León Karen Acosta, Inca Alexandra, Tallini Luciana R, Osorio Edison H, Robles Jessica, Bastida Jaume, Oleas Nora H
Grupo de Investigación de Productos Naturales y Farmacia, Facultad de Ciencias, Escuela Superior Politécnica del Chimborazo, Panamericana Sur km 1 1/2, Riobamba EC060155, Ecuador.
Grup de Productes Naturals, Departament de Biologia, Sanitat i Medi Ambient, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona, Av. Joan XXIII, 27-31, Barcelona 08028, Spain.
S Afr J Bot. 2021 Jan;136:91-99. doi: 10.1016/j.sajb.2020.09.007. Epub 2020 Sep 18.
Alzheimer's disease is considered the most common cause of dementia and, in an increasingly aging population worldwide, the quest for treatment is a priority. Amaryllidaceae alkaloids are of main interest because of their cholinesterase inhibition potential, which is the main palliative treatment available for this disease. We evaluated the alkaloidal profile and the inhibitory activity on acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) of bulb alkaloid extract of and collected in Ecuador. Using gas chromatography coupled to mass spectrometry (GC-MS), we identified typical Amaryllidaceae alkaloids in these species, highlighting the presence of lycorine-type alkaloids in and haemanthamine/crinine-type in . The species and showed inhibitory activities against AChE (IC values of 25.48 ± 0.39 and 3.45 ± 0.29 μg.mL, respectively) and BuChE (IC values of 114.96 ± 4.94 and 58.89 ± 0.55 μg.mL, respectively). Computational experiments allowed us to understand the interactions of the alkaloids identified in these samples toward the active sites of AChE and BuChE. , some alkaloids detected in these Amaryllidaceae species presented higher estimated binding free energy toward BuChE than galanthamine. This is the first study about the alkaloid profile and biological potential of species.
阿尔茨海默病被认为是痴呆症最常见的病因,在全球人口老龄化日益加剧的情况下,寻求治疗方法成为当务之急。石蒜科生物碱因其具有胆碱酯酶抑制潜力而备受关注,这是该疾病目前主要的姑息治疗方法。我们评估了从厄瓜多尔采集的 和 的鳞茎生物碱提取物的生物碱谱及其对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BuChE)的抑制活性。通过气相色谱-质谱联用(GC-MS),我们在这些物种中鉴定出了典型的石蒜科生物碱,突出了 在 中存在石蒜碱型生物碱,而在 中存在海芒果碱/水仙环素型生物碱。 和 这两个物种对AChE(IC 值分别为25.48±0.39和3.45±0.29 μg/mL)和BuChE(IC 值分别为114.96±4.94和58.89±0.55 μg/mL)均表现出抑制活性。计算实验使我们能够了解这些样品中鉴定出的生物碱与AChE和BuChE活性位点之间的相互作用。 ,在这些石蒜科物种中检测到的一些生物碱对BuChE的估计结合自由能高于加兰他敏。这是关于 物种生物碱谱和生物潜力的首次研究。