CAJ | 학술논문

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。
목적：합성화후박분연생물병대기항초필활성진행평개，진이초보분석화후박분중항초필작용적약효기단。방법이중약후박중활성성분화후박분위원료，통과갑기화、환원、전자중배、붕경화등반응합성료화후박분연생물，병채용목전국내외상용적항초필평개모형“고가십자미궁”법대원료급소득연생물재불동제량하진행료활성평개。결과소득화후박분연생물경광보방법감정료결구，기중화합물1화2구유명현적항초필활성。결론대소득화합물진행활성평개，기중유2충연생물구유항초필활성，병통과결과분석득출화후박분중측련단기시항초필필수적약효단，분간기대항초필활성유일정영향。
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 .