Department of Neurology, Neurological Institute, Graduate School of Medical Sciences, Kyushu University, Fukuoka, Japan.
Department of Geriatric Medicine and Neurology, Graduate School of Medicine, Ehime University, Ehime, Japan.
J Alzheimers Dis. 2017;58(4):1151-1161. doi: 10.3233/JAD-160344.
Apomorphine (APO) promotes intraneuronal amyloid-β (Aβ) degradation and improves memory function in an Alzheimer's disease (AD) model, 3xTg-AD mice. Since insulin resistance is increased in AD neurons, we investigated the effects of APO on brain insulin resistance in 3xTg-AD mice at early and late stages. After 1-month subcutaneous injection of Apokyn® to 3xTg-AD mice at 6 or 12 months of age, memory function was significantly improved in both age groups. Protein levels of insulin-degrading enzyme (IDE), which is linked to insulin signaling and degrades Aβ, significantly increased in the 3xTg-AD mice brain compared with non-transgenic mice, and were further increased by APO. Protein levels of two types of serine-phosphorylated insulin receptor substrate-1 (IRS-1), pS616 and pS636/639, significantly decreased following APO treatment in the 13-month-old 3xTg-AD mice brain, suggesting improved brain insulin resistance. Immunostaining of the IDE, pS616 and pS636/639 IRS-1 demonstrated similar changes due to APO treatment. Thus, brain insulin resistance is considered an important therapeutic target in AD, and APO may provide improved neuronal insulin resistance.
阿扑吗啡(APO)可促进脑内淀粉样β(Aβ)降解,并改善阿尔茨海默病(AD)模型,即 3xTg-AD 小鼠的记忆功能。由于 AD 神经元中的胰岛素抵抗增加,我们研究了 APO 对 6 个月和 12 个月龄的 3xTg-AD 小鼠早期和晚期大脑胰岛素抵抗的影响。经过 1 个月的皮下注射 Apokyn®,6 个月和 12 个月龄的 3xTg-AD 小鼠的记忆功能均显著改善。与非转基因小鼠相比,3xTg-AD 小鼠大脑中与胰岛素信号相关并降解 Aβ的胰岛素降解酶(IDE)蛋白水平显著增加,APO 进一步增加了其蛋白水平。在 13 个月龄的 3xTg-AD 小鼠大脑中,APO 处理后两种类型的丝氨酸磷酸化胰岛素受体底物-1(IRS-1),pS616 和 pS636/639 的蛋白水平显著降低,表明大脑胰岛素抵抗得到改善。由于 APO 处理,IDE、pS616 和 pS636/639 IRS-1 的免疫染色也显示出相似的变化。因此,大脑胰岛素抵抗被认为是 AD 的一个重要治疗靶点,APO 可能提供改善的神经元胰岛素抵抗。