Weinreb Orly, Bar-Am Orit, Amit Tamar, Chillag-Talmor Orly, Youdim Moussa B H
Eve Topf and Rappaport Family Research Institute, Technion-Faculty of Medicine, Haifa, Israel.
FASEB J. 2004 Sep;18(12):1471-3. doi: 10.1096/fj.04-1916fje. Epub 2004 Jul 9.
This study provides new insights into neuroprotection involving interaction of protein kinase C (PKC) pathway with Bcl-2 family proteins. Using a model of serum deprivation, we investigated the mechanism by which the anti-Parkinson/monoamine oxidase (MAO)-B inhibitor drug, rasagiline, exerts its neuroprotective effect in rat pheochromocytoma PC12 cells. Here, we report that rasagiline (0.1-10 microM) decreased apoptosis via multiple protection mechanisms, including the stimulation of PKC phosphorylation; up-regulation of PKCalpha and PKC mRNAs, induction of Bcl-xL, Bcl-w, and brain-derived neurotrophic factor (BDNF) mRNAs; and down-regulation of Bad and Bax mRNAs. Moreover, rasagiline inhibited the cleavage and activation of procaspase-3 and poly (ADP-ribose) polymerase (PARP), whereas the PKC inhibitor, GF109203X, reversed these actions. Similarly, rasagiline decreased serum-free-induced levels of the important regulator of cell death, Bad, which was also blocked by GF109203X, indicating the involvement of PKC in rasagiline-induced cell survival. Furthermore, these studies have established that PKC- and Bcl-2-dependent neuroprotective activity of rasagiline is dependent on its propargyl moiety, because propargylamine had similar effects with the same potency.
本研究为涉及蛋白激酶C(PKC)通路与Bcl-2家族蛋白相互作用的神经保护提供了新见解。利用血清剥夺模型,我们研究了抗帕金森病/单胺氧化酶(MAO)-B抑制剂药物雷沙吉兰在大鼠嗜铬细胞瘤PC12细胞中发挥神经保护作用的机制。在此,我们报告雷沙吉兰(0.1 - 10 microM)通过多种保护机制减少细胞凋亡,包括刺激PKC磷酸化;上调PKCalpha和PKC mRNA,诱导Bcl-xL、Bcl-w和脑源性神经营养因子(BDNF)mRNA;以及下调Bad和Bax mRNA。此外,雷沙吉兰抑制procaspase-3和聚(ADP-核糖)聚合酶(PARP)的切割和激活,而PKC抑制剂GF109203X可逆转这些作用。同样,雷沙吉兰降低了无血清诱导的细胞死亡重要调节因子Bad的水平,这也被GF109203X阻断,表明PKC参与了雷沙吉兰诱导的细胞存活。此外,这些研究证实雷沙吉兰的PKC和Bcl-2依赖性神经保护活性依赖于其炔丙基部分,因为炔丙胺具有相同效力的类似作用。