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Bioactive Aporphine Alkaloids from the Roots of Artabotrys spinosus: Cholinesterase Inhibitory Activity and Molecular Docking Studies

机译:来自Artabotrys Spinosus的根源的生物活性白孔生物碱:胆碱酯酶抑制活性和分子对接研究

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Six aporphine alkaloids (1-6) were isolated from Artabotrys spinosus roots based on bioassay-guided fraction and chromatographic methods. All isolated alkaloids were evaluated for their cholinesterase (ChEs) inhibitory activities, in which compounds 4 and 6 exhibited the highest activity toward butyrylcholinesterase (BChE) and acetylcholinesterase (AChE), respectively. The Lineweaver-Burk plots suggested that 4 and 6 were mixed mode inhibitors toward BChE and AChE enzymes, respectively. In addition, the experimental results were also confirmed by molecular docking analysis. This information can help in designing a new inhibitor in the class of aporphine alkaloids in against Alzheimer's disease.
机译:基于生物测定引导的分数和色谱方法,从Artabotrys Spinosus根中分离出六种白血孔生物碱(1-6)。 对其胆碱酯酶(Ches)抑制活性评价所有分离的生物碱,其中化合物4和6分别向丁酰胆碱酯酶(BCHE)和乙酰胆碱酯酶(ACHE)表现出最高的活性。 线织机-Burk图表明,4和6分别与BCHE和ACHE酶的混合模式抑制剂分别。 此外,还通过分子对接分析证实了实验结果。 这些信息可以有助于在针对阿尔茨海默病的嗜啡生物碱类中设计一种新的抑制剂。

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