Karanian David A, Baude Andrea S, Brown Queenie B, Parsons Christopher G, Bahr Ben A
Department of Pharmaceutical Sciences, University of Connecticut, Storrs, Connecticut 06269-3092, USA.
Hippocampus. 2006;16(10):834-42. doi: 10.1002/hipo.20214.
The over-activation of glutamate receptors can lead to excitotoxic cell death and is believed to be involved in the progression of neurodegenerative events in the vulnerable hippocampus. Here, we used an in vitro slice model to study toxicity produced in the hippocampus by the mitochondrial toxin 3-nitropropionic acid (3-NP). The organotypic slice cultures exhibit native cellular organization as well as dense arborization of neuronal processes and synaptic contacts. The hippocampal slices were exposed to 3-NP for 2-20 days, causing calpain-mediated breakdown of the spectrin cytoskeleton, a loss of pre- and postsynaptic markers, and neuronal atrophy. The N-methyl-D-aspartate (NMDA) receptor antagonist memantine reduced both the cytoskeletal damage and synaptic decline in a dose-dependent manner. 3-NP-induced cytotoxicity, as determined by the release of lactate dehydrogenase, was also reduced by memantine with EC50 values from 1.7 to 2.3 microM. Propidium iodide fluorescence and phase contrast microscopy confirmed memantine neuroprotection against the chronic toxin exposure. In addition, the protected tissue exhibited normal neuronal morphology in the major hippocampal subfields. These results indicate that antagonists of NMDA-type glutamate receptors are protective during the toxic outcome associated with mitochondrial dysfunction. They also provide further evidence of memantine's therapeutic potential against neurodegenerative diseases.
谷氨酸受体的过度激活可导致兴奋性毒性细胞死亡,并且被认为与脆弱海马体中神经退行性病变的进展有关。在此,我们使用体外脑片模型来研究线粒体毒素3-硝基丙酸(3-NP)在海马体中产生的毒性。器官型脑片培养物呈现出天然的细胞组织以及神经元突起和突触连接的密集分支。将海马体脑片暴露于3-NP中2至20天,会导致钙蛋白酶介导的血影蛋白细胞骨架分解、突触前和突触后标志物的丧失以及神经元萎缩。N-甲基-D-天冬氨酸(NMDA)受体拮抗剂美金刚以剂量依赖性方式减少了细胞骨架损伤和突触衰退。美金刚还降低了由乳酸脱氢酶释放所确定的3-NP诱导的细胞毒性,其半数有效浓度(EC50)值为1.7至2.3微摩尔。碘化丙啶荧光和相差显微镜证实了美金刚对慢性毒素暴露的神经保护作用。此外,受保护的组织在主要海马亚区呈现出正常的神经元形态。这些结果表明,NMDA型谷氨酸受体拮抗剂在与线粒体功能障碍相关的毒性结果中具有保护作用。它们还为美金刚治疗神经退行性疾病的潜在疗效提供了进一步证据。