染料木素结构修饰及其抗氧化活性构效关系的研究

Research on Structural Modification of Genistein and Antioxidation Structure-Activity Relationship

[目的]研究染料木素抗氧化活性与其侧链乙酰化修饰的构效关系。[方法]用乙酸酐对染料木素进行乙酰化结构修饰,然后经制备薄层层析将不同产物分离,硅胶柱层析洗脱得到单一产物,用紫外分光光度计对产物进行扫描得到紫外图谱,加入各种诊断剂根据波峰变化情况分析产物结构,采用邻苯三酚自氧化法研究各产物的抗氧化活性。[结果]获得5-乙酰染料木素(化合物1)和5,7-二乙酰染料木素(化合物2)2个乙酰化产物。当浓度为0.001 43 mg/ml时,原料染料木素及化合物1、2对邻苯三酚自氧化抑制率分别为55%、70%、65%。[结论]乙酰化可明显地提高染料木素抗氧化活性。

[ Objective ] The research aimed to explore the effects of acetylation to genistein on its antioxidant activity. [ Methods] The structural modification of the acetylation with acetic anhydride was used. The acetylated products were separated by preparative TLC method and their structures were elucidated by UV spectrums. Then, the antioxidation abilities of the compounds were evaluated by using autoxidation of pyrogallic acid. [ Result ] Two compounds, 5,7-diacetyl genistein （1） and 5-acetyl genistein （2）, were obtained. And at the concentration of 0. 001 43 mg/ml, the inhibiting rates of genistein l and 2 reached 55% , 70% and 65% , respectively. [ Conclusion] Acetylation modification could increase the in-vitro antioxidant activity of genistein