(Circulation. 2000;102:2022.)
© 2000 American Heart Association, Inc.
Editorial |
Aspirin and Salicylate
An Old Remedy With a New Twist
From the Vascular Biology Research Center and Division of Hematology, University of Texas-Houston Health Science Center, Houston, Texas.
Correspondence to Kenneth K. Wu, Division of Hematology, University of Texas–Houston Medical School, 6431 Fannin St, Houston, TX 77030. E-mail Kenneth.K.Wu@uth.tmc.edu
Key Words: Editorials • aspirin • salicylates
Salicylic acid was identified in willow bark extracts as an active anti-inflammatory compound over a century ago. Because of its bitter taste, chemical derivatives of salicylic acid (2-hydroxybenzoic acid) were synthesized and tested. Acetylsalicylic acid (aspirin) eliminated the bitter taste but retained the anti-inflammatory action, and it was introduced for treating human maladies >100 years ago. It has remained the most commonly used drug for relieving pain, inflammatory symptoms, and fever. Aspirin also has established efficacy for preventing myocardial infarction and ischemic stroke, as well as for treating acute myocardial infarction.1 Furthermore, recent epidemiological studies indicate that aspirin use is accompanied by a reduction in cancers, especially colon cancer.2
How does a simple compound exert such broad therapeutic actions? Vane and Botting3 4 discovered that aspirin and nonsteroidal anti-inflammatory drugs inhibit the synthesis of proinflammatory prostaglandin E2. Subsequently, others demonstrated that aspirin inhibits cyclooxygenase-1 (COX-1) activity by acetylating serine 530, which is located close to the active site (tyrosine 385 of COX-1), and that acetylation of this serine residue hinders the access of arachidonic acid to the active site.5 6 Aspirin inhibits COX-2 by a similar mechanism but is less potent7 because the substrate channel of COX-2 is larger and more flexible than that of COX-1.8 The therapeutic efficacy of aspirin in myocardial infarction and ischemic stroke has been clearly attributed to its inhibition of platelet COX-1 activity.1 In contrast, the mechanisms by which aspirin and salicylate exert their anti-inflammatory and antineoplastic actions are less clear.
Such actions were attributed to
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