Journal ArticleDOI
New insights into the mode of action of anti-inflammatory drugs
John R. Vane,Regina M. Botting +1 more
TLDR
The constitutive cyclooxygenase-1 (COX-1) can thus be considered a “housekeeping” enzyme, in contrast to cyclo oxygenogenase-2 ( COX-2) which is activated by tissue damage.Abstract:
The discovery of a second cyclooxygenase has provided fresh impetus to the search for new anti-inflammatory drugs. The second enzyme is effectively absent from healthy tissues but its levels rise dramatically during inflammation. It can be induced in migratory cells by bacterial lipopolysaccharide, cytokines and growth factors. The constitutive cyclooxygenase-1 (COX-1) can thus be considered a "housekeeping" enzyme, in contrast to cyclooxygenase-2 (COX-2) which is activated by tissue damage. Both enzymes have a molecular weight of around 70 kDa and similar Km and Vmax values for their reaction with arachidonic acid. Several non steroid anti-inflammatory drugs which have more than 1,000 fold selectivity for COX-2 over COX-1 are in the early stages of drug development.read more
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Curcumin: From ancient medicine to current clinical trials
TL;DR: Curcumin exhibits great promise as a therapeutic agent, and is currently in human clinical trials for a variety of conditions, including multiple myeloma, pancreatic cancer, myelodysplastic syndromes, colon cancer, psoriasis and Alzheimer’s disease.
Journal ArticleDOI
Phytochemistry: ibuprofen-like activity in extra-virgin olive oil.
Gary K. Beauchamp,Russell Keast,Russell Keast,Diane W. Morel,Jianming Lin,Jana Pika,Qiang Han,Chi-Ho Lee,Chi-Ho Lee,Amos B. Smith,Amos B. Smith,Paul A. S. Breslin +11 more
TL;DR: It is shown that newly pressed extra-virgin olive oil contains oleocanthal, a compound whose pungency induces a strong stinging sensation in the throat, not unlike that caused by solutions of the non-steroidal anti-inflammatory drug ibuprofen, which is an indicator of a shared pharmacological activity.
Journal ArticleDOI
Inhibition of cyclo-oxygenase 2 expression in colon cells by the chemopreventive agent curcumin involves inhibition of NF-kappaB activation via the NIK/IKK signalling complex.
Simon M. Plummer,Karen A. Holloway,Margaret M. Manson,Rebecca Jl Munks,Allard Kaptein,Stuart N. Farrow,Lynne M. Howells +6 more
TL;DR: Curcumin inhibits COX2 induction by the colon tumour promoters, tumour necrosis factor α or fecapentaene-12, making curcumin an important candidate for consideration in colon cancer prevention.
Journal ArticleDOI
Anti-inflammatory drugs and their mechanism of action
John R. Vane,Regina M. Botting +1 more
TL;DR: Selective COX-2 inhibitors may demonstrate new important therapeutic benefits as anticancer agents, as well as in preventing premature labor and perhaps even retarding the progression of Alzheimer's disease.
Journal ArticleDOI
Gastric Mucosal Defense and Cytoprotection: Bench to Bedside
TL;DR: Conditions in which mucosal injury is directly related to impairment in mucosal defense are discussed, focusing on disorders with important clinical sequelae: nonsteroidal anti-inflammatory drug (NSAID)-associated injury, which is primarily related to inhibition of cyclooxygenase-mediated PG synthesis, and stress-related mucosal disease (SRMD), which occurs with local ischemia.
References
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TL;DR: Experiments with guinea-pig lung suggest that some of the therapeutic effects of sodium salicylate and aspirin-like drugs are due to inhibition of the synthesis of prostaglandins.
Journal Article
Collaborative overview of randomized trials of antiplatelet therapy .1. prevention of death, myocardial-infarction, and stroke by prolonged antiplatelet therapy in various categories of patients
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TL;DR: There was no appreciable evidence that either a higher aspirin dose or any other antiplatelet regimen was more effective than medium dose aspirin in preventing vascular events, so in each of the four main high risk categories overall mortality was significantly reduced.
Journal ArticleDOI
Inhibition of NF-kappa B by sodium salicylate and aspirin
Elizabeth Kopp,Sankar Ghosh +1 more
TL;DR: The anti-inflammatory drugs sodium salicylate and aspirin inhibited the activation of NF-kappa B, which further explains the mechanism of action of these drugs.
Journal ArticleDOI
Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mrna splicing
TL;DR: A distinguishing feature of src-inducible prostaglandin synthase mRNA is its low abundance in nonproliferating chicken embryo fibroblasts and its relatively high abundance in src-transformed cells.
Journal ArticleDOI
Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase
TL;DR: BF 389, an experimental drug currently being tested in humans, was the most potent and most selective inhibitor of COX-2 in intact cells, indicating there are clear pharmacological differences between the two enzymes.