和厚朴酚衍生物的合成及其抗焦虑活性研究  

Synthesis and anti-anxiety activity evaluation of honokiol derivatives

作　　者：崔帅[1] 张剑[1] 黄建梅[1] 蒋芦荻 梁英喜 李斌[1] 叶小彤 张小华[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《西北药学杂志》2015年第3期279-282,共4页Northwest Pharmaceutical Journal

基　　金：国家自然科学基金项目(编号:81173541);北京中医药大学自主课题(编号:2014-JYBZZ-XS-107)

摘　　要：目的合成和厚朴酚衍生物并对其抗焦虑活性进行评价,进而初步分析和厚朴酚中抗焦虑作用的药效基团。方法以中药厚朴中活性成分和厚朴酚为原料,通过甲基化、还原、电子重排、硼氢化等反应合成了和厚朴酚衍生物,并采用目前国内外常用的抗焦虑评价模型"高架十字迷宫"法对原料及所得衍生物在不同剂量下进行了活性评价。结果所得和厚朴酚衍生物经光谱方法鉴定了结构,其中化合物1和2具有明显的抗焦虑活性。结论对所得化合物进行活性评价,其中有2种衍生物具有抗焦虑活性,并通过结果分析得出和厚朴酚中侧链端基是抗焦虑必需的药效团,酚羟基对抗焦虑活性有一定影响。Objective To analyze the anti‐anxiety pharmacophore of honokiol ,five honokiol derivatives were synthesized and their anti‐anxiety activities were evaluated .Methods The derivatives were synthesized through methylation ,reduction ,electronic rear‐rangement ,hydroboration and so on using the active ingredient honokiol in traditional Chinese medicine Houpu as raw material . The raw material and derivatives were evaluated in different doses by the method of high plus maze .Results The structures of the derivatives were characterized by spectral techniques .Compound 1 and 2 showed obvious anti‐anxiety activity .Conclusion The activities of the obtained compounds were evaluated and two of them had the anti‐anxiety activity .The results also showed that the double bonds of honokiol are the essential groups ;the phenolic hydroxyl groups have an effect on anti‐anxiety activity and the position of them does not much affect the biological activity .

关 键 词：和厚朴酚衍生物 合成 抗焦虑 活性评价 

分 类 号：R914[医药卫生—药物化学]