A review of mechanism of action of steroid and non-steroid anti-inflammatory drugs

  • S. Tsurufuji
  • K. Sugio
  • H. Sato
  • K. Ohuchi
Part of the Inflammation: Mechanisms and Treatment book series (FTIN, volume 4)


The present article will review our work on the anti-exudative action of steroidal and non-steroidal anti-inflammatory drugs. In the light of present knowledge, both steroidal and non-steroidal anti-inflammatory drugs appear to inhibit production of pro-inflammatory prostaglandins (PGs) in a variety of biological systems involving cultured cells and isolated tissues maintained under appropriate incubation conditions1–6. Glucocorticoids appear to inhibit PG production or its release from the cells by suppression of the action of phospholipase A2 or by some unknown mechanisms7–9. Non-steroidal antiinflammatory drugs such as indomethacin block cyclo-oxygenase10,11. However, it remains to be established whether decrease in the production or release of prostaglandins takes place at the inflammatory locus in parallel with the inhibition of the vascular permeability response.


Human Serum Albumin Vascular Permeability Chemical Mediator Arachidonic Acid Release Prostaglandin Biosynthesis 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Vane, J. R. (1971). Inhibition of prostaglandin synthesis as a mechanism of action for aspirin-like drugs. Nature (London), New Biol. 231, 232Google Scholar
  2. 2.
    Flower, R., Gryglewski, R., Herbaczynska-Cedro, K. et al. (1972). Effects of anti-inflammatory drugs on prostaglandin biosynthesis. Nature (London), New Biol., 238, 104Google Scholar
  3. 3.
    Kantrowtiz, F., Robinson, D. R., McGaire, M. B. et al. (1975). Cortiscosteroids inhibit prostaglandin production by rheumatoid synovia. Nature (London), 258, 737CrossRefGoogle Scholar
  4. 4.
    Gryglewski, R. J., Panczenko, B., Korbut, R. et al. (1975). Corticosteroids inhibit prostaglandin release from perfused mesenteric blood vessels of rabbit and from perfused lungs of sensitized guinea pig. Prostaglandins, 10, 343PubMedGoogle Scholar
  5. 5.
    Tam, S., Hong, S. C. and Levine, L. (1977). Relationships, among the steroids, of antiinflammatory properties and inhibition of prostaglandin production and arachidonic acid release by transformed mouse fibroblasts. J. Pharmacol. Exp. Ther. 203, 162PubMedGoogle Scholar
  6. 6.
    Floman, Y. and Zor, U. (1976). Mechanism of steroid action in inflammation: inhibition of prostaglandin synthesis and release. Prostaglandins, 12, 403PubMedCrossRefGoogle Scholar
  7. 7.
    Hong, S. L. and Levine, L. (1976). Inhibition of arachidonic acid release from cells as the biochemical action of anti-inflammatory corticosteroids. Proc. Natl. Acad. Sci. (USA), 73, 1730CrossRefGoogle Scholar
  8. 8.
    Blackwell, G.J., Flower, R. J., Nijkamp, F.P. et al. (1978). Phospholipase A2 activity of guinea-pig isolated perfused lungs: stimulation, and inhibition by anti-inflammatory steroids. Br. J. Pharmacol., 62, 79PubMedGoogle Scholar
  9. 9.
    Chang, J., Lewis, G. P. and Piper, P. J. (1977). Inhibition by glucocorticoids of prostaglandin release from adipose tissue in vitro. Br. J. Pharmacol., 59, 425PubMedGoogle Scholar
  10. 10.
    Yamamoto, S., Ogino, N., Ohki, S. et al. (1977). Enzymological studies on prostaglandin biosynthesis. In Karashe, N. and Fried, J. (eds.) Biochemical Aspects of Prostaglandins and Thromboxanes, pp. 1–13. (New York: Academic Press)Google Scholar
  11. 11.
    Hamberg, M. and Samuelsson, B. (1974). Prostaglandin endoperoxides. Novel transformations of arachidonic acid in human platelets. Proc. Natl. Acad. Sci. (USA), 71, 3400CrossRefGoogle Scholar
  12. 12.
    Fukuhara, M. and Tsurufuji, S. (1969). The effect of locally injected anti-inflammatory drugs on the carrageenin granuloma in rats. Biochem. Pharmacol., 18, 475PubMedCrossRefGoogle Scholar
  13. 13.
    Tsurufuji, S., Sugio, K. and Endo, Y. (1977). Inhibition of vascular permeability by cyclo-heximide in granulomatous inflammation. Biochem. Pharmacol., 26, 1131PubMedCrossRefGoogle Scholar
  14. 14.
    Chang, W.C., Murota, S. and Tsurufuji, S. (1975). Contents of Prostaglandin E in the exudate of rat carrageenin granuloma. Japan. J. Pharmacol., 25, 219CrossRefGoogle Scholar
  15. 15.
    Ohuchi, K., Sato, H. and Tsurufuji, S. (1976). The content of prostaglandin E and prostaglandin F2alpha in the exudate of carrageenin granuloma of rats. Biochim. Biophys. Acta, 424, 439PubMedGoogle Scholar
  16. 16.
    Wiseman, E. H. (1974). Drug kinetic studies with nonsteroidal antiinflammatory agents in animals and man. In Scherrer R. A. and Whitehouse, M. W. (eds.) Antiinflammatory Agents, Chemistry and Pharmacology, pp. 235–243. (New York: Academic Press)Google Scholar
  17. 17.
    Majno, G., Shea, S. M. and Leventhal, M. (1969). Endothelial contraction induced by histamine-type mediators: an electron microscopic study. J. Cell. Biol., 42, 647PubMedCrossRefGoogle Scholar
  18. 18.
    Baxter, J. D. and Forsham, P. H. (1972). Tissue effects of glucocorticoids. Am. J. Med., 53, 573PubMedCrossRefGoogle Scholar
  19. 19.
    Chan, L. and O’Malley, B. W. (1976). Mechanism of action of the sex steroid hormones. N. Engl. J. Med., 294, 1322, 1372, 1430PubMedCrossRefGoogle Scholar
  20. 20.
    Baxter, J. D. and Funder, J. W. (1979). Hormone receptors. N. Engl. J. Med., 301, 1149PubMedCrossRefGoogle Scholar
  21. 21.
    Leung, K. and Munck, A. (1975). Peripheral actions of glucocorticoids. Ann. Rev. Physiol., 37, 245CrossRefGoogle Scholar
  22. 22.
    Danon, A. and Assouline, G. (1978). Inhibition of prostaglandin biosynthesis by corticosteroids requires RNA and protein synthesis. Nature (London), 273, 552CrossRefGoogle Scholar
  23. 23.
    Flower, R. J. and Blackwell, G. J. (1979). Anti-inflammatory steroids induce biosynthesis of a phospholipase A2 inhibitor which prevents prostaglandin generation. Nature (London), 278, 456CrossRefGoogle Scholar
  24. 24.
    DiRosa, M. and Persico, P. (1979). Mechanism of inhibition of prostaglandin biosynthesis by hydrocortisone in rat leucocytes. Br. J. Pharmacol., 66, 161Google Scholar
  25. 25.
    Daum, A. and Römer, D. (1970). Die Wirkung von Antiphlogistica auf die durch Bradykinin induzierte Permeabilitätserhöhung in der Ratten haut und an der Rattenpfote. Nauyn-Schmiedebergs Arch. Pharmakol., 266, 313CrossRefGoogle Scholar
  26. 26.
    Ikeda, K., Tanaka, K. and Katori, M. (1975). Potentiation of bradykinin-induced vascular permeability increase by prostaglandin E2 and arachidonic acid in rabbit skin. Prostaglandins, 10, 747PubMedGoogle Scholar
  27. 27.
    Williams, T.J. and Peck, M.J. (1977). Role of prostaglandin-mediated vasodilation in inflammation. Nature (London).270, 530CrossRefGoogle Scholar
  28. 28.
    Williams, T. J. (1979). Prostaglandin E2, prostaglandin I2 and the vascular changes of inflammation. Br. J. Pharmacol., 65, 517PubMedGoogle Scholar
  29. 29.
    Samuels, H. H. and Tomkins, G. M. (1970). Relation of steroid structure to enzyme induction in hepatoma tissue culture cells. J. Mol. Biol., 52, 57PubMedCrossRefGoogle Scholar
  30. 30.
    Rousseau, G. G., Baxter, J. D. and Tomkins, G. M. (1972). Glucocorticoid receptors: relations between steroid binding and biological effects. J. Mol. Biol., 67, 99PubMedCrossRefGoogle Scholar
  31. 31.
    Tsurufuji, S., Sugio, K. and Takemasa, F. (1979). The role of glucocorticoid receptor and gene expression in the anti-inflammatory action of dexamethasone. Nature (London), 280, 408CrossRefGoogle Scholar
  32. 32.
    Tsurufuji, S., Sugio, K., Takamasa, F. and Yoshizawa, S. (1980). J. Pharmacol. Exp. Ther. (In press)Google Scholar
  33. 33.
    Tsurufuji, S. and Kazuo, S. (1978). Molecular mechanisms in the manifestation of antiinflammatory activity of glucocorticoids. Eur. J. Rheumatol. Inflammation., 1, 226Google Scholar

Copyright information

© MTP Press Limited 1980

Authors and Affiliations

  • S. Tsurufuji
    • 1
  • K. Sugio
    • 1
  • H. Sato
    • 1
  • K. Ohuchi
    • 1
  1. 1.Japan

Personalised recommendations