Orhan Ilkay, Kartal Murat, Tosun Fatma, Sener Bilge
Department of Pharmacognosy, Faculty of Pharmacy, Gazi University, 06330 Ankara, Turkey.
Z Naturforsch C J Biosci. 2007 Nov-Dec;62(11-12):829-32. doi: 10.1515/znc-2007-11-1210.
Alzheimer's disease (AD), the most common form of dementia, is a neurodegenerative disease characterized by progressive cognitive deterioration together with declining activities of daily living and neuropsychiatric symptoms or behavioural changes. The oldest, on which most currently available drug therapies are based, is known as the "cholinergic hypothesis" and suggests that AD begins as a deficiency in the production of the neurotransmitter acetylcholine. Therefore, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors have gained a great popularity for the treatment of AD. In this study, we screened in vitro inhibitory activities of a number of phenolic acids (chlorogenic, caffeic, gallic, and quinic acids) as well as of various flavonoid derivatives (genistein, biochanin A, naringin, apigenin, quercetin, luteolin-7-O-rutinoside, kaempferol-3-O-galactoside, diosmin, silibinin, and silymarin) against AChE and BChE at 1 mg/ml concentration using a microplate-reader assay based on the Ellman method. Among them, only quercetin showed a substantial inhibition (76.2%) against AChE, while genistein (65.7%), luteolin-7-O-rutinoside (54.9%), and silibinin (51.4%) exerted a moderate inhibition on BChE.
阿尔茨海默病（AD）是最常见的痴呆形式，是一种神经退行性疾病，其特征为进行性认知衰退，同时日常生活活动能力下降以及出现神经精神症状或行为改变。目前大多数可用药物疗法所基于的最古老理论被称为“胆碱能假说”，该假说认为AD始于神经递质乙酰胆碱产生不足。因此，乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BChE）抑制剂在AD治疗中广受欢迎。在本研究中，我们使用基于埃尔曼方法的酶标仪检测法，在1mg/ml浓度下筛选了多种酚酸（绿原酸、咖啡酸、没食子酸和奎尼酸）以及各种黄酮类衍生物（染料木黄酮、鹰嘴豆芽素A、柚皮苷、芹菜素、槲皮素、木犀草素-7-O-芸香糖苷、山柰酚-3-O-半乳糖苷、地奥司明、水飞蓟宾和水飞蓟素）对AChE和BChE的体外抑制活性。其中，只有槲皮素对AChE表现出显著抑制（76.2%），而染料木黄酮（65.7%）、木犀草素-7-O-芸香糖苷（54.9%）和水飞蓟宾（51.4%）对BChE有中度抑制作用。
