Section on Molecular Neurobiology, National Institute of Mental Health, National Institutes of Health, Bethesda, MD 20892-1363, USA.
Neuropsychopharmacology. 2011 Nov;36(12):2406-21. doi: 10.1038/npp.2011.128. Epub 2011 Jul 27.
Emerging evidence suggests that the mood stabilizers lithium and valproate (VPA) have broad neuroprotective and neurotrophic properties, and that these occur via inhibition of glycogen synthase kinase 3 (GSK-3) and histone deacetylases (HDACs), respectively. Huntington's disease (HD) is an inherited neurodegenerative disorder characterized by impaired movement, cognitive and psychiatric disturbances, and premature death. We treated N171-82Q and YAC128 mice, two mouse models of HD varying in genetic backgrounds and pathological progressions, with a diet containing therapeutic doses of lithium, VPA, or both. Untreated, these transgenic mice displayed a decrease in levels of GSK-3β serine 9 phosphorylation and histone H3 acetylation in the striatum and cerebral cortex around the onset of behavioral deficits, indicating a hyperactivity of GSK-3β and HDACs. Using multiple well-validated behavioral tests, we found that co-treatment with lithium and VPA more effectively alleviated spontaneous locomotor deficits and depressive-like behaviors in both models of HD mice. Furthermore, compared with monotherapy with either drug alone, co-treatment more successfully improved motor skill learning and coordination in N171-82Q mice, and suppressed anxiety-like behaviors in YAC128 mice. This combined treatment consistently inhibited GSK-3β and HDACs, and caused a sustained elevation in striatal as well as cortical brain-derived neurotrophic factor and heat shock protein 70. Importantly, co-treatment markedly prolonged median survival of N171-82Q mice from 31.6 to 41.6 weeks. Given that there is presently no proven treatment for HD, our results suggest that combined treatment with lithium and VPA, two mood stabilizers with a long history of safe use in humans, may have important therapeutic potential for HD patients.
新出现的证据表明,心境稳定剂锂和丙戊酸(VPA)具有广泛的神经保护和神经营养特性,分别通过抑制糖原合酶激酶 3(GSK-3)和组蛋白去乙酰化酶(HDACs)实现。亨廷顿病(HD)是一种遗传性神经退行性疾病,其特征为运动障碍、认知和精神障碍以及过早死亡。我们用含有治疗剂量锂、VPA 或两者的饮食治疗 N171-82Q 和 YAC128 两种不同遗传背景和病理进展的 HD 小鼠模型。未经治疗,这些转基因小鼠在行为缺陷出现之前,纹状体和大脑皮层中的 GSK-3β丝氨酸 9 磷酸化和组蛋白 H3 乙酰化水平下降,表明 GSK-3β和 HDACs 过度活跃。使用多种经过充分验证的行为测试,我们发现锂和 VPA 的联合治疗更有效地缓解了两种 HD 小鼠模型的自发运动缺陷和抑郁样行为。此外,与单独使用一种药物的单药治疗相比,联合治疗更成功地改善了 N171-82Q 小鼠的运动技能学习和协调能力,并抑制了 YAC128 小鼠的焦虑样行为。这种联合治疗一致地抑制了 GSK-3β和 HDACs,并持续升高纹状体和皮质脑源性神经营养因子和热休克蛋白 70。重要的是,联合治疗将 N171-82Q 小鼠的中位寿命从 31.6 周延长至 41.6 周。鉴于目前尚无针对 HD 的有效治疗方法,我们的结果表明,锂和 VPA 这两种心境稳定剂联合治疗,具有在人类中安全使用的悠久历史,对 HD 患者可能具有重要的治疗潜力。