ZLJ-601抗炎作用及其机制研究  

Anti-inflammatory effect and mechanism of compound ZLJ-601

作　　者：黄秋菊[1] 季晖[1] 赖宜生[2] 张奕华[2] 李立文[1] 敖桂珍[3] 

机构地区：[1]中国药科大学药理学教研室,南京210009 [2]中国药科大学新药研究中心,南京210009 [3]苏州大学药学院,苏州215006

出　　处：《中国药科大学学报》2008年第4期333-337,共5页Journal of China Pharmaceutical University

基　　金：江苏省普通高校研究生科研创新计划资助项目~~

摘　　要：目的：考察对甲磺酰基苯乙烯环酮类衍生物ZLJ-601对大鼠急性胸膜炎的作用以及对体外培养巨噬细胞炎症细胞因子释放和吞噬功能的影响，对其抗炎作用机制进行初步研究。方法：将角叉菜胶注入大鼠胸膜腔造成急性炎症模型，观察药物对急性炎症渗出、白细胞游出、炎症介质（PGE2、NO）释放及脂质过氧化产物（MDA）生成的影响。用脂多糖刺激原代小鼠腹腔巨噬细胞，观察药物对其释放细胞因子（IL-1）及NO的影响；利用巨噬细胞吞噬中性红实验考察药物对巨噬细胞吞噬功能的影响。结果：ZLJ-601能显著地抑制急性炎症中的渗出、白细胞游走和PGE。NO释放，能减少MDA的生成；ZLJ-601在1×10^-5、1×10^-6mol／L均能抑制脂多糖刺激的巨噬细胞NO的释放，在1×10^-5mol／L能抑制IL-1的释放；在1×10^-5-1×10^-7mol／L均能增强巨噬细胞吞噬功能。结论：ZLJ-601有较强的抗炎活性，作用机制包括抑制炎症细胞因子及其炎症介质的释放和增强巨噬细胞吞噬功能。Aim： To investigate the anti-inflammatory effects of compound ZLJ-601 in the carrageenan-induced rat pleurisy model and to underline the mechanisms on in vitro cultured mouse peritoneal macrophages. Methods： The carrageenan-induced rat pleurisy model was applied to investigate the in vivo anti-inflammatory effects of ZLJ- 601 by detecting the volume of exudates, leukoeytes efflux, the protein content, the releases of inflammatory medi- ators PGE2 and NO, and MDA concentration in the exudates. Lipopolysaccharide （LPS）-induced mouse pe- ritoneal macrophages were used to study if compound ZLJ-601 could simultaneously inhibit the production of pro- inflammatory cytokine IL-1 and NO. Furthermore, mouse peritoneal macrophages were used to find out if ZLJ-601 could enhance phagoeytosis of the macrophages. Results： ZLI-601 exhibited comparable anti-inflammatory effects with positive drug equimolar CI-1004 in terms of the inhibitions on the exudation and leukocytes efflux, the releases of inflammatory mediator （PGE2, NO） and the production of MDA. On LPS-induced mouse peritoneal macrophages, ZLJ-601 signifieandy inhibited NO production at 1 × 10^-5 mol/L and 1× 10^-6 and remarkably re- duced IL-1 production at 1 ×10^-6 mol/L. ZLJ-601 also significantly elevated phagocytosis of mouse macrophages at 1 × 10^-5,1×10^-6, and 1 × 10^-7 mol/L. Conclusion： ZLJ-601 has a profound anti-inflammatory action against the acute inflammations, and the suppression in the production of pro-inflammatory cytokine and mediators in inflammatory cells may partially account for its anti-inflammatory mechanisms.

关 键 词：ZLJ-601 胸膜炎 巨噬细胞 抗炎作用 吞噬作用 

分 类 号：R96[医药卫生—药理学]