INSERM/UEVE, UMR 861, Université Paris Saclay, I-STEM, AFM-Telethon, Rue Henri Desbruères, 91100, Corbeil-Essonnes, France.
Department of Neuroscience "Rita Levi Montalcini", Neuroscience Institute Cavalieri Ottolenghi, University of Turin, Regione Gonzole 10, Orbassano, 10043, Turin, TO, Italy.
Cell Mol Life Sci. 2022 Jul 22;79(8):441. doi: 10.1007/s00018-022-04450-8.
Spinal muscular atrophy (SMA) is a genetic disease resulting in the loss of α-motoneurons followed by muscle atrophy. It is caused by knock-out mutations in the survival of motor neuron 1 (SMN1) gene, which has an unaffected, but due to preferential exon 7 skipping, only partially functional human-specific SMN2 copy. We previously described a Drosophila-based screening of FDA-approved drugs that led us to discover moxifloxacin. We showed its positive effect on the SMN2 exon 7 splicing in SMA patient-derived skin cells and its ability to increase the SMN protein level. Here, we focus on moxifloxacin's therapeutic potential in additional SMA cellular and animal models. We demonstrate that moxifloxacin rescues the SMA-related molecular and phenotypical defects in muscle cells and motoneurons by improving the SMN2 splicing. The consequent increase of SMN levels was higher than in case of risdiplam, a potent exon 7 splicing modifier, and exceeded the threshold necessary for a survival improvement. We also demonstrate that daily subcutaneous injections of moxifloxacin in a severe SMA murine model reduces its characteristic neuroinflammation and increases the SMN levels in various tissues, leading to improved motor skills and extended lifespan. We show that moxifloxacin, originally used as an antibiotic, can be potentially repositioned for the SMA treatment.
脊髓性肌萎缩症(SMA)是一种遗传性疾病,导致α运动神经元丧失,随后肌肉萎缩。它是由运动神经元生存 1(SMN1)基因的敲除突变引起的,该基因有一个未受影响的,但由于优先外显子 7 跳跃,只有部分功能的人类特异性 SMN2 拷贝。我们之前描述了一种基于果蝇的 FDA 批准药物筛选,该筛选导致我们发现了莫西沙星。我们表明它对 SMA 患者来源的皮肤细胞中 SMN2 外显子 7 剪接具有积极作用,并能够增加 SMN 蛋白水平。在这里,我们专注于莫西沙星在其他 SMA 细胞和动物模型中的治疗潜力。我们证明莫西沙星通过改善 SMN2 剪接来挽救肌肉细胞和运动神经元中的 SMA 相关分子和表型缺陷。随后 SMN 水平的增加高于强效外显子 7 剪接修饰剂利司扑兰,并且超过了生存改善所需的阈值。我们还证明,在严重的 SMA 小鼠模型中,每日皮下注射莫西沙星可减少其特征性神经炎症,并增加各种组织中的 SMN 水平,从而提高运动技能并延长寿命。我们表明,最初用作抗生素的莫西沙星可能被重新用于 SMA 的治疗。