Lin H Q, Ho Michelle T, Lau Lesley S, Wong Kelvin K, Shaw P C, Wan David C C
Department of Biochemistry, The Chinese University of Hong Kong, Shatin, N.T., Hong Kong, SAR, China.
Chem Biol Interact. 2008 Sep 25;175(1-3):352-4. doi: 10.1016/j.cbi.2008.05.030. Epub 2008 Jun 23.
Alzheimer's disease (AD) is a neurodegenerative disease characterized by progressive memory loss and cognitive impairment. It is the most common type of dementia in the ageing population due to a severe loss of cholinergic neurons in selected brain area. At present, acetylcholinesterase inhibitors (AChEI) are the first group of drugs approved by the FDA to treat mild to moderate Alzheimer's disease. Most of these drugs such as huperzine and galanthamine are originally isolated from plants. In this study, the AChE inhibitory activities from extracts of Chinese medicinal herbs that have traditionally been prescribed to treat insomnia and brain function disorders were examined in a 96-well plate assay based on Ellman's method. Both ethanol and aqueous extracts of 26 traditional Chinese medicinal herbs were tested. Inhibitory effects were expressed as the percentage of inhibition. For the herbal extracts that were shown to exert a significant inhibition, dose-dependent inhibitory assays were also performed. Ethanol and aqueous extracts of six herbs were found to have high AChE inhibitory activities in a dose-dependent manner. The IC(50) of these herbal extracts on inhibition of AChE are at around 5-85 microm/ml. The results of this study indicate that there is a great potential to search for novel usage of these medicinal herbs for the treatment of AD.
阿尔茨海默病(AD)是一种神经退行性疾病,其特征为进行性记忆丧失和认知障碍。由于特定脑区胆碱能神经元的严重丧失,它是老年人群中最常见的痴呆类型。目前,乙酰胆碱酯酶抑制剂(AChEI)是美国食品药品监督管理局(FDA)批准用于治疗轻至中度阿尔茨海默病的首批药物。这些药物中的大多数,如石杉碱和加兰他敏,最初是从植物中分离出来的。在本研究中,基于埃尔曼方法,在96孔板试验中检测了传统上用于治疗失眠和脑功能障碍的中草药提取物的乙酰胆碱酯酶(AChE)抑制活性。对26种传统中草药的乙醇提取物和水提取物都进行了测试。抑制作用以抑制百分比表示。对于显示出显著抑制作用的草药提取物,还进行了剂量依赖性抑制试验。发现六种草药的乙醇提取物和水提取物具有剂量依赖性的高AChE抑制活性。这些草药提取物对AChE抑制的半数抑制浓度(IC50)约为5 - 85微摩尔/毫升。本研究结果表明,探索这些草药在治疗AD方面的新用途具有很大潜力。