Institut für Pharmakologie und Klinische Pharmazie, Fachbereich Pharmazie, Philipps-Universität Marburg, Marburg, Germany.
Experimental Neurology, Philipps-Universität Marburg, Marburg, Germany.
Cell Death Dis. 2014 Jan 16;5(1):e999. doi: 10.1038/cddis.2013.530.
Small-conductance Ca(2+)-activated K(+) channel activation is an emerging therapeutic approach for treatment of neurological diseases, including stroke, amyotrophic lateral sclerosis and schizophrenia. Our previous studies showed that activation of SK channels exerted neuroprotective effects through inhibition of NMDAR-mediated excitotoxicity. In this study, we tested the therapeutic potential of SK channel activation of NS309 (25 μM) in cultured human postmitotic dopaminergic neurons in vitro conditionally immortalized and differentiated from human fetal mesencephalic cells. Quantitative RT-PCR and western blotting analysis showed that differentiated dopaminergic neurons expressed low levels of SK2 channels and high levels of SK1 and SK3 channels. Further, protein analysis of subcellular fractions revealed expression of SK2 channel subtype in mitochondrial-enriched fraction. Mitochondrial complex I inhibitor rotenone (0.5 μM) disrupted the dendritic network of human dopaminergic neurons and induced neuronal death. SK channel activation reduced mitochondrial membrane potential, while it preserved the dendritic network, cell viability and ATP levels after rotenone challenge. Mitochondrial dysfunction and delayed dopaminergic cell death were prevented by increasing and/or stabilizing SK channel activity. Overall, our findings show that activation of SK channels provides protective effects in human dopaminergic neurons, likely via activation of both membrane and mitochondrial SK channels. Thus, SK channels are promising therapeutic targets for neurodegenerative disorders such as Parkinson's disease, where dopaminergic cell loss is associated with progression of the disease.
小电导钙激活钾通道(SK 通道)的激活是治疗神经退行性疾病(如中风、肌萎缩性侧索硬化症和精神分裂症)的新兴治疗方法。我们之前的研究表明,SK 通道的激活通过抑制 N-甲基-D-天冬氨酸受体(NMDAR)介导的兴奋性毒性发挥神经保护作用。在这项研究中,我们测试了 NS309(25 μM)激活 SK 通道对体外条件永生化和分化的人胎中脑多巴胺能神经元的治疗潜力。定量 RT-PCR 和 Western blot 分析表明,分化的多巴胺能神经元表达低水平的 SK2 通道和高水平的 SK1 和 SK3 通道。此外,亚细胞部分的蛋白质分析显示 SK2 通道亚型在富含线粒体的部分表达。线粒体复合物 I 抑制剂鱼藤酮(0.5 μM)破坏了人多巴胺能神经元的树突网络并诱导神经元死亡。SK 通道激活降低了线粒体膜电位,但在鱼藤酮挑战后,保留了树突网络、细胞活力和 ATP 水平。通过增加和/或稳定 SK 通道活性,防止了线粒体功能障碍和多巴胺能神经元的延迟死亡。总的来说,我们的研究结果表明,激活 SK 通道可提供对人多巴胺能神经元的保护作用,这可能是通过激活膜和线粒体 SK 通道实现的。因此,SK 通道是治疗神经退行性疾病的有前途的治疗靶点,如帕金森病,其中多巴胺能神经元的丧失与疾病的进展有关。
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