目的:明确儿茶酚衍生物苯环上羟基及甲氧基取代对小鼠焦虑行为的影响。方法:采用小鼠高架十字迷宫模型,评价含有酚羟基的3,4-二羟基苯乙酮、香草乙酮、阿魏酸和不含酚羟基的3,4-二甲氧基肉桂酸、甲基丁香酚、甲基香草醛等儿茶酚衍生物对小鼠焦虑行为的影响。结果:含有2个酚羟基的3,4-二羟基苯乙酮(20mg/kg)具有明显的抗焦虑活性(P〈0.01);含有1个酚羟基的阿魏酸(5、10、20mg/kg)具有明显的抗焦虑作用(P〈0.05,P〈0.01),而香草乙酮有增加评价指标的趋势但无显著抗焦虑作用;不含酚羟基的3,4-二甲氧基肉桂酸无抗焦虑和致焦虑活性,甲基丁香酚(5mg/kg)及甲基香草醛(1.25mg/kg)具有明显的致焦虑活性(P〈0.05,P〈0.01)。结论:儿茶酚苯环上羟基、甲氧基取代衍生物可分别产生抗焦虑、致焦虑两种相反的作用,儿茶酚衍生物影响小鼠焦虑行为的构效关系值得深入研究。
Objective: To clarity the effects of catechol derivatives with hydroxyl or methoxy groups in substituted on anxiety behaviors in mice. Methods: The effects of catechol derivatives contained 3,4-dihydroxyacetophenone, acetovanillone, ferulic acid and did not contain 3,4-dihydroxyacetophenone, methyleugenol, methylvanillin on the anxiety behavior of mice were evaluated by elevated plus maze. Results: In the elevated plus maze, 3,4-dihydroxyacetophenone(20mg/kg) with two phenolic hydroxyl showed significant anxiolytic effects(P〈0.01). Ferulic acid(5, 10, 20 mg/kg) with one phenolic hydroxyl had significant anxiolytic effects(P〈0.05, P〈0.01), while acetovanillone showed an increasing trend in the evaluation index but without significant anxiolytic effect. 3,4-dimethoxycinnamic acid without phenolic hydroxyl did not have anxiolytic or anxiogenic activity. However, methyleugenol(5mg/kg), methylvanillin(1.25mg/kg) showed obviously anxiogenic activities(P〈0.05, P〈0.01). Conclusion: Catechol derivatives with hydroxyl or methoxy groups in substituted had anxiolytic or anxiogenic effects on the anxiety behaviors in mice, the specific structure-activity relationship was worthy of further investigation.