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Cyclooxygenase isoforms in health and disease

机译：环氧合酶同工型在健康和疾病中的作用

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Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) have long been used for the treatment of pain and inflammation owing to their inhibitory effects on cyclooxygenase (COX). Ever since NSAIDs have been in use, multiple adverse effects have been noted. Assessment of many of these effects has been complicated due to the discovery of multiple splice variants of the COX gene, greater array of COX and specific COX-2 inhibitor availability. The effect of these drugs on COX cannot be readily explained. This has sparked a new field of investigation on splice variants of COX and effects of COX inhibitors. This review summarizes our current understanding of the role of cyclooxygenase in health and disease. Introduction The mechanism of action of NSAIDs has long been proposed based on their inhibition of prostaglandin biosynthesis, enzyme cyclooxygenase (COX or prostaglandin H2 synthase). Two decades after COX discovery the existence of at least two COX isoforms; COX-1 and COX-2 were demonstrated in 1990 (Figure 1). Currently the research is focused on developing safer NSAIDs based on their mechanisms of action and physiological roles in the pathogenesis of inflammation. New classes of COX-2 selective inhibitors have entered the worldwide market. These new medications offer safer alternatives to NSAIDs in terms of gastrointestinal safety; however, toxicological concerns regarding their renal and cardiovascular safety remain. These COX-2 specific inhibitors benefit arthritic patients, slow down tumor growth, delay the birth process, and impede degenerative changes associated with Alzheimer’s disease and Parkinson’s disease. There has been much speculation in the field on the possibility of a third COX isoform COX-3, that is potently inhibited by some NSAIDs. Thus, inhibition of COX-3 could represent an additional mechanism by which these drugs decrease pain and possibly fever.
机译：由于非甾体类抗炎药对环氧合酶（COX）的抑制作用，长期以来一直用于治疗疼痛和炎症。自从使用NSAID以来，已经注意到了多种不良反应。由于发现了COX基因的多个剪接变体，更多的COX阵列和特定的COX-2抑制剂可利用性，因此许多此类效应的评估变得十分复杂。这些药物对COX的作用尚不能轻易解释。这引发了关于COX的剪接变体和COX抑制剂作用的新研究领域。这篇综述总结了我们目前对环氧合酶在健康和疾病中的作用的理解。引言基于NSAID抑制前列腺素生物合成，酶环氧合酶（COX或前列腺素H2合酶）的作用，长期以来一直被提出。发现COX后二十年，至少存在两种​​COX同工型。 1990年证明了COX-1和COX-2（图1）。目前，研究基于其作用机制和炎症发病机理中的生理作用，致力于开发更安全的NSAID。新型的COX-2选择性抑制剂已进入全球市场。这些新药在胃肠道安全性方面为NSAID提供了更安全的替代品。然而，关于其肾脏和心血管安全的毒理学问题仍然存在。这些特定于COX-2的抑制剂对关节炎患者有益，可延缓肿瘤生长，延迟生育过程并阻止与阿尔茨海默氏病和帕金森氏病相关的退行性改变。在该领域中，已经有许多关于第三种COX同工型COX-3被某些NSAID有效抑制的可能性的猜测。因此，抑制COX-3可能代表了这些药物减轻疼痛甚至发烧的另一种机制。

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