水杨酸糖酯制备及活性研究

Synthesis of Salicylic Acid Saccharide Carboxylate and Evaluation of Their Bioactivity

目的:制备水杨酸糖酯,考察其刺激性和生物活性。方法:用羧酸有机碱法制备水杨酸糖酯;用1H-NMR和IR确认结构;用小鼠断尾法和小鼠耳肿胀法评价抗凝血活性和抗炎活性,组织切片法观察刺激性。结果:合成了4个β-构型的水杨酸糖酯,其中有3个的抗炎作用与阿司匹林相当,1个的抗凝血活性高于阿司匹林;合成物的刺激性均小于原药。结论:水杨酸糖酯类修饰可以降低刺激性。

Objective：To prepare salicylic acid saccharide carboxylate,evaluate their irritation activity and biology activity.Methods：The salicylic acid saccharide carboxylate were prepared through carboxylic acid-organic alkali,and the acetylated salicylic glucopyranose tetraacetate was synthesized by sequential elution;The structure of the products were identified by 1H-NMR and IR;The anticoagulant activity and anti-inflammatory activities were respectively evaluated by the cutting tail in mice and the models of mice ear edema induced by xylene,and the irritation activity was observed by tissue slices.Results：Fourβ-onfiguration salicylic acid saccharide carboxylate were prepared and three of them showed nearly the same bioactivities with aspirin in anticoagulant activity and anti-inflammation,and one of the products showed superior to their primary drug in anticoagulant activity;The irritation of the prepared products was less than the primary drug.Conclusion：The preparation of salicylic acid saccharide carboxylate could reduce the irritation of their corresponding primary drug.