Institute of Pharmacy, Free University of Berlin, D-14195 Berlin, Germany.
Acta Pharm. 2010 Mar;60(1):119-28. doi: 10.2478/v10007-010-0006-y.
Acetylcholinesterase (AChE) inhibitors are widely used for the symptomatic treatment of Alzheimer's disease (AD) to enhance central cholinergic transmission. On the other hand, butyrylcholinesterase (BuChE) inhibitors were reported to produce a significant increase in brain extracellular AChE without triggering severe peripheral or central side effects. In the present study, we selected twelve plants used in traditional European medicine to treat different central nervous system (CNS) disorders or to improve memory. Methanolic and hexane extracts of these plants were tested for the AChE and BuChE inhibitory activity using Ellman's colorimetric method. The most potent AChE and BuChE inhibition was observed in the hexane extracts of the flowers of Arnica chamissonis Less. subs. foliosa and Ruta graveolens L. herb at a concentration of 400 microg mL(-1). However, methanolic extracts of the flowers of Arnica chamissonis Less. subs. foliosa and the Hypericum perforatum L. herb demonstrated at the same concentration, selective inhibition only against AChE but not against BuChE. The other extracts did not show any significant AChE or BuChE inhibitory activity. Our results show that further investigations of the extracts of arnica, rue and St. John's Wort are needed to identity the compounds responsible for the AChE and BuChE inhibitory activity.
乙酰胆碱酯酶（AChE）抑制剂被广泛用于治疗阿尔茨海默病（AD）的症状，以增强中枢胆碱能传递。另一方面，丁酰胆碱酯酶（BuChE）抑制剂据报道可显著增加脑细胞外的 AChE，而不会引发严重的外周或中枢副作用。在本研究中，我们选择了 12 种用于治疗不同中枢神经系统（CNS）疾病或改善记忆的传统欧洲医学植物。使用 Ellman 的比色法测试这些植物的甲醇和己烷提取物对 AChE 和 BuChE 的抑制活性。在 400 μg/mL 的浓度下，Arnica chamissonis Less. subs. foliosa 和 Ruta graveolens L. herb 的花的己烷提取物表现出最强的 AChE 和 BuChE 抑制作用。然而，在相同浓度下，Arnica chamissonis Less. subs. foliosa 的花和贯叶连翘（Hypericum perforatum L.）草的甲醇提取物仅对 AChE 具有选择性抑制作用，而对 BuChE 没有抑制作用。其他提取物没有显示出任何显著的 AChE 或 BuChE 抑制活性。我们的结果表明，需要进一步研究山金车、芸香和贯叶连翘的提取物，以确定负责 AChE 和 BuChE 抑制活性的化合物。
