increases with aging in the human, has been shown to blunt glucocorticoid-mediated amyloid β (Ab) formation in vitro. In this article, we investigated the role of this pathway in modulating the development of the corticosteroid-dependent AD-like phenotype in the triple transgenic mice (3xTg). Dexamethasone was administered for 1 week to 3xTg or 3xTg genetically deficient for 5LO (3xTg/5LO-/-) mice, and its effect on memory, amyloid-β and tau levels, and metabolism assessed. At the end of the treatment, we observed that dexamethasone did not induce changes in behavior. Compared with controls, treated mice did not show significant alterations in brain soluble Aβ levels. While total tau protein levels were unmodified in all groups, we found that dexamethasone significantly increased tau phosphorylation at S396, as recognized by the antibody PHF-13, which was specifically associated with an increase in the GSK3β activity. Additionally, dexamethasone-treated mice had a significant increase in the tau insoluble fraction and reduction in the postsynaptic protein PDS-95. By contrast, these modifications were blunted in the 3xTg/5LO-/- mice. Our findings highlight the functional role that 5LO plays in stress-induced AD tau pathology and support the hypothesis that pharmacologic inhibition of this enzyme could be a useful tool for individuals with this risk factor.
新出现的证据表明,调节应激激素(如糖皮质激素)的异常会使老年人更容易患上阿尔茨海默病(AD)。然而,这种脆弱性的机制仍有待阐明。在体外研究中,5-脂氧合酶(5LO)的药理学抑制作用已被证明可以阻止糖皮质激素介导的淀粉样β(Ab)形成,5LO 是 AD 发病机制中的一个活跃参与者,其蛋白水平会随着人类年龄的增长而增加。在本文中,我们研究了该途径在调节三重转基因小鼠(3xTg)中糖皮质激素依赖性 AD 样表型发展中的作用。用地塞米松处理 3xTg 或 5LO 基因缺失的 3xTg(3xTg/5LO-/-)小鼠 1 周,并评估其对记忆、淀粉样蛋白-β和 tau 水平以及代谢的影响。在治疗结束时,我们观察到地塞米松不会引起行为变化。与对照组相比,治疗组小鼠脑中可溶性 Aβ水平没有明显变化。虽然各组总 tau 蛋白水平没有改变,但我们发现地塞米松显著增加了 PHF-13 抗体识别的 S396 处 tau 的磷酸化,这与 GSK3β 活性的增加有关。此外,地塞米松处理的小鼠 tau 不溶性部分显著增加,突触后蛋白 PDS-95 减少。相比之下,这些改变在 3xTg/5LO-/-小鼠中被减弱。我们的研究结果强调了 5LO 在应激诱导的 AD tau 病理学中发挥的功能作用,并支持了药理学抑制该酶可能是具有这种风险因素的个体的有用工具的假说。