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厚朴酚与和厚朴酚衍生物的合成及其生物活性

李笑迪, 郭兴龙, 戴荣继, 吕芳, 丛林, 邓玉林

李笑迪, 郭兴龙, 戴荣继, 吕芳, 丛林, 邓玉林. 厚朴酚与和厚朴酚衍生物的合成及其生物活性[J]. 中国药科大学学报, 2017, 48(5): 536-542. DOI: 10.11665/j.issn.1000-5048.20170505
引用本文: 李笑迪, 郭兴龙, 戴荣继, 吕芳, 丛林, 邓玉林. 厚朴酚与和厚朴酚衍生物的合成及其生物活性[J]. 中国药科大学学报, 2017, 48(5): 536-542. DOI: 10.11665/j.issn.1000-5048.20170505
LI Xiaodi, GUO Xinglong, DAI Rongji, LYU Fang, CONG Lin, DENG Yulin. Synthesis and activities of derivatives of magnolol and honokiol[J]. Journal of China Pharmaceutical University, 2017, 48(5): 536-542. DOI: 10.11665/j.issn.1000-5048.20170505
Citation: LI Xiaodi, GUO Xinglong, DAI Rongji, LYU Fang, CONG Lin, DENG Yulin. Synthesis and activities of derivatives of magnolol and honokiol[J]. Journal of China Pharmaceutical University, 2017, 48(5): 536-542. DOI: 10.11665/j.issn.1000-5048.20170505

厚朴酚与和厚朴酚衍生物的合成及其生物活性

基金项目: 国家自然科学基金资助项目(No.81503353)

Synthesis and activities of derivatives of magnolol and honokiol

  • 摘要: 基于传统天然产物厚朴酚与和厚朴酚的多种药理活性,以治疗阿尔茨海默病为方向,设计了一系列厚朴酚与和厚朴酚衍生物,借助分子模拟平台Discovery Studio,以Aβ蛋白、Tau蛋白为靶蛋白,筛选出5种衍生物 6a ~ 6e 。并通过化学方法对其进行合成,用硫碘素T检测目标化合物的生物活性。结果显示:化合物 6a 在100 μmol/L浓度下,对于两种靶蛋白的聚集都有抑制作用,具有进一步研究价值。
    Abstract: Based on the chemical structures of magnolol and honokiol, a series of small molecular derivatives were designed for the treatment of Alzheimer′s disease. Through the Discovery Studio, five compounds( 6a - 6e )exhibited the inhibitory activity against Aβ and Tau proteins in all of the designed compounds. Then the five compounds are chemically synthesized and their biological activities were tested by thioflavin T. The result showed that compound 6a had inhibitory effect on the aggregation of two kinds of target proteins at the concentration of 100 μmol/L, which deserves further research.
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  • 刊出日期:  2017-10-24

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