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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 clarify the influence of hydroxyl and methoxy substitution on benzene ring of catechol derivatives on anxiety behavior in mice. Methods: The mouse model of elevated plus maze was used to evaluate the effects of 3,4-dihydroxyacetophenone, phenylethylketone, ferulic acid and 3,4-dimethoxycinnamic acid containing no phenolic hydroxyl groups Effects of catechol and methyl vanillin on anxiety in mice. RESULTS: 3,4-Dihydroxyacetophenone (2 mg / kg) containing 2 phenolic hydroxyl groups showed significant anti-anxiety activity (P <0.01). Ferulic acid with 1 phenolic hydroxyl group kg) had significant anti-anxiety effects (P <0.05, P <0.01), whereas vanillone had the tendency to increase the evaluation index but had no significant anti-anxiety effect; 3,4-dimethoxycinnamic acid There was no anxiety and anxiety-causing activity. Methyl eugenol (5 mg / kg) and methyl vanillin (1.25 mg / kg) had obvious anxiety-causing activity (P <0.05, P <0.01). CONCLUSION: Hydroxyl and methoxy substituted derivatives on the catechol ring can produce the opposite effects of anxiolytic and anxiogenic, respectively. The structure-activity relationship of catechol derivatives affecting anxiety behavior in mice deserves further study.