Ex vivo assay to determine the cyclooxygenase selectivity of non-steroidal anti-inflammatory drugs

British Journal of Pharmacology

Volumn 126, Issue 8, 1999, Pages 1824-1830

  Giuliano, Francesco ^a   Warner, Timothy D ^a  

^a QUEEN MARY UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

COX 1; COX 2; Ex vivo evaluation; NSAIDs activation; NSAIDs inactivation; NXAIDs selectivity

Indexed keywords

6 (2,4 DIFLUOROPHENYLTHIO) 5 METHANESULFONAMIDO 1 INDANONE; ACETYLSALICYLIC ACID; DICLOFENAC; INTERLEUKIN 1BETA; NIMESULIDE; NONSTEROID ANTIINFLAMMATORY AGENT; PRODRUG; PROSTAGLANDIN SYNTHASE; PROSTANOID; SALICYLIC ACID; SULINDAC; THIOBUTABARBITAL;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG ACTIVATION; DRUG METABOLISM; DRUG SELECTIVITY; ENZYME INACTIVATION; ENZYME INHIBITION; HUMAN; HUMAN CELL; INTRAPERITONEAL DRUG ADMINISTRATION; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PRIORITY JOURNAL; PROSTAGLANDIN SYNTHESIS INHIBITION; RAT;

ANALGESICS; ANIMALS; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ASPIRIN; BLOOD PLATELETS; BLOOD PRESSURE; CARCINOMA; CYCLOOXYGENASE 1; CYCLOOXYGENASE 2; CYCLOOXYGENASE 2 INHIBITORS; CYCLOOXYGENASE INHIBITORS; DICLOFENAC; DINOPROSTONE; HUMANS; INDANS; ISOENZYMES; MALE; MEMBRANE PROTEINS; PROSTAGLANDIN-ENDOPEROXIDE SYNTHASES; RATS; RATS, WISTAR; SALICYLATES; SUBSTRATE SPECIFICITY; SULFONAMIDES; SULINDAC; THROMBOXANE B2; TUMOR CELLS, CULTURED;

EID: 0032927066     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702518     Document Type: Article

References (35)

1. Bernareggi, A. (1993). The pharmacokinetics profile of nimesulide in healthy volunteers. Drugs, 46 (suppl. 1), 64-72.
2. Brideau, C., Kargman, S., Liu, S., Dallob, A.L., Ehrich, E.W., Rodger, I.W. & Chan, C.C. (1996). A human whole blood assay for clinical evaluation of biochemical efficacy of cyclooxygenase inhibitors. Inflamm. Res., 45, 68-74.
3. Brouwers, J.R.B.J. & De Smet, P.A.G.M. (1994). Pharmakokinetic-pharmacodinamic drug interactions with nonsteroidal anti-inflammatory drugs. Clin. Pharmacokinet., 27, 462-485.
4. Chan, C.-C., Boyce, S., Brideau, C., Ford-Hutchinson, A.W., Gordon, R., Guay, D., Hill, R.G., Li, C.-S., Mancini, J., Penneton, M., Prasit, P., Rasori, R., Riendeau, D., Roy, P., Tagari, P., Vickers, P., Wong, E. & Rodger, W. (1995). Pharmacology of a selective cyclooxygenase-2 inhibitor, L-745,337: A novel nonsteroidal anti-inflammatory agent with an ulcerogenic sparing effect in rat and nonhuman primate stomach. J. Pharmacol. Exp. Therap., 274, 1531-1537.
5. Cromlish, W.A. & Kennedy, B.P. (1996). Selective inhibition of cyclooxygenase-1 and -2 using intact insect cell assay. Biochem. Pharmacol., 52, 1777-1785.
6. Famaey, J.P. (1997). In vitro pharmacological evidence of selective cyclooxygenase-2 inhibition by nimesulide: An overview. Inflamm. Res., 46, 437-446.
7. 2 synthase (cyclooxygenase) in human monocytes. J. Biol. Chem., 265, 16737-16740.
8. Garcia Rodriguez, L.A., Cattaruzzi, C., Troncon, M.G., Agostinis, L. (1998). Risk of hospitalization for upper gastrointestinal tract bleeding associated with ketorolac, other nonsteroidal anti-inflammatory drugs, calcium antagonists, and other antihypersensitive drugs. Arch. Intern. Med., 158, 33-39.
9. Henry, D., Lim, L.L.-Y., Garcia Rodriguez, L.A., Perez Gutthann, S., Carson, J.L., Griffin, M., Savage, R., Logan, R., Moride, Y., Hawkey, C., Hill, S., Fries, J.T. (1996). Variability in risk of gastrointestinal complications with individual non-steroidal anti-inflammatory drugs: Results of a collaborative meta-analysis. BMJ, 312, 1563-1566.
10. Herschman, H.R. (1996). Prostaglandin synthase 2. Biochim. Biophis. Acta, 1299, 125-140.
11. Higgs, G.A., Salmon, J.A., Henderson, B. & Vane, J.R. (1987). Pharmacokinetics of aspirin and salicylate in relation to inhibition of arachidonate cyclooxygenase and antiinflammatory activity. Proc. Natl. Acad. Sci. USA. 84, 1417-1420.
12. Kujubu, D.A., Fletcher, B.S., Varnum, B.C., Lim, R.W., Herschman, H.R. (1991). TIS10, a phorbol ester tumor promoter-inducible mRNA from Swiss 3T3 cells, encodes a novel prostaglandin synthase/cyclooxygenase homologue. J. Biol. Chem., 266, 12866-12872.
13. Kwan, K.C. & Duggan, D.E. (1977). Pharmakokinetics of sulindac. Acta. Rheumatol. Belg., 1, 168-178.
14. Lee, S.H., Soyoola, E., Chanmugam, P., Hart, S., Sun, W., zhong, H., Liou, S., Simmons, D.L. & Hwang, G. (1992). Selective expression of mitogen-inducible cyclooxygenase in macropahges stimulated with lipopolysaccharide. J. Biol. Chem., 267, 25934-25938.
15. Marini, U. & Spotti, D. (1993). Gastric tolerability of nimesulide. A double-blind comparison of 2 oral dosage regimens and placebo. Drugs, 46 (suppl. 1), 249-252.
16. Masferr, J.L., Zweifel, B.S., Seibert, K., Needleman, P. (1990). Selective regulation of cellular cyclooxygenase by dexamethasone and endotoxin in mice. J. of Clin. Invest., 86, 1375-1379.
17. Meade, E.A., Smith, W.L. & Dewitt, D.L. (1993). Differential inhibition of prostaglandin endoperoxide synthase (cyclooxygenase) isozymes by aspirin and other non-steroidal antiinflammatory drugs. J. Biol. Chem., 268, 6610-6614.
18. Mitchell, J.A., Akarasereenont, P., Thiemermann, C., Flower, R.J. & Vane, J.R. (1993). Selectivity of nonsteroidal antiinflammatory drugs as inhibitors of constitutive and inducible cyclooxygenase. Proc. Natl. Acad. Sci. USA, 90, 11693-11697.
19. Mitchell, J.A., Belvisi, M.G., Akarasereenont, P., Robbins, R.A., Known, O.-J., Croxtall, J., Barnes, P.J. & Vane, J.R. (1994). Induction of cyclo-oxygenase-2 by cytokines in human pulmonary epithelial cells: Regulation by dexamethasone. Br. J. Pharmacol., 113, 1008-1014.
20. Mitchell, J.A., Saunders, M., Barnes, P.J., Newton, R. & Belvisi, M.G. (1997). Sodium salicylate inhibits cyclo-oxygenase-2 activity independently of transcription factor (nuclear factor κB) activation: Role of arachidonic acid. Mol. Pharmacol., 51, 907-912.
21. Moncada, S., Gryglewski, R., Bunting, S. & Vane, J.R. (1976). An enzyme isolated from arteries transforms prostaglandin endoperoxides to an unstable substance that inhibits platelet aggregation. Nature (London), 263, 663-665.
22. O'Banion, M.K., Sadowski, H.B., Winn, v. & Young, D.A. (1991). A serum- and glucocorticoid-regulated 4-kilobase mRNA encodes a cyclooxygenase-related protein. J. Biol. Chem., 266, 23261-23267.
23. O'Banion, M.K., Winn, V.D. & Young, D.A. (1992). cDNA cloning and functional activity of a glucocortocoid-regulated inflammatory cyclooxygenase. Proc. Natl. Acad. Sci. USA, 89, 4888-4892.
24. Patrignani, P., Panara, M.R., Greco, A., Fusco, O., Natoli, C., Iacobelli, S., Cipollone, F., Ganci, A., Créminon, C., Maclouf, J. & Patrono, C. (1994). Biochemical and pharmacological characterisation of the cyclooxygenase activity of human blood prostaglandin endoperoxide synthases. J. Pharmacol. Exp. Therap., 271, 1705-1712.
25. Patrignani, P., Panara, M.R., Sciulli, M.G., Santini, G., Renda, G. & Patrono, C. (1997). Differential inhibition of human prostaglandin endoperoxide synthase-1 and -2 by nonsteroidal anti-inflammatory drugs. J. Phisiol. Pharmacol., 48, 623-631.
26. Raz, A., Wyche, A., Siegel, N. & Needleman, P. (1988). Regulation of fibroblast cyclooxygenase synthesis by interleukin-1. J. Biol. Chem., 263, 3022-3025.
27. Vane, J.R. (1971). Inhibition of prostaglandin synthesis as a mechanism of action for the aspirin-like drugs. Nature (London), 231, 232-235.
28. Vane, J.R., Bakhle, Y.S. & Botting, R.M. (1998). Cyclooxygenases 1 and 2. Annu. Rev. Pharmacol. Toxicol., 38, 97-120.
29. Warrington, S.J., Ravic, M. & Dawnay, A. (1993). Renal tolerabilily of repeated doses of nimesulide in normal subjects. Drugs, 46 (suppl. 1), 263-269.
30. Whittle, B.J.R., Higgs, G.A., Eakins, K.E., Moncada, S. & Vane, J.R. (1980). Selective inhibition of prostaglandin production in inflammatory exudates and gastric mucosa. Nature (London), 284, 271-273.
31. Willis, J.V., Kendall, M.J., Flinn, R.M., Thornhill, D.P. & Welling, P.G. (1979). The pharmacokinetics of diclofenac sodium following intravenous and oral administration. Eur. J. Clin. Pharmacol., 16, 405-410.
32. Wong, W.Y.L. & Richards, J.S. (1991). Evidence for two antigenically distinct molecular weight variants of prostaglandin H synthase in the rat ovary. Mol. Endocrinol., 5, 1269-1279.
33. Xie, W.L., Chipman, J.G., Robertson, D.L., Erikson, R.L. & Simmonds, D.L. (1991). Expression of a mitogen-responsive gene encoding prostaglandin synthase is regulated by mRNA splicing. Proc. Natl. Acad. Sci. USA, 88, 2692-2696.
34. Xie, W., Robertson, D.L. & Simmons, D.L. (1992). Mitogen-inducible prostaglandin G/H synthase: A new target for nonsteroidal antiinflammatory drugs. Drug Dev. Res., 25, 249-265.
35. 2 production. Inflamm. Res., 45, 246-253.