Mandel Silvia A, Sagi Yotam, Amit Tamar
Eve Topf Center of Excellence for Neurodegenerative Diseases Research, Department of Pharmacology, Technion-Rappaport Faculty of Medicine, P.O. Box 9697, Haifa, 31096, Israel.
Neurochem Res. 2007 Oct;32(10):1694-9. doi: 10.1007/s11064-007-9351-8. Epub 2007 Aug 16.
The anti-Parkinson drug rasagiline (Azilect), an irreversible and selective monoamine oxidase (MAO)-B inhibitor, was shown to possess neuroprotective activities, involving multiple survival pathways among them the up-regulation of protein kinase C (PKC)alpha, PKCepsilon, the anti-apoptotic Bcl-2, Bcl-xL, and Bcl-w and the induction of brain-derived- and glial cell line-derived neurotrophic factors (BDNF, GDNF). More recently, employing conventional neurochemical techniques, as well as transcriptomic and proteomic screening tools, combined with a biology-based clustering method, it was shown that rasagiline also possesses neurorescue/neurogenesis activity in mice midbrain dopaminergic neurons when given chronically, post-MPTP (N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine). This action was attributed to the activation of cell signaling mediators associated with neurotrophic factors responsive-tyrosine kinase receptor (Trk) pathway, including ShcC, SOS, AF6, Rin1, and Ras and the increase in the Trk-downstream effecter phosphatidylinositol 3 kinase (PI3K) protein and its substrate, Akt/PKB. It is interesting to determine whether a similar effect is seen in Parkinsonian patients after long-term treatment with rasagiline, which may have implications as a possible disease modifying agent.
抗帕金森病药物雷沙吉兰(Azilect)是一种不可逆的选择性单胺氧化酶(MAO)-B抑制剂,已被证明具有神经保护活性,涉及多种生存途径,其中包括蛋白激酶C(PKC)α、PKCε、抗凋亡蛋白Bcl-2、Bcl-xL和Bcl-w的上调,以及脑源性神经营养因子和胶质细胞源性神经营养因子(BDNF、GDNF)的诱导。最近,采用传统神经化学技术以及转录组学和蛋白质组学筛选工具,并结合基于生物学的聚类方法,研究表明,在给予MPTP(N-甲基-4-苯基-1,2,3,6-四氢吡啶)后长期给药时,雷沙吉兰在小鼠中脑多巴胺能神经元中也具有神经挽救/神经发生活性。这种作用归因于与神经营养因子反应性酪氨酸激酶受体(Trk)途径相关的细胞信号介质的激活,包括ShcC、SOS、AF6、Rin1和Ras,以及Trk下游效应器磷脂酰肌醇3激酶(PI3K)蛋白及其底物Akt/PKB的增加。确定长期使用雷沙吉兰治疗帕金森病患者是否会出现类似效果很有意思,这可能意味着它是一种可能的疾病修饰剂。