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Ligand fishing and identification of acetylcholinesterase inhibitors in Mahonia bealei (Fort.) Carr. using high performance liquid chromatography-mass spectrometry
Journal of Liquid Chromatography & Related Technologies ( IF 1.0 ) Pub Date : 2020-04-01 , DOI: 10.1080/10826076.2020.1745229
Yang Huang 1, 2 , Tiejie Wang 1, 3 , Jue Wang 1, 3 , Guo Yin 1, 3 , Jiasheng Tu 2
Affiliation  

Abstract A fishing platform was developed using immobilized capillary enzyme reactors in combination with liquid chromatography-mass spectrometry (LC-MS) to fish acetylcholinesterase inhibitor (AChEI) from Mahonia bealei (Fort.) Carr. (M. bealei) extract. Four potential AChEIs (columbamine, jatrorrhizine, berberine, and palmatine) were successfully screened out and identified. Their AChE inhibitory activities were further verified by an in vitro assay with IC50 values of 0.93 ± 0.12 μg/mL (columbamine), 3.50 ± 0.15 μg/mL (jatrorrhizine), 2.51 ± 0.12 μg/mL (berberine), and 1.52 ± 0.13 μg/mL (palmatine). A synergy study of these AChEIs was subsequently investigated. In comparison with the IC50 value of M. bealei extract (IC50=0.83 ± 0.21 μg/mL), it can be stated that M. bealei extract is much more active than any single AChEI. Thereafter, the determination of these four alkaloids were investigated and AChE inhibitory effect were compared in terms of the extract and corresponding contents of these four alkaloids. The inhibitory effects of extract at each concentration were stronger than four alkaloids mixture. The results demonstrated that not the four AChEI mixture cause the synergistic effect but rather than the concentrations or ratios of these AChEIs play a vital role in their synergy study. Graphical Abstract

中文翻译:

Mahonia bealei (Fort.) Carr 中的配体捕捞和乙酰胆碱酯酶抑制剂的鉴定。使用高效液相色谱-质谱法

摘要 利用固定化毛细管酶反应器结合液相色谱-质谱联用技术(LC-MS) 开发了一种捕捞平台,用于捕获来自Mahonia bealei (Fort.) Carr 的鱼类乙酰胆碱酯酶抑制剂(AChEI)。(M. bealei) 提取物。成功筛选并鉴定了四种潜在的 AChEI(天冬酰胺、药根碱、小檗碱和巴马汀)。它们的 AChE 抑制活性通过体外试验得到进一步验证,IC50 值为 0.93 ± 0.12 μg/mL(莨菪碱)、3.50 ± 0.15 μg/mL(药根碱)、2.51 ± 0.12 μg/mL(黄连素)和 1.53 ± 0。微克/毫升(巴马汀)。随后研究了这些 AChEI 的协同作用研究。与 M. bealei 提取物的 IC50 值 (IC50=0.83 ± 0.21 μg/mL) 相比,可以说 M. bealei 提取物比任何单一 AChEI 的活性都要高得多。此后,考察了这四种生物碱的测定方法,比较了这四种生物碱的提取物和相应含量对乙酰胆碱酯酶的抑制作用。各浓度提取物的抑制作用均强于四种生物碱混合物。结果表明,不是四种 AChEI 混合物引起协同效应,而是这些 AChEI 的浓度或比例在它们的协同研究中起重要作用。图形概要 结果表明,不是四种 AChEI 混合物引起协同效应,而是这些 AChEI 的浓度或比例在它们的协同研究中起重要作用。图形概要 结果表明,不是四种 AChEI 混合物引起协同效应,而是这些 AChEI 的浓度或比例在它们的协同研究中起重要作用。图形概要
更新日期:2020-04-01
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