Abramson S
New York University Medical Center, New York.
Curr Opin Rheumatol. 1991 Jun;3(3):336-40. doi: 10.1097/00002281-199106000-00002.
Nonsteroidal anti-inflammatory drugs have anti-inflammatory, analgesic, and antipyretic properties. Although most nonsteroidal anti-inflammatory drugs inhibit prostaglandin synthesis, these agents also have important pharmacologic actions unrelated to their effects on prostaglandins. Among these properties is the ability to inhibit the release of mediators of inflammation from neutrophils and macrophages. These effects are due to the ability of nonsteroidal anti-inflammatory drugs to intercalate into the lipid bilayer of the plasma membrane and thereby disrupt protein-protein and protein-lipid interactions critical for cell responses (eg, calcium translocations, membrane phospholipid turnover). Our data, for example, indicate that nonsteroidal anti-inflammatory drugs exert direct inhibitory actions at the regulatory GTP protein (G protein) within the plasma membrane. This exhibit examines the evidence for diverse mechanisms of action of nonsteroidal anti-inflammatory drugs including effects directed at the G protein as well as new evidence that nonsteroidal anti-inflammatory drugs regulate the expression of the cyclooxygenase enzyme at the level of gene transcription.
非甾体抗炎药具有抗炎、镇痛和解热特性。尽管大多数非甾体抗炎药抑制前列腺素合成，但这些药物也具有与其对前列腺素的作用无关的重要药理作用。其中包括抑制中性粒细胞和巨噬细胞释放炎症介质的能力。这些作用归因于非甾体抗炎药插入质膜脂质双层的能力，从而破坏对细胞反应（如钙转运、膜磷脂周转）至关重要的蛋白质-蛋白质和蛋白质-脂质相互作用。例如，我们的数据表明，非甾体抗炎药在质膜内的调节性GTP蛋白（G蛋白）上发挥直接抑制作用。本展览探讨了非甾体抗炎药多种作用机制的证据，包括针对G蛋白的作用以及非甾体抗炎药在基因转录水平调节环氧化酶表达的新证据。
