Perasso L, Adriano E, Ruggeri P, Burov S V, Gandolfo C, Balestrino M
Department of Neuroscience, Ophthalmology and Genetics, University of Genova, Genova, Italy.
Brain Res. 2009 Aug 18;1285:158-63. doi: 10.1016/j.brainres.2009.06.009. Epub 2009 Jun 11.
Phosphocreatine-Mg-complex acetate (PCr-Mg-CPLX) is a creatine-derived compound that in previous in vitro research was able to increase neuronal creatine independently of the creatine transporter, thus providing hope to cure the hereditary syndrome of creatine transporter deficiency. In previous research we showed that it reproduces in vitro the known neuroprotective effect of creatine against anoxic damage. In the present paper we investigated if PCr-Mg-CPLX reproduces this neuroprotective effect in vivo, too. We used a mouse model of transient middle cerebral artery occlusion. Mice received PCr-Mg-CPLX or a mixture of the two separate compounds phosphocreatine (PCr) and MgSO(4), or vehicle. The injections were done 60 min and 30 min before ischemia. Forty-eight hours after ischemia neurological damage was evaluated with Clark's behavioural tests, then the infarct volume was measured. PCr-Mg-CPLX reduced the infarct volume by 48%, an effect that was not duplicated by the separate administration of PCr and MgSO(4) and the neurological damage was decreased in a statistically significant way. We conclude that PCr-Mg-CPLX affords in vivo neuroprotection when administered before ischemia. These results are comparable to previous research on creatine administration in experimental stroke. PCr-Mg-CPLX maintains creatine-like neuroprotective effects in vivo as well as in vitro. Our study suggests that PCr-Mg-CPLX might have a therapeutic role in the treatment of hereditary creatine transporter deficiency and of conditions where there is a high risk of impending stroke or cerebral ischemic damage, like high-risk transient ischemic attacks, open heart surgery, and carotid surgery.
磷酸肌酸 - 镁复合醋酸盐(PCr - Mg - CPLX)是一种源自肌酸的化合物,在先前的体外研究中,它能够独立于肌酸转运体增加神经元中的肌酸,从而为治愈肌酸转运体缺乏的遗传性综合征带来了希望。在先前的研究中,我们表明它在体外再现了肌酸对缺氧损伤的已知神经保护作用。在本文中,我们研究了PCr - Mg - CPLX在体内是否也能再现这种神经保护作用。我们使用了短暂性大脑中动脉闭塞的小鼠模型。小鼠接受PCr - Mg - CPLX或两种单独化合物磷酸肌酸(PCr)和硫酸镁(MgSO₄)的混合物,或赋形剂。在缺血前60分钟和30分钟进行注射。缺血48小时后,用克拉克行为测试评估神经损伤,然后测量梗死体积。PCr - Mg - CPLX使梗死体积减少了48%,单独给予PCr和MgSO₄并没有重复这种效果,并且神经损伤在统计学上有显著降低。我们得出结论,PCr - Mg - CPLX在缺血前给药时能在体内提供神经保护。这些结果与先前关于在实验性中风中给予肌酸的研究结果相当。PCr - Mg - CPLX在体内和体外都保持类似肌酸的神经保护作用。我们的研究表明,PCr - Mg - CPLX可能在治疗遗传性肌酸转运体缺乏以及存在即将发生中风或脑缺血损伤高风险的病症(如高风险短暂性脑缺血发作、心脏直视手术和颈动脉手术)中具有治疗作用。