白花树种子抗乙酰胆碱酯酶活性成分研究
首发时间:2013-08-23
摘要:综合利用硅胶柱、葡聚糖柱、制备HPLC等色谱技术分离白花树种子化学成分,从白花树种子乙酸乙酯和甲醇提取物中共分离获得8个苯并呋喃类衍生物(1-8),分别鉴定为7-demethoxylegonol-2-methylbutanoate (1), egonol-2-methylbutanoate (2), egonol acetate (3), 7-demethoxyegonol (4) and egonol (5), egonol glucoside (6), egonol gentiobioside (7)和demethoxyegonol gentiobioside (8),以上化合物均为首次从该植物中分离得到;体外对乙酰胆碱酯酶(AChE)测试表明化合物1和2显著抑制AChE活性,IC50分别为5.5 micromolar和1.8 micromolar,进一步测试表明化合物1和2能显著抑制Aβ淀粉样蛋白聚集活性,其抑制率分别为67.6%和70.5%。
关键词: 阿尔茨海默氏疾病 乙酰胆碱酯酶 Aβ淀粉样蛋白 白花树 苯并呋喃衍生物
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Anti-acetylcholinesterase Constituents from the Seeds of Styrax tonkinensis
Abstract: Chemical investigation of the extracts of the seeds of Styrax tonkinensis (Pierre) Craib ex Hart resulted in the isolation of eight known compounds (1-8) by using various chromatographic techniques such as silica gel, Sephadex LH-20 and preparative HPLC process, their chemical structures were then elucidated as: 7-demethoxylegonol-2-methylbutanoate (1), egonol-2-methylbutanoate (2), egonol acetate (3), 7-demethoxyegonol (4) egonol (5), egonol glucoside (6), egonol gentiobioside (7) and demethoxyegonol gentiobioside (8), respectively. Compounds 1-8 are obtained from this plant for the first time. Compounds 1 and 2 exhibited strong inhibitory activity against acetylcholinesterase with IC50 values of 5.5 micromolar and 1.8 micromolar, and compounds 3-8 did not showed any acetylcholinesterase inhibitory activity; Further studies showed that 1 and 2 also significantly inhibited AChE-induced Aβ aggregation by 67.6% and 70.5%, respectively.
Keywords: Alzheimer's disease acetylcholinesterase beta-amyloid Styrax tonkinensis Benzofurans
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