环氧化酶-2/5-脂氧合酶双效抑制剂的抗炎研究进展  

Advances in Anti-Inflammatory Research on Dual Cyclooxygenase-2/5-Lipoxygenase Inhibitors

作　　者：蒋世云[1] 魏娜[1] 傅凤鸣[1] 

机构地区：[1]广西科技大学生物与化学工程学院,广西柳州545006

出　　处：《昆明理工大学学报（自然科学版）》2017年第4期73-78,共6页Journal of Kunming University of Science and Technology(Natural Science)

基　　金：广西自然科学基金项目(2013GXNSFAA019168)

摘　　要：对化学合成类以及天然产物类COX-2/5-LOX双效抑制剂在炎症方面的研究进展进行综述.COX-2/5-LOX双效抑制剂从酶活性和酶生成量两方面对COX-2/5-LOX进行抑制.研究报道表明,目前进入临床阶段的化学合成类化合物二叔丁基苯酚类、吡咯里嗪衍生物以及修饰型NSAIDs类化合物通过抑制COX-2/5-LOX活性从酶水平上发挥抗炎作用.天然产物提取液及单体化合物(黄酮类、多酚类、生物碱类、有机酸、萜类等化合物)既可通过调节NF-κB信号通路、p38MAPK信号通路抑制COX-2/5-LOX蛋白表达,减少COX-2/5-LOX生成量,又可通过氧自由基影响COX-2/5-LOX活性,对COX-2/5-LOX从基因水平和酶水平两方面进行抑制.In this paper,the chemical synthetic and natural products dual COX-2/5-LOX inhibitors in inflammation research progress are summarized.The dual inhibitor reduces the enzyme activity and enzyme production of COX-2/5-LOX.Reports of the clinical studies indicate that the chemical synthetic compounds ditert butyl phenol,pyrrole oxazine derivatives and the modification NSAIDs compounds inhibit COX-2/5-LOX activities,which induces anti-inflammatory activities on the enzyme levels.Natural product extracts and monomer compounds（flavonoids,polyphenols,alkaloids,organic acid,and terpenoids） not only suppress COX-2/5-LOX gene expression,reduce the COX-2/5-LOX production by adjusting NF-κB and p38 MAPK signal pathway,but also inhibit COX-2/5-LOX activities by reducing the ROS production.

关 键 词：COX-2/5-LOX双重抑制剂 作用机制 抗炎 

分 类 号：R971[医药卫生—药品]