线粒体钠/钙交换器,在大鼠海马切片中神经保护的新靶点。
Mitochondrial Na+/Ca2+ exchanger, a new target for neuroprotection in rat hippocampal slices.
机构信息
Instituto Teófilo Hernando, Facultad de Medicina, Universidad Autónoma de Madrid, 28029 Madrid, Spain.
出版信息
Biochem Biophys Res Commun. 2010 Sep 10;400(1):140-4. doi: 10.1016/j.bbrc.2010.08.028. Epub 2010 Aug 14.
We tested here the hypothesis that the pharmacological modulation of the mitochondrial Na(+)/Ca(2+) exchanger (mNCX) could be a new neuroprotective strategy to rescue stressed vulnerable neurons from death. We used rat hippocampal slices incubated with veratridine to cause neuronal death through a mechanism involving Na(+) and Ca(2+) overload. CGP37157 (CGP), an inhibitor of the mNCX, rescued veratridine vulnerable neurons from death, showing an EC(50) of 5 μM. This neuroprotection was associated to mitigation of veratridine-elicited overproduction of free radicals and to inhibition of the p38 MAPK-linked apoptotic pathway. These results suggest that the mNCX could become a new target to develop compounds with potential therapeutic neuroprotective actions in neurodegenerative diseases.
我们在这里检验了一个假说,即通过药理学调节线粒体 Na(+) / Ca(2+) 交换器(mNCX)可能是一种新的神经保护策略,可以挽救处于应激状态的易损神经元免于死亡。我们使用用藜芦碱孵育的大鼠海马切片来引起神经元死亡,该机制涉及 Na(+) 和 Ca(2+) 过载。mNCX 的抑制剂 CGP37157(CGP)可挽救藜芦碱易损神经元免于死亡,其 EC(50)为 5 μM。这种神经保护作用与减轻藜芦碱引起的自由基过度产生以及抑制 p38 MAPK 相关的凋亡途径有关。这些结果表明,mNCX 可能成为开发具有治疗神经退行性疾病潜在神经保护作用的化合物的新靶点。