Group of Natural Products, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII, 27-31, 08028 Barcelona, Spain.
Faculty of Pharmacy, Federal University of Rio Grande do Sul, Av. Ipiranga 2752, Porto Alegre RS 90610-000, Brazil.
Molecules. 2020 Apr 30;25(9):2092. doi: 10.3390/molecules25092092.
It is estimated that 50 million people in the world live with dementia, 60-70% of whom suffer from Alzheimer's disease (AD). Different factors are involved in the development of AD, including a reduction in the cholinergic neurotransmission level. The Amaryllidaceae plant family contains an exclusive, large, and still understudied alkaloid group characterized by a singular skeleton arrangement and a broad spectrum of biological activities. The chemistry and biodiversity of Ecuadorian representatives of the genus (Amaryllidaceae) have not been widely studied. In this work, five Ecuadorian species were examined in vitro for their activity towards the enzymes acetyl- (AChE) and butyrylcholinesterase (BuChE), and the alkaloid profile of bulb extracts was analyzed by GC-MS. The species and showed the most AChE and BuChE inhibitory activity, respectively. To obtain insight into the potential role of the identified alkaloids in these inhibitory effects, docking experiments were carried out, and cantabricine showed in silico inhibitory activity against both cholinesterase structures. Our results show that Amaryllidaceae species from Ecuador are a potential source of new drugs for the palliative treatment of AD.
据估计，全球有 5000 万人患有痴呆症，其中 60-70%患有阿尔茨海默病（AD）。AD 的发展涉及多种因素，包括胆碱能神经传递水平的降低。石蒜科植物家族含有独特的、大型的、仍未充分研究的生物碱群，其特征是独特的骨架排列和广泛的生物活性。厄瓜多尔属（石蒜科）代表植物的化学和生物多样性尚未得到广泛研究。在这项工作中，对五种厄瓜多尔物种进行了体外研究，以评估它们对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）的活性，并用 GC-MS 分析了鳞茎提取物的生物碱谱。和 分别显示出最强的 AChE 和 BuChE 抑制活性。为了深入了解鉴定出的生物碱在这些抑制作用中的潜在作用，进行了对接实验，发现 cantabricine 对两种胆碱酯酶结构均具有体外抑制活性。我们的结果表明，来自厄瓜多尔的石蒜科物种是治疗 AD 的姑息性治疗的潜在新药来源。
