NO供体型丹皮酚衍生物的合成及其生物活性研究

Synthesis and Bioactivity of NO-Donating Paeonol Derivatives

以丹皮酚与溴乙酸为原料制备丹皮酚乙酸,利用其羧基与不同碳数的二溴烷烃反应得到相应的丹皮酚乙酸溴代烷基酯(3a^3e),再与硝酸银反应生成目标化合物NO供体型丹皮酚衍生物4a^4e。目标化合物的结构经过红外光谱、核磁共振氢谱和质谱确证。对合成的NO供体型丹皮酚衍生物进行体外抗血小板聚集及体内调血脂作用的生物活性测试,结果表明,目标化合物均具有一定的体外抗血小板聚集活性及较强的体内降脂作用,其中化合物4c的活性最强。

Paeonol acetic acid were synthesized by the reaction between paeonol（1）with bromoacetic acid,followed by treating paeonol acetic acid with dibromoalkanes[C（2）~C（6）]in the presence of K_2CO_3 to provide the compounds of bromo alkyl ester of paeonol acetate（3 a^3 e）.Next,3 a^3 ereacted with silver nitrate for yielding the target compounds of 4 a^4 e（NO-donating paeonol derivatives）.Their structures were confirmed by IR,MS,and ~1H NMR.Anti-platelet aggregation and lipidemic-modulating activities of the target compounds were evaluated.It is found that all of the synthesized compounds possess anti-platelet aggregation and lipidemic-modulating activity.In particular,compound 4 cshows significant anti-platelet aggregation activity in comparison with that of control aspirin,and stronger lipidemic-modulating action than that of control paeonol.