Title:Cyclooxygenase-2 Inhibitors as a Therapeutic Target in Inflammatory Diseases
Volume: 26
Issue: 18
关键词:
环氧合酶，COX抑制剂，炎症，白介素，天然化合物。 前列腺素。
摘要: Inflammation plays a crucial role in the development of many complex diseases
and disorders including autoimmune diseases, metabolic syndrome, neurodegenerative diseases,
and cardiovascular pathologies. Prostaglandins play a regulatory role in inflammation.
Cyclooxygenases are the main mediators of inflammation by catalyzing the initial step of arachidonic
acid metabolism and prostaglandin synthesis. The differential expression of the constitutive
isoform COX-1 and the inducible isoform COX-2, and the finding that COX-1 is the
major form expressed in the gastrointestinal tract, lead to the search for COX-2-selective
inhibitors as anti-inflammatory agents that might diminish the gastrointestinal side effects of
traditional non-steroidal anti-inflammatory drugs (NSAIDs). COX-2 isoform is expressed
predominantly in inflammatory cells and decidedly upregulated in chronic and acute inflammations,
becoming a critical target for many pharmacological inhibitors. COX-2 selective inhibitors
happen to show equivalent efficacy with that of conventional NSAIDs, but they have
reduced gastrointestinal side effects. This review would elucidate the most recent findings on
selective COX-2 inhibition and their relevance to human pathology, concretely in inflammatory
pathologies characterized by a prolonged pro-inflammatory status, including autoimmune
diseases, metabolic syndrome, obesity, atherosclerosis, neurodegenerative diseases, chronic
obstructive pulmonary disease, arthritis, chronic inflammatory bowel disease and cardiovascular
pathologies.
