Biomaterial Database

Biochemical pharmacology of nonsteroidal anti-inflammatory drugs. 1998

K K Wu

Vascular Biology Research Center and Division of Hematology, University of Texas-Houston Medical Center, 77030, USA. kkwu@heart.med.uth.tmc.edu

Aspirin and conventional nonsteroidal anti-inflammatory drugs are nonselective inhibitors of cyclooxygenase-1 (COX-1) and COX-2 enzymes. Two classes of selective COX-2 inhibitors: (1) sulfonamides, such as L-745,337, and (2) tricyclic methyl sulfone derivatives, such as SC58125, have been developed. X-ray crystal structures of COX-1 and COX-2 have provided valuable information regarding the structural basis for their COX-2 selectivity. These compounds have less gastrointestinal complications in animal experiments. Their clinical efficacy and side-effects are being evaluated. Salicylate has very weak activity against either COX isoform and yet possesses anti-inflammatory actions. Recent studies indicate that it suppresses the expression of genes involved in inflammation. These activities may provide a plausible explanation for the pharmacological dilemma and, furthermore, may represent novel mechanisms for controlling inflammation.

UI	MeSH Term	Description	Entries
D007527	Isoenzymes	Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.	Alloenzyme,Allozyme,Isoenzyme,Isozyme,Isozymes,Alloenzymes,Allozymes
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000894	Anti-Inflammatory Agents, Non-Steroidal	Anti-inflammatory agents that are non-steroidal in nature. In addition to anti-inflammatory actions, they have analgesic, antipyretic, and platelet-inhibitory actions. They act by blocking the synthesis of prostaglandins by inhibiting cyclooxygenase, which converts arachidonic acid to cyclic endoperoxides, precursors of prostaglandins. Inhibition of prostaglandin synthesis accounts for their analgesic, antipyretic, and platelet-inhibitory actions; other mechanisms may contribute to their anti-inflammatory effects.	Analgesics, Anti-Inflammatory,Aspirin-Like Agent,Aspirin-Like Agents,NSAID,Non-Steroidal Anti-Inflammatory Agent,Non-Steroidal Anti-Inflammatory Agents,Nonsteroidal Anti-Inflammatory Agent,Anti Inflammatory Agents, Nonsteroidal,Antiinflammatory Agents, Non Steroidal,Antiinflammatory Agents, Nonsteroidal,NSAIDs,Nonsteroidal Anti-Inflammatory Agents,Agent, Aspirin-Like,Agent, Non-Steroidal Anti-Inflammatory,Agent, Nonsteroidal Anti-Inflammatory,Anti-Inflammatory Agent, Non-Steroidal,Anti-Inflammatory Agent, Nonsteroidal,Anti-Inflammatory Analgesics,Aspirin Like Agent,Aspirin Like Agents,Non Steroidal Anti Inflammatory Agent,Non Steroidal Anti Inflammatory Agents,Nonsteroidal Anti Inflammatory Agent,Nonsteroidal Anti Inflammatory Agents,Nonsteroidal Antiinflammatory Agents
D012459	Salicylates	The salts or esters of salicylic acids, or salicylate esters of an organic acid. Some of these have analgesic, antipyretic, and anti-inflammatory activities by inhibiting prostaglandin synthesis.	Salicylate,Salicylic Acids,Acids, Salicylic
D016861	Cyclooxygenase Inhibitors	Compounds or agents that combine with cyclooxygenase (PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES) and thereby prevent its substrate-enzyme combination with arachidonic acid and the formation of eicosanoids, prostaglandins, and thromboxanes.	Cyclo-Oxygenase Inhibitor,Cyclooxygenase Inhibitor,Prostaglandin Endoperoxide Synthase Inhibitor,Prostaglandin Endoperoxide Synthase Inhibitors,Prostaglandin Synthase Inhibitor,Prostaglandin Synthase Inhibitors,Prostaglandin Synthesis Antagonist,Prostaglandin Synthesis Antagonists,Cyclo-Oxygenase Inhibitors,Inhibitors, Cyclo-Oxygenase,Inhibitors, Cyclooxygenase,Inhibitors, Prostaglandin Synthase,Inhibitors, Prostaglandin-Endoperoxide Synthase,Antagonist, Prostaglandin Synthesis,Antagonists, Prostaglandin Synthesis,Cyclo Oxygenase Inhibitor,Cyclo Oxygenase Inhibitors,Inhibitor, Cyclo-Oxygenase,Inhibitor, Cyclooxygenase,Inhibitor, Prostaglandin Synthase,Inhibitors, Cyclo Oxygenase,Inhibitors, Prostaglandin Endoperoxide Synthase,Synthase Inhibitor, Prostaglandin,Synthesis Antagonist, Prostaglandin
D020156	Salicylic Acid	A compound obtained from the bark of the white willow and wintergreen leaves. It has bacteriostatic, fungicidal, and keratolytic actions.	2-Hydroxybenzoic Acid,o-Hydroxybenzoic Acid,ortho-Hydroxybenzoic Acid,2 Hydroxybenzoic Acid,Acid, 2-Hydroxybenzoic,Acid, Salicylic,Acid, o-Hydroxybenzoic,Acid, ortho-Hydroxybenzoic,o Hydroxybenzoic Acid,ortho Hydroxybenzoic Acid