Departament de Biologia, Sanitat i Medi Ambient, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Av. Joan XXIII 27-31, 08028 Barcelona, Spain.
Independent Researcher, C/Caridad 8, Planta 2, Puerta 8, 29680 Estepona, Spain.
Molecules. 2023 Jan 27;28(3):1239. doi: 10.3390/molecules28031239.
Amaryllidaceae alkaloids are secondary metabolites with interesting medicinal properties. Almost every species can synthesize them and constitute an excellent source for their isolation and study. Several Amaryllidaceae alkaloids have shown acetylcholinesterase inhibitory activities and are a promising tool for treating cholinergic disorders such as Alzheimer's disease (AD). Indeed, three of the four palliative treatments approved for AD are acetylcholinesterase (AChE) inhibitors and one of them, galanthamine, is an Amaryllidaceae alkaloid itself. This molecule is currently isolated from natural sources. However, its production is insufficient to supply the increasing demand for the active principle. Our main aim is to discover tools to improve galanthamine production and to prospect for potential new and more efficient drugs for AD treatment. Furthermore, we seek to broaden the knowledge of plants of the genus from a chemotaxonomic perspective. Hence, in this study, we evaluate the alkaloid content through GC-MS and the AChE inhibitory activity of ten autumn-flowering , which have been less studied than their spring-flowering counterparts. A total of thirty Amaryllidaceae alkaloids have been found, twenty-eight properly identified. Two contained galanthamine, and seven were able to inhibit AChE.
石蒜科生物碱是具有有趣药用性质的次生代谢产物。几乎每个物种都可以合成它们,是分离和研究它们的极好来源。一些石蒜科生物碱具有乙酰胆碱酯酶抑制活性,是治疗胆碱能紊乱(如阿尔茨海默病)的有前途的工具。事实上,批准用于 AD 的四种姑息治疗中有三种是乙酰胆碱酯酶 (AChE) 抑制剂,其中一种加兰他敏本身就是一种石蒜科生物碱。这种分子目前是从天然来源中分离出来的。然而,其产量不足以满足对活性成分的日益增长的需求。我们的主要目标是发现工具来提高加兰他敏的产量,并寻找潜在的新的、更有效的 AD 治疗药物。此外,我们试图从化学分类学的角度拓宽对该属植物的认识。因此,在这项研究中,我们通过 GC-MS 评估了十种秋季开花植物的生物碱含量,这些植物比春季开花的植物研究得更少。总共发现了三十种石蒜科生物碱,其中二十八种得到了正确鉴定。两种植物含有加兰他敏,七种植物能够抑制乙酰胆碱酯酶。