Center of Excellence for Novel Approaches to Neurodiagnostics and Neurotherapeutics, Brain Institute, Center of Excellence for Research in Complementary and Alternative Medicine in Alzheimer's Disease, Department of Neurology, Mount Sinai School of Medicine, New York, NY 10029, USA.
Expert Rev Proteomics. 2010 Aug;7(4):579-89. doi: 10.1586/epr.10.69.
A diverse group of neurodegenerative diseases are characterized by progressive, age-dependent intracellular formation of misfolded protein aggregates. These include Alzheimer's disease, Huntington's disease, Parkinson's disease and a number of tau-mediated disorders. There is no effective treatment for any of these disorders; currently approved interventions are designed to treat disease symptoms and generally lead to modest modulation of clinical symptoms. None are known to mitigate underlying neuropathologic mechanisms and, thus, it is not unexpected that existing treatments appear ineffective in modulating disease progression. We note that these neurodegenerative disorders all share a common mechanistic theme in that depositions of misfolded protein in the brain is a key molecular feature underlying disease onset and/or progression. While previous studies have identified a number of drugs and nutraceuticals capable of interfering with the formation and/or stability of misfolded protein aggregates, none have been demonstrated to be effective in vivo for treating any of the neurodegenerative disorders. We hereby review accumulating evidence that a select nutraceutical grape-seed polyphenolic extract (GSPE) is effective in vitro and in vivo in mitigating certain misfolded protein-mediated neuropathologic and clinical phenotypes. We will also review evidence implicating bioavailability of GSPE components in the brain and the tolerability as well as safety of GSPE in animal models and in humans. Collectively, available information supports continued development of the GSPE for treating a variety of neurodegenerative disorders involving misfolded protein-mediated neuropathologic mechanisms.
一组不同的神经退行性疾病的特征是进行性的、年龄依赖性的细胞内错误折叠蛋白聚集的形成。这些疾病包括阿尔茨海默病、亨廷顿病、帕金森病和许多 tau 介导的疾病。目前还没有针对这些疾病的有效治疗方法;目前批准的干预措施旨在治疗疾病症状,通常只能适度调节临床症状。目前还没有已知的方法可以减轻潜在的神经病理机制,因此,现有的治疗方法似乎对疾病进展没有效果也就不足为奇了。我们注意到,这些神经退行性疾病都有一个共同的机制主题,即在大脑中错误折叠蛋白的沉积是疾病发病和/或进展的关键分子特征。虽然以前的研究已经确定了许多能够干扰错误折叠蛋白聚集体形成和/或稳定性的药物和营养保健品,但没有一种被证明对治疗任何神经退行性疾病都有效。我们在此回顾了越来越多的证据,证明一种特定的营养保健品——葡萄籽多酚提取物(GSPE)在体外和体内都能有效减轻某些错误折叠蛋白介导的神经病理和临床表型。我们还将回顾 GSPE 成分在大脑中的生物利用度以及在动物模型和人类中的耐受性和安全性的证据。总的来说,现有信息支持继续开发 GSPE 来治疗涉及错误折叠蛋白介导的神经病理机制的各种神经退行性疾病。