Laboratory of Molecular Neuropharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka 565-0871, Japan.
Laboratory of Molecular Neuropharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka 565-0871, Japan; Laboratory of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka 565-0871, Japan.
Pharmacol Biochem Behav. 2019 Jan;176:1-5. doi: 10.1016/j.pbb.2018.11.003. Epub 2018 Nov 9.
Growing evidence suggests pivotal roles for epigenetic mechanisms in both animal models of and individuals with autism spectrum disorders (ASD). Neuron-restrictive silencer factor (NRSF) binds to neuron-restrictive silencing elements in neuronal genes and recruits co-repressors, such as mSin3, to epigenetically inhibit neuronal gene expression. Because dysregulation of NRSF is related to ASD, here we examined the effects of mS-11, a chemically optimized mimetic of the mSin3-binding helix in NRSF, on the behavioral and morphological abnormalities found in a mouse model of valproic acid (VPA)-induced ASD. Chronic treatment with mS-11 improved prenatal VPA-induced deficits in social interaction. Additionally, we found that NRSF mRNA expression was greater in the somatosensory cortex of VPA-exposed mice than of controls. Agreeing with these behavioral findings, mice that were prenatally exposed to VPA showed lower dendritic spine density in the somatosensory cortex, which was reversed by chronic treatment with mS-11. These findings suggest that mS-11 has the potential for improving ASD-related symptoms through inhibition of mSin3-NRSF binding.
越来越多的证据表明,表观遗传机制在自闭症谱系障碍(ASD)的动物模型和个体中都起着关键作用。神经元限制沉默因子(NRSF)与神经元基因中的神经元限制沉默元件结合,并募集共抑制因子,如 mSin3,从而表观遗传抑制神经元基因表达。由于 NRSF 的失调与 ASD 有关,因此我们在这里研究了 mS-11(NRSF 中 mSin3 结合螺旋的化学优化模拟物)对丙戊酸(VPA)诱导的 ASD 小鼠模型中发现的行为和形态异常的影响。慢性 mS-11 治疗可改善产前 VPA 诱导的社交互动缺陷。此外,我们发现 VPA 暴露的小鼠体感皮层中的 NRSF mRNA 表达高于对照组。与这些行为发现一致,产前暴露于 VPA 的小鼠在体感皮层中的树突棘密度较低,而慢性 mS-11 治疗可逆转这种情况。这些发现表明,mS-11 通过抑制 mSin3-NRSF 结合,有可能改善与 ASD 相关的症状。