Höglinger Günter U, Carrard Géraldine, Michel Patrick P, Medja Fadia, Lombès Anne, Ruberg Merle, Friguet Bertrand, Hirsch Etienne C
INSERM U289, Experimental Neurology and Therapeutics, Hôpital de la Salpêtrière, 47 Boulevard de l'Hôpital, 75651 Paris Cedex 13, France.
J Neurochem. 2003 Sep;86(5):1297-307. doi: 10.1046/j.1471-4159.2003.01952.x.
Two biochemical deficits have been described in the substantia nigra in Parkinson's disease, decreased activity of mitochondrial complex I and reduced proteasomal activity. We analysed interactions between these deficits in primary mesencephalic cultures. Proteasome inhibitors (epoxomicin, MG132) exacerbated the toxicity of complex I inhibitors [rotenone, 1-methyl-4-phenylpyridinium (MPP+)] and of the toxic dopamine analogue 6-hydroxydopamine, but not of inhibitors of mitochondrial complex II-V or excitotoxins [N-methyl-d-aspartate (NMDA), kainate]. Rotenone and MPP+ increased free radicals and reduced proteasomal activity via adenosine triphosphate (ATP) depletion. 6-hydroxydopamine also increased free radicals, but did not affect ATP levels and increased proteasomal activity, presumably in response to oxidative damage. Proteasome inhibition potentiated the toxicity of rotenone, MPP+ and 6-hydroxydopamine at concentrations at which they increased free radical levels >/= 40% above baseline, exceeding the cellular capacity to detoxify oxidized proteins reduced by proteasome inhibition, and also exacerbated ATP depletion caused by complex I inhibition. Consistently, both free radical scavenging and stimulation of ATP production by glucose supplementation protected against the synergistic toxicity. In summary, proteasome inhibition increases neuronal vulnerability to normally subtoxic levels of free radicals and amplifies energy depletion following complex I inhibition.
帕金森病患者黑质中已发现两种生化缺陷,即线粒体复合体I活性降低和蛋白酶体活性降低。我们分析了原代中脑培养物中这些缺陷之间的相互作用。蛋白酶体抑制剂(环氧霉素、MG132)加剧了复合体I抑制剂[鱼藤酮、1-甲基-4-苯基吡啶鎓(MPP+)]以及毒性多巴胺类似物6-羟基多巴胺的毒性,但对线粒体复合体II-V抑制剂或兴奋性毒素[N-甲基-D-天冬氨酸(NMDA)、红藻氨酸]则无此作用。鱼藤酮和MPP+通过三磷酸腺苷(ATP)耗竭增加自由基并降低蛋白酶体活性。6-羟基多巴胺也增加自由基,但不影响ATP水平,并增加蛋白酶体活性,这可能是对氧化损伤的反应。蛋白酶体抑制在鱼藤酮、MPP+和6-羟基多巴胺使自由基水平高于基线≥40%的浓度下增强了它们的毒性,超过了细胞对因蛋白酶体抑制而减少的氧化蛋白进行解毒的能力,并且还加剧了复合体I抑制所导致的ATP耗竭。同样,自由基清除和通过补充葡萄糖刺激ATP生成均可预防协同毒性。总之,蛋白酶体抑制增加了神经元对正常情况下处于亚毒性水平的自由基的易感性,并放大了复合体I抑制后的能量耗竭。