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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 progress in the research on chemical synthesis and the natural product COX-2/5-LOX double-effect inhibitor in inflammation was reviewed.COX-2/5-LOX double- -2 / 5-LOX.Recent studies have shown that the chemical compounds di-tert-butylphenols, pyrrolizine derivatives and modified NSAIDs entering clinical phase can inhibit the activity of COX-2/5-LOX Which can exert its anti-inflammatory activity at the level of enzyme.Extracts of natural products and monomeric compounds (flavonoids, polyphenols, alkaloids, organic acids, terpenoids and other compounds) can regulate NF-κB signaling pathway, p38MAPK signaling pathway LOX protein expression and COX-2/5-LOX production were reduced by oxygen free radicals and COX-2/5-LOX activity by COX-2 / Enzyme levels inhibit both.