【摘要】 目的　考察呋咱氮氧化物偶联的双氯芬酸衍生物的抗炎活性与胃肠道副作用的关系以及其 NO的释放情况。方法　采用小鼠耳二甲苯致炎和角叉菜胶致大鼠足跖肿胀两种实验模型对系列化合物进行了抗炎活性初步筛选 ,并对抗炎活性较好的化合物进行了胃肠道副作用的观察及 NO体内外释放量的测定。结果　抗炎活性较好的化合物其胃肠道副作用明显轻于双氯芬酸 ,也轻于已知的非甾体抗炎药 ,且 3 h体内均有明显的NO释放。结论　 NO的引入能有效对抗非甾体抗炎药所致的胃肠道副作用。更多还原

【Abstract】 AIM The purpose is to study the relationship in NO-NSAIDs be tween the anti-i nflammatory activities and the gastrointestinal (GI) side effects as well as NO release. METHODS Two screening models were used to determine the anti-inflammatory effects of the tested drugs. One is xylene-induced mice ear swelling. The other is carrageenan-induced rat paw edema. Then the effects of the target compounds on rats′ GI system were examined. In addition, the experi ments for qualitative detection of occult blood in feces were made, and some he matology indexes (red blood cell count and hemoglobin content) was also determi ned. These studies were used to examine the extent of GI tract hemorrhage. The q u antity of NO release \%in vitro\% and \%in vivo\% was determined too. RES ULTS\ A nti-inflammatory activities are greater with the GI side effects small er. The GI side effects of all the target compounds with greater anti-inflammat ory activities were less than DC and Nitrofenac, and NO release \%in vivo\% at 3 h increased significantly. CONCLUSION\ The release of NO c an resist GI side effects caused by NSAIDs. Accordingly, the favorable evidences are provided for the further studies of the NO-NSAIDs.更多还原