Avila Amy M, Burnett Barrington G, Taye Addis A, Gabanella Francesca, Knight Melanie A, Hartenstein Parvana, Cizman Ziga, Di Prospero Nicholas A, Pellizzoni Livio, Fischbeck Kenneth H, Sumner Charlotte J
Neurogenetics Branch, National Institute of Neurological Disorders and Stroke (NINDS), NIH, Bethesda, MA 20892, USA.
J Clin Invest. 2007 Mar;117(3):659-71. doi: 10.1172/JCI29562. Epub 2007 Feb 22.
The inherited motor neuron disease spinal muscular atrophy (SMA) is caused by mutation of the telomeric survival motor neuron 1 (SMN1) gene with retention of the centromeric SMN2 gene. We sought to establish whether the potent and specific hydroxamic acid class of histone deacetylase (HDAC) inhibitors activates SMN2 gene expression in vivo and modulates the SMA disease phenotype when delivered after disease onset. Single intraperitoneal doses of 10 mg/kg trichostatin A (TSA) in nontransgenic and SMA model mice resulted in increased levels of acetylated H3 and H4 histones and modest increases in SMN gene expression. Repeated daily doses of TSA caused increases in both SMN2-derived transcript and SMN protein levels in neural tissues and muscle, which were associated with an improvement in small nuclear ribonucleoprotein (snRNP) assembly. When TSA was delivered daily beginning on P5, after the onset of weight loss and motor deficit, there was improved survival, attenuated weight loss, and enhanced motor behavior. Pathological analysis showed increased myofiber size and number and increased anterior horn cell size. These results indicate that the hydroxamic acid class of HDAC inhibitors activates SMN2 gene expression in vivo and has an ameliorating effect on the SMA disease phenotype when administered after disease onset.
遗传性运动神经元疾病脊髓性肌萎缩症(SMA)由端粒生存运动神经元1(SMN1)基因突变引起,同时保留着着丝粒SMN2基因。我们试图确定强效且特异的异羟肟酸类组蛋白去乙酰化酶(HDAC)抑制剂在疾病发作后给药时,是否能在体内激活SMN2基因表达并调节SMA疾病表型。在非转基因和SMA模型小鼠中单次腹腔注射10mg/kg曲古抑菌素A(TSA),导致组蛋白H3和H4乙酰化水平升高,SMN基因表达适度增加。每日重复给予TSA可使神经组织和肌肉中SMN2衍生转录本和SMN蛋白水平升高,这与小核核糖核蛋白(snRNP)组装的改善有关。当从出生后第5天开始每日给予TSA,即在体重减轻和运动功能障碍发作后给药时,可提高生存率、减轻体重减轻并增强运动行为。病理分析显示肌纤维大小和数量增加以及前角细胞大小增加。这些结果表明,异羟肟酸类HDAC抑制剂在体内可激活SMN2基因表达,并且在疾病发作后给药时对SMA疾病表型具有改善作用。