水杨酸-g-壳聚糖衍生物的合成及药效研究  

Synthesis and bioactivies of salicylic acid-g-chitosan derivatives

作　　者：武雪芬[1] 李伟[1] 王磊[1] 胡建梅[1] 李桂兰[2] 

机构地区：[1]河南中医学院,河南郑州450008 [2]郑州大学化学系,河南郑州450052

出　　处：《药学学报》2007年第5期481-487,共7页Acta Pharmaceutica Sinica

基　　金：河南省自然科学基金资助项目(0611045900).

摘　　要：制备水杨酸-g-壳聚糖载体衍生物,观察两者在药效上的协同和互补作用。通过二甲苯致小鼠耳肿胀实验观察水杨酸与壳聚糖抗炎的协同作用;通过小鼠扭体实验和热板痛实验观察衍生物的镇痛作用;通过胃黏膜形态学变化评价壳聚糖与水杨酸的互补作用。实验结果表明,水杨酸-g-壳聚糖衍生物外用抗炎作用优于水杨酸、壳聚糖和皮炎平,内服优于阿司匹林;即时镇痛作用低于阿司匹林,长效镇痛作用与阿司匹林相近;对胃黏膜的刺激性远远低于阿司匹林;水杨酸-g-壳聚糖衍生物具有抗炎协同作用和药效互补作用。To prepare the derivatives of salicylic acid-g-chitosan and study their synergistic and complementary actions, the synergism of anti-inflammatory action of the derivatives was investigated with the experiments of xylene-induces mice ear edema, the analgesic activities by the tartaric emetic-induced mice twist test and the hot-plate test, and the complementary effects between salicylic acid and chitosan through morphological changes of stomach mucous membrane of rat, separately. The anti-lnflammatory activities of salicylic acid-g-chitosan derivatives for anti-inflammatory activities were more potent than that of salicylic acid and chitosan and dexamethasone cream in external use, and more potent than that of aspirin orally. However, immediate analgesic activity of the derivatives was lower than that of aspirin and persistent activity was similar as that of aspirin. And the stomach mucous membrane morphology change of the derivatives was much milder than that of aspirin. The salicylic acid grafted chitosan derivatives showed synergistic and complementary effect on the anti-inflammatory and analgesic activities and so on.

关 键 词：水杨酸 壳聚糖 接枝 抗炎 镇痛 胃黏膜刺激性 

分 类 号：R916[医药卫生—药学]