Dall'Igna Oscar P, Bobermin Larissa D, Souza Diogo O, Quincozes-Santos André
Rua Ramiro Barcelos 2600-Anexo, Departamento de Bioquímica, Universidade Federal do Rio Grande do Sul, Porto Alegre, CEP 90035-000, Brazil.
Int J Dev Neurosci. 2013 Nov;31(7):482-6. doi: 10.1016/j.ijdevneu.2013.06.002. Epub 2013 Jun 15.
Riluzole is a drug approved for the treatment of amyotrophic lateral sclerosis (ALS) and may be effective for the treatment of other neurodegenerative and neuropsychiatric disorders. Riluzole exerts diverse actions on the central nervous system, including altering glutamate release and uptake, and therefore act diminishing glutamate extracellular levels, but the underlying mechanism of these actions is still unknown. Here, we demonstrate that riluzole stimulated glutamate uptake and augmented the expression of the glutamate EAAC1 transporter in C6 astroglial cell cultures. The effect of riluzole on glutamate uptake was reduced to below controls when it was co-administered with inhibitors of protein kinase C (PKC; bisindolylmaleimide II), phosphatidylinositol 3-kinase (PI3K; wortmannin) and fibroblast growth factor receptor 1 (FGFR1; PD173074). Riluzole also decreased reactive oxygen species load with no effect on glutathione levels. This study investigates three independent intracellular pathways and the mechanism of action of riluzole on glutamate metabolism.
利鲁唑是一种被批准用于治疗肌萎缩侧索硬化症(ALS)的药物,可能对治疗其他神经退行性疾病和神经精神疾病有效。利鲁唑对中枢神经系统有多种作用,包括改变谷氨酸的释放和摄取,从而降低细胞外谷氨酸水平,但其这些作用的潜在机制仍不清楚。在此,我们证明利鲁唑刺激谷氨酸摄取并增强C6星形胶质细胞培养物中谷氨酸EAAC1转运体的表达。当利鲁唑与蛋白激酶C(PKC;双吲哚马来酰亚胺II)、磷脂酰肌醇3激酶(PI3K;渥曼青霉素)和成纤维细胞生长因子受体1(FGFR1;PD173074)的抑制剂共同给药时,其对谷氨酸摄取的作用降低至对照组以下。利鲁唑还降低了活性氧负荷,对谷胱甘肽水平无影响。本研究探讨了三个独立的细胞内途径以及利鲁唑对谷氨酸代谢的作用机制。