Central Laboratory, Changchun Normal University, Changchun, P. R. China.
Guelph Research and Development Center, Agriculture and Agri-Food Canada, Guelph, Ontario, Canada.
J Sep Sci. 2020 Apr;43(8):1531-1543. doi: 10.1002/jssc.201901252. Epub 2020 Feb 24.
A simple and efficient ultrafiltration-liquid chromatography-mass spectrometry-based method was developed for the rapid screening and identification of ligands from Citrus limon peel, which are suitable acetylcholinesterase inhibitors. Subsequently, the anti-Alzheimer's activity of these compounds was assessed using a PC12 cell model. Six major compounds, viz. neoeriocitrin, isonaringin, naringin, hesperidin, neohesperidin, and limonin, were identified as potent acetylcholinesterase inhibitors. A continuous and efficient online method, which involved the use of a microwave-assisted extraction device, solvent concentration tank, and centrifugal partition chromatography column, was developed for the scale-up of these compounds, and the obtained compounds presented high purity. Next, their bioactivity was evaluated using a PC12 cell model. This novel approach, which was based on ultrafiltration-liquid chromatography-mass spectrometry, microwave-assisted extraction online coupled with solvent concentration tank, and centrifugal partition chromatography along with in vitro evaluation, could represent a powerful tool for the screening and extraction of acetylcholinesterase inhibitors from complex matrices, and could be a useful platform for the large-scale production of bioactive and nutraceutical ingredients.
建立了一种简单高效的超滤-液相色谱-质谱联用方法，用于快速筛选和鉴定柠檬果皮中适合乙酰胆碱酯酶抑制剂的配体。随后，采用 PC12 细胞模型评估了这些化合物的抗阿尔茨海默病活性。鉴定出 6 种主要化合物，即新橙皮苷、异柚皮苷、柚皮苷、橙皮苷、新橙皮苷和柠檬苦素，它们是有效的乙酰胆碱酯酶抑制剂。开发了一种连续高效的在线方法，包括使用微波辅助提取装置、溶剂浓缩罐和离心分配色谱柱，对这些化合物进行放大，得到的化合物具有高纯度。然后，使用 PC12 细胞模型评估它们的生物活性。这种基于超滤-液相色谱-质谱、微波辅助提取在线耦合溶剂浓缩罐和离心分配色谱以及体外评估的新方法，可以成为从复杂基质中筛选和提取乙酰胆碱酯酶抑制剂的有力工具，并可以成为大规模生产生物活性和营养成分的有用平台。
