Ueda Hiroshi
Division of Molecular Pharmacology and Neuroscience, Nagasaki University Graduate School of Biomedical Sciences, 1-14 Bunkyo-machi, Nagasaki, 852-8521, Japan.
Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):315-23. doi: 10.1007/s00210-007-0254-7. Epub 2008 Jan 5.
After stroke or traumatic damages, both necrotic and apoptotic neuronal death cause a loss of functions including memory, sensory perception, and motor skills. From the fact that necrosis has a nature to expand, while apoptosis to cease the cell death cascade in the brain, it is considered that the promising target for the rapid treatment for stroke is the necrosis. In this study, I introduce the discovery of prothymosin alpha (ProTalpha), which inhibits neuronal necrosis, and propose its potentiality of clinical use for stroke. First of all, it should be noted that ProTalpha inhibits the neuronal necrosis induced by serum-free starvation or ischemia-reperfusion stress, which causes a rapid internalization of GLUT1/4, leading a decrease in glucose uptake and cellular ATP levels. Underlying mechanisms are determined to be through an activation of Gi/o, phospholipase C and PKCbetaII. ProTalpha also causes apoptosis later through a similar mechanism. However, we found that ProTalpha-induced apoptosis is completely inhibited by the concomitant treatment with neurotrophins, which are up-regulated by ischemic stress in the brain. Of most importance is the finding that the systemic injection of ProTalpha completely inhibits the brain damages, motor dysfunction and learning memory defect induced by cerebral ischemia-reperfusion stress. As ProTalpha almost entirely prevents the focal ischemia-induced motor dysfunction 4 h after the start of ischemia, this protein seems to have a promising potentiality for clinical use.
中风或创伤性损伤后,坏死性和凋亡性神经元死亡都会导致包括记忆、感觉知觉和运动技能在内的功能丧失。鉴于坏死具有扩展的特性,而凋亡则会终止大脑中的细胞死亡级联反应,因此坏死被认为是中风快速治疗的有前景的靶点。在本研究中,我介绍了抑制神经元坏死的前胸腺素α(ProTα)的发现,并提出了其在中风临床应用中的潜力。首先,应该注意到ProTα抑制由无血清饥饿或缺血再灌注应激诱导的神经元坏死,这种应激会导致GLUT1/4迅速内化,导致葡萄糖摄取和细胞ATP水平降低。其潜在机制被确定为通过激活Gi/o、磷脂酶C和PKCβII。ProTα随后也会通过类似机制导致细胞凋亡。然而,我们发现,通过与神经营养因子联合治疗,ProTα诱导的细胞凋亡被完全抑制,而神经营养因子在大脑中会因缺血应激而上调。最重要的发现是,全身注射ProTα能完全抑制脑缺血再灌注应激诱导的脑损伤、运动功能障碍和学习记忆缺陷。由于ProTα在缺血开始后4小时几乎完全预防了局灶性缺血诱导的运动功能障碍,这种蛋白质似乎具有临床应用的前景。