Grup de Productes Naturals, Departament de Biologia, Sanitat i Medi Ambient, Facultat de Farmàcia, Universitat de Barcelona, 08028 Barcelona, Spain.
Grupo de Investigación en Sustancias Bioactivas, Facultad de Ciencias Farmacéuticas y Alimentarias, Universidad de Antioquia UdeA, Calle 70 No, 52-21, Medellín 050010, Colombia.
Molecules. 2018 Jun 26;23(7):1532. doi: 10.3390/molecules23071532.
Amaryllidaceae plants are the commercial source of galanthamine, an alkaloid approved for the clinical treatment of Alzheimer’s disease. The chemistry and bioactivity of Chilean representatives of genus from the family of Amaryllidaceae have not been widely studied so far. Ten collections of five different Chilean were analyzed in vitro for activity against enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) as well as for their alkaloid composition by GC-MS. To obtain an insight into the potential AChE and BuChE inhibitory activity of the alkaloids identified in the most active samples, docking experiments were carried out. Although galanthamine was found neither in aerial parts nor in bulbs of , these plant materials were the most active inhibitors of AChE (IC: 5.78 and 3.62 μg/mL, respectively) and BuChE (IC: 16.26 and 14.37 μg/mL, respectively). Some 37 known alkaloids and 40 still unidentified compounds were detected in the samples, suggesting high potential in the Chilean Amaryllidaceae plants as sources of both novel bioactive agents and new alkaloids.
石蒜科植物是加兰他敏的商业来源，加兰他敏是一种被批准用于治疗阿尔茨海默病的生物碱。迄今为止，尚未广泛研究来自石蒜科的智利属代表植物的化学和生物活性。对五个不同的智利 属的十个集合作了体外分析，以研究它们对乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BuChE) 等酶的活性以及通过 GC-MS 分析其生物碱组成。为了深入了解在最活跃的样品中鉴定出的生物碱对 AChE 和 BuChE 的潜在抑制活性，进行了对接实验。尽管在 的地上部分和鳞茎中都没有发现加兰他敏，但这些植物材料是 AChE（IC：5.78 和 3.62 μg/mL，分别）和 BuChE（IC：16.26 和 14.37 μg/mL，分别）的最有效抑制剂。在样品中检测到 37 种已知生物碱和 40 种尚未鉴定的化合物，这表明智利石蒜科植物作为新型生物活性物质和新生物碱的来源具有很高的潜力。
