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从竹节参叶中提取潜在乙酰胆碱酯酶抑制剂并进行体外筛选

Extraction and in vitro screening of potential acetylcholinesterase inhibitors from the leaves of Panax japonicus.

作者信息

Li Sainan, Liu Chengyu, Liu Chunming, Zhang Yuchi

机构信息

Central Laboratory, Changchun Normal University, No. 677 North Chang-ji Road, Changchun 130032, China.

Clinical Department of Rehabilitation, College of Acupuncture and Massage, Changchun University of Traditional Chinese Medicine, Changchun 130117, China.

出版信息

J Chromatogr B Analyt Technol Biomed Life Sci. 2017 Sep 1;1061-1062:139-145. doi: 10.1016/j.jchromb.2017.07.019. Epub 2017 Jul 12.

DOI:10.1016/j.jchromb.2017.07.019
PMID:28734162
Abstract

Ultrafiltration liquid chromatography-mass spectrometry (UFLC-MS) is an efficient method that can be applied to rapidly screen and identify ligands for acetylcholinesterase (AChE) from the leaves of Panax japonicus. Using this method, we identified 5 major compounds, chikusetsusaponins V, Ib, IV, IVa, and IVa ethyl ester, as potent AChE inhibitors, which were assessed for anti-Alzheimer disease activity using the PC12 cell model. A continuous online method, which consisted of microwave-assisted extraction, a solvent concentration tank, and centrifugal partition chromatography (MAE-SCT-CPC), was newly developed for scaled up production of these compounds with high purity and efficiency. The bioactivities of the compounds separated were assessed by the PC12 cell model. This novel approach of using UFLC-MS coupled with MAE-SCT-CPC and a PC12 cell model could be applied to efficiently screen, extract, and separate AChE inhibitors from complex samples, and could serve as an important platform for the large-scale production of functional food and nutraceutical ingredients.

摘要

超高效液相色谱 - 质谱联用(UFLC-MS)是一种高效的方法,可用于从竹节参叶片中快速筛选和鉴定乙酰胆碱酯酶(AChE)的配体。利用该方法,我们鉴定出5种主要化合物,即竹节人参皂苷V、Ib、IV、IVa和IVa乙酯,它们是有效的AChE抑制剂,并使用PC12细胞模型对其抗阿尔茨海默病活性进行了评估。一种由微波辅助萃取、溶剂浓缩罐和离心分配色谱组成的连续在线方法(MAE-SCT-CPC)被新开发出来,用于高效大规模生产这些高纯度化合物。通过PC12细胞模型评估分离出的化合物的生物活性。这种将UFLC-MS与MAE-SCT-CPC及PC12细胞模型相结合的新方法,可用于从复杂样品中高效筛选、提取和分离AChE抑制剂,并可作为大规模生产功能性食品和营养成分的重要平台。

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