Lipsky P E
Rheumatic Diseases Division and the Harold C. Simmons Arthritis Research Center, The University of Texas Southwestern Medical Center at Dallas, USA.
Am J Orthop (Belle Mead NJ). 1999 Mar;28(3 Suppl):8-12.
Animal and human data demonstrate that cyclooxygenase (COX)-2 upregulation in osteoarthritis and rheumatoid arthritis is associated with the pain and inflammation of the disease state. The COX-1 isoform, however, is a constitutive enzyme with homeostatic functions. Unlike conventional nonsteroidal anti-inflammatory drugs, which inhibit both forms of the COX enzyme, celecoxib inhibits COX-2 preferentially to COX-1 in vitro. Celecoxib reversed signs of arthritis and pain in an animal model as effectively as indomethacin. Data from murine studies as well as in vitro and epidemiologic data indicate that COX-2 plays a role in the development of colon cancer, and epidemiologic studies also suggest that COX inhibition can slow the progression of Alzheimer's disease.
动物和人体数据表明,骨关节炎和类风湿性关节炎中环氧合酶(COX)-2的上调与疾病状态下的疼痛和炎症相关。然而,COX-1同工型是一种具有稳态功能的组成型酶。与抑制两种形式COX酶的传统非甾体抗炎药不同,塞来昔布在体外对COX-2的抑制作用优先于COX-1。在动物模型中,塞来昔布逆转关节炎和疼痛症状的效果与吲哚美辛一样有效。来自小鼠研究以及体外和流行病学的数据表明,COX-2在结肠癌的发生中起作用,并且流行病学研究还表明,COX抑制可减缓阿尔茨海默病的进展。