Folco G C
Istituto di Scienze Farmacologiche, Università di Milano, Italy.
Ital J Gastroenterol. 1996 Dec;28 Suppl 4:28-9.
Two isoforms of cyclooxygenase (COX) are described: COX-1 is a constitutive enzyme and is widely expressed in most tissues, COX-2 is an inducible enzyme and is abundant throughout the gastrointestinal tract. Expression of COX-2 can be induced locally by inflammatory stimuli and appears coincident with local prostaglandin (PG) production. Currently available non-steroidal antiinflammatory drugs (NSAIDs) are widely used for the treatment of inflammatory diseases; however, significant side-effects due to inhibition of COX-1 limit their use. Inhibitors of COX-2 are as active as non-selective NSAIDs and inhibit PG synthesis in inflammatory cells. In contrast to other NSAIDs, selective COX-2 inhibitors do not cause ulcers in the stomach or intestine.
环氧化酶（COX）有两种同工型：COX-1是一种组成型酶，在大多数组织中广泛表达；COX-2是一种诱导型酶，在整个胃肠道中大量存在。COX-2的表达可由炎症刺激局部诱导，且与局部前列腺素（PG）的产生同时出现。目前可用的非甾体抗炎药（NSAIDs）广泛用于治疗炎症性疾病；然而，由于抑制COX-1而产生的显著副作用限制了它们的使用。COX-2抑制剂与非选择性NSAIDs一样有效，并且能抑制炎症细胞中的PG合成。与其他NSAIDs不同，选择性COX-2抑制剂不会导致胃或肠道溃疡。
