The effects of anti-inflammatory drugs on prostaglandin production by rheumatoid synovial tissue |
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| Affiliation: | 1. Department of Medicine, Harvard Medical School and the Arthritis Unit of the Medical Services, Massachusetts General Hospital, Boston, Massachusetts 02114, USA;2. Graduate Department of Biochemistry, Brandeis University, Waltham, Massachusetts 02154, USA;1. Department of Pathology, Sapporo Medical University School of Medicine, South-1, West-17, Chuo-ku, Sapporo 060-8556, Japan;2. Department of Neurology, Sapporo Medical University School of Medicine, South-1, West-17, Chuo-ku, Sapporo 060-8556, Japan;3. Department of Neurology, Clinical Brain Research Laboratory, Toyokura Memorial Hall, Sapporo Yamano-ue Hospital, Japan;1. Organic Chemistry Division, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune 411008, India;2. Academy of Scientific and Innovative Research (AcSIR), New Delhi 110 025, India;1. Department of Zoology, College of Science, King Saud University, 11451 Riyadh, Saudi Arabia;2. Department of Zoology and Entomology, Faculty of Science, Helwan University, Cairo, Egypt;3. Department of Zoology, Faculty of Science, Beni-Suef University, Beni-Suef, Egypt;4. Transplantation Diagnostics and Cell Therapeutics, Heinrich-Heine-University, Duesseldorf, Germany;5. Computational Biology and Systems Biomedicine, Biodonostia Health Research Institute, San Sebastion, Spain;6. IKERBASQUE, Basque Foundation for Science, Bilbao, Spain;7. Department of Biology, Heinrich-Heine-University, Duesseldorf, Germany;8. Boehringer-Ingelheim, Biberach, Germany |
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| Abstract: | The effect of anti-inflammatory drugs on prostaglandin production by rheumatoid synovial tissue has been investigated. Synovial explants were maintained in tissue culture for periods up to six days and PGE2 concentrations in culture were determined by radioimmunoassay. The more potent nonsteroidal inhibitors of PGE2 production and their IC50 (μM) values were indomethacin 0.005, flufenamic acid 0.2, flurbiprofen 0.6, ibuprofen 2.0, naproxen 6.0, phenylbutazone 10.0, and aspirin 20.0. Drugs with weak or insignificant effects were hydroxychloroquin, acetaminophen, azathioprine, chloroquin, penicillamine, gold Na thiomalate, and Na salicylate. Glucocorticoids were potent inhibitors; dexamethasone 0.003, prednisolone 0.01, hydrocortisone 0.03; while mineralocorticoids deoxycorticosterone and aldosterone were inactive at 1.0 μM. There is a reasonably good correlation between the IC50 concentrations of the nonsteroidal inhibitors and their peak free plasma concentration achieved during therapy in man. Inhibition of prostaglandin synthesis may contribute to the effects of many but not all anti-inflammatory drugs. |
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