【作者】 武雪芬； 侯益民； 马金刚；

【Author】 WU Xuefen,HOU Yimin,MA Jingang (Henan College of Traditional Chinese Medicine,Zhenzhou 450008,china)

【机构】 河南中医学院药学院；

【摘要】 目的制备水杨酸糖酯,考察其生物活性。方法用羧酸有机碱法和羧酸盐直接反应两种方法制备水杨酸糖酯;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。结果合成了5个β-构型的水杨酸糖酯,其中有3个的抗凝血活性和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,5个合成物的刺激性均有明显的降低。结论羧酸盐直接反应法制备水杨酸糖酯简便易行,优于相转移催化法:水杨酸糖酯类修饰可以提高抗凝血作用,降低刺激性。更多还原

【Abstract】 OBJECTIVE To prepare salicylic acid saccharide carboxylate and evaluate their Anticoagulant activity.METHOEDS The salicylic acid saccharide carboxylate were prepared through carboxylic acid-organic alkali and carboxylic salts,and the acetylated salicylic glucopyranose tetraacetate was synthesized by sequential elution;The structure of the products were identified by ~1H-NMR and IR,and the anticoagulant activity and anti-inflammation activities were respectively evaluated by the cutting tail in mice and the models of mice ear edema induced by xylene.RESULTS Fourβ-configuration and oneα-configuration salicylic acid saccharide carboxylate were prepared and three of them showed nearly the same bioactivies 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 methods of arboxylic salts and sequential elution were firstly respectively applied in the preparation of salicylic acid saccharide carboxylate, and the methods were operated easily and better than the methods of phase-transfer catalysis;The preparation of salicylic acid saccharide carboxylate could increase the anticoagulant activity of their corresponding primary drug..更多还原