Ren Zhili, Yang Nan, Ji Chao, Zheng Ji, Wang Tao, Liu Yanyong, Zuo Pingping
Department of Pharmacology, Institute of Basic Medical Sciences, Center of Neuroscience, Chinese Academy of Medical Sciences &School of Basic Medicine, Peking Union Medical College, Beijing, 100005, China.
Department of Pharmacology, Institute of Basic Medical Sciences, Center of Neuroscience, Chinese Academy of Medical Sciences &School of Basic Medicine, Peking Union Medical College, Beijing, 100005, China.
Neuropharmacology. 2015 Jun;93:209-18. doi: 10.1016/j.neuropharm.2015.01.030. Epub 2015 Feb 11.
Parkinson's disease (PD) is a neurological disorder characterized by degeneration of nigrostriatal dopaminergic (DAergic) system. Present treatment targeting to DAergic system solely ameliorated the symptoms but failed to retard the DAergic neuron degeneration, therefore new therapeutic methods aiming at preventing or delaying the neurodegenerative process are urgently needed. In the present study, we found that 5-(4-hydroxy-3-dimethoxybenzylidene)-2-thioxo-4-thiazolidinone (RD-1), a compound derived from rhodanine, protected DAergicneurons from neurotoxicity of MPTP/MPP(+). Firstly, RD-1 significantly improved the locomotor ability in the MPTP mice model, and elevated the tyrosine hydroxylase (TH) positive cell numbers in substantianigra pars compacta (SNpc) and the integrated optical density (IOD) of TH-positive nerve fibers in striatum respectively. Since mitochondrial dysfunction plays an important role in pathogenesis of PD, thereby we investigated the molecular mechanisms of RD-1 against MPTP/MPP(+) neurotoxicity, focusing on its effects on the mitochondrial dysfunction. Immunoblotting analysis showed that RD-1 significantly elevated the Parkin and Miro2 expression levels in acute MPTP treated mice, and improved mitochondrial membrane potential and ATP synthesis in MPP(+)-treated Neuro-2a cells. Moreover, RD-1attenuated impaired mitochondrial transport and vesicle release dysfunction evoked by MPP(+) cytotoxicity in cultured primary mesencephalic neurons. Taken together, these results indicate that improving the mitochondrial dysfunction may be a good choice to delay the neurodegenerative progression commonly associated with PD.
帕金森病(PD)是一种神经退行性疾病,其特征是黑质纹状体多巴胺能(DAergic)系统退化。目前仅针对DAergic系统的治疗方法只能缓解症状,但无法延缓DAergic神经元的退化,因此迫切需要旨在预防或延缓神经退行性过程的新治疗方法。在本研究中,我们发现5-(4-羟基-3-二甲氧基亚苄基)-2-硫代-4-噻唑烷酮(RD-1),一种来自罗丹宁的化合物,可保护DAergic神经元免受MPTP/MPP(+)的神经毒性。首先,RD-1显著改善了MPTP小鼠模型的运动能力,并分别提高了黑质致密部(SNpc)中酪氨酸羟化酶(TH)阳性细胞数量和纹状体中TH阳性神经纤维的积分光密度(IOD)。由于线粒体功能障碍在PD发病机制中起重要作用,因此我们研究了RD-1对抗MPTP/MPP(+)神经毒性的分子机制,重点关注其对线粒体功能障碍的影响。免疫印迹分析表明,RD-1显著提高了急性MPTP处理小鼠中Parkin和Miro2的表达水平,并改善了MPP(+)处理的Neuro-2a细胞中的线粒体膜电位和ATP合成。此外,RD-1减轻了培养的原代中脑神经元中MPP(+)细胞毒性引起的线粒体运输受损和囊泡释放功能障碍。综上所述,这些结果表明改善线粒体功能障碍可能是延缓通常与PD相关的神经退行性进展的一个不错选择。