Institute of Molecular and Cellular Biology, Faculty of Biological Sciences, University of Leeds, Leeds, LS2 9JT, United Kingdom.
J Mol Neurosci. 2012 Mar;46(3):569-77. doi: 10.1007/s12031-011-9644-x. Epub 2011 Sep 20.
Alzheimer's disease (AD) is accompanied by memory loss due to neuronal cell death caused by toxic amyloid β-peptide (Aβ) aggregates. In the healthy brain, a group of amyloid-degrading enzymes including neprilysin (NEP) maintain Aβ levels at physiologically low concentrations but, with age and under some pathological conditions, expression and activity of these enzymes decline predisposing to late-onset AD. Hence, up-regulation of NEP might be a viable strategy for prevention of Aβ accumulation and development of the disease. As we have recently shown, inhibitors of histone deacetylases, in particular, valproic acid (VA), were capable of up-regulating NEP expression and activity in human neuroblastoma SH-SY5Y cell lines characterised by very low levels of NEP. In the present study, analysing the effect of i.p. injections of VA to rats, we have observed up-regulation of expression and activity of NEP in rat brain structures, in particular, in the hippocampus. This effect was brain region- and age-specific. Administration of VA has also restored NEP activity and memory deficit in adult rats caused by prenatal hypoxia. This suggests that VA and more specific HDAC inhibitors can be considered as potential pharmaceutical agents for up-regulation of NEP activity and improvement of cognitive functions of ageing brain.
阿尔茨海默病(AD)伴随着神经元细胞死亡导致的记忆丧失,而神经元细胞死亡是由毒性淀粉样β肽(Aβ)聚集引起的。在健康的大脑中,一组包括神经肽酶(NEP)在内的淀粉样蛋白降解酶将 Aβ 水平维持在生理浓度下,但随着年龄的增长和某些病理条件下,这些酶的表达和活性下降,易患迟发性 AD。因此,上调 NEP 可能是预防 Aβ 积累和疾病发展的可行策略。正如我们最近所表明的,组蛋白去乙酰化酶抑制剂,特别是丙戊酸(VA),能够上调人类神经母细胞瘤 SH-SY5Y 细胞系中 NEP 的表达和活性,该细胞系的 NEP 水平非常低。在本研究中,通过分析腹腔注射 VA 对大鼠的影响,我们观察到 NEP 的表达和活性在大鼠脑结构中上调,特别是在海马体中。这种作用具有脑区和年龄特异性。VA 的给药还恢复了产前缺氧引起的成年大鼠的 NEP 活性和记忆缺陷。这表明 VA 和更特异的 HDAC 抑制剂可以被认为是上调 NEP 活性和改善衰老大脑认知功能的潜在药物。