丹皮酚合成过程中抑菌活性的变化研究

Study on the Changes of Antifungal Activity during the Synthesis of Paeonol

研究了在丹皮酚的合成过程中,原料间苯二酚、中间产物2,4-二羟基苯乙酮及主产物丹皮酚对11种植物病原真菌的抑菌活性,并通过抑菌活性的变化来推测影响抑菌活性的主要官能团。结果表明:0.5g.L-1的2,4-二羟基苯乙酮对11种真菌的抑菌率大于或等于同浓度丹皮酚的抑菌率,两者均远远大于同浓度间苯二酚的抑菌率。由此可推测,酚类分子中乙酰基的引入对抑菌活性起到了非常重要的作用,而酚羟基的甲基化的作用却并不显著。该结论对寻求具有更高抑菌活性的酚类衍生物有着非常重要的意义。

The antifungal activities to 11 fungi of three compounds（raw material m-dihydroxybenzene,intermediate product 2,4-dihydroxyacetophenone and main product paeonol） were studied during the synthesis of paeonol.The main functional group that impacted on the antifungal activity was found based on the changes of antifungal activity.Results showed that：to these 11 fungi,the antifungal activities of 0.5 g·L-1 2,4-dihydroxyacetophenone were greater than or equal to those of paeonol at same concentration,both of them were far greater than those of m-dihydroxybenzene at same concentration.So it could be speculated that the introduction of acetyl group in the phenolic molecules played a very important role on antifungal activity,but the methylation of phenolic hydroxyl had less effect on it.This conclusion is very important for seeking more phenolic derivatives with higher antifungal activities.