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Research ArticleArticle

Differential Contribution of R and SIsomers in Ketoprofen Anti-inflammatory Activity: Role of Cytokine Modulation

Pietro Ghezzi, Gabriella Melillo, Cristina Meazza, Silvano Sacco, Luigi Pellegrini, Cinzia Asti, Stefano Porzio, Antonello Marullo, Vilma Sabbatini, Gianfranco Caselli and Riccardo Bertini
Journal of Pharmacology and Experimental Therapeutics December 1998, 287 (3) 969-974;
Pietro Ghezzi
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Gabriella Melillo
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Cristina Meazza
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Silvano Sacco
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Luigi Pellegrini
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Cinzia Asti
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Stefano Porzio
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Antonello Marullo
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Vilma Sabbatini
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Gianfranco Caselli
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Riccardo Bertini
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Abstract

Among nonsteroidal anti-inflammatory drugs (NSAIDs), 2-arylpropionic acids exist as a racemic mixture of its enantiomeric forms, withS-enantiomers primarily responsible for inhibition of prostaglandin synthesis and of inflammatory events. The aim of this study was to compare the anti-inflammatory effects of R- andS-ketoprofen in vitro and in vivo.S-Ketoprofen efficiently inhibited carrageenan-induced edema formation, but it could also amplify the LPS-induced production of the inflammatory cytokines tumor necrosis factor (TNF) and interleukin-1 (IL-1), in close correlation with its ability to inhibit prostaglandin synthesis. Because these inflammatory cytokines are among the factors involved in carrageenan-induced inflammation and also are possibly involved in gastric damage, enhanced cytokine production could partially mask the analgesic effect of S-ketoprofen, and it can be associated with the clinical evidence of its gastric toxicity. On the other hand, R-ketoprofen contributes to the overall activity of the racemate, by playing the main role in ketoprofen-induced analgesia. Unlike the S-isomer,R-ketoprofen did not induce a significant increase of cytokine production even at cyclooxygenase-blocking concentrations. It is concluded that the R-isomer directly contributes to the anti-inflammatory effects of ketoprofen, being more analgesic, and because it does not amplify inflammatory cytokine production.

Footnotes

  • Send reprint requests to: Dr. Riccardo Bertini, DompéS.p.A., via Campo di Pile, 67100 L’Aquila, Italy.

  • ↵1 This work was partially supported by the contract “Programma Nazionale di Ricerca e Formazione sui Farmaci (seconda fase), Tema 4,” granted by the Italian Ministry of University and Scientific and Technological Research.

  • Abbreviations:
    NSAID
    nonsteroidal anti-inflammatory drug
    PGE2
    prostaglandin E2
    LPS
    bacterial endotoxin
    TNF
    tumor necrosis factor
    IL
    interleukin
    • Received December 9, 1997.
    • Accepted July 6, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics
Vol. 287, Issue 3
1 Dec 1998
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Research ArticleArticle

Differential Contribution of R and SIsomers in Ketoprofen Anti-inflammatory Activity: Role of Cytokine Modulation

Pietro Ghezzi, Gabriella Melillo, Cristina Meazza, Silvano Sacco, Luigi Pellegrini, Cinzia Asti, Stefano Porzio, Antonello Marullo, Vilma Sabbatini, Gianfranco Caselli and Riccardo Bertini
Journal of Pharmacology and Experimental Therapeutics December 1, 1998, 287 (3) 969-974;

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Research ArticleArticle

Differential Contribution of R and SIsomers in Ketoprofen Anti-inflammatory Activity: Role of Cytokine Modulation

Pietro Ghezzi, Gabriella Melillo, Cristina Meazza, Silvano Sacco, Luigi Pellegrini, Cinzia Asti, Stefano Porzio, Antonello Marullo, Vilma Sabbatini, Gianfranco Caselli and Riccardo Bertini
Journal of Pharmacology and Experimental Therapeutics December 1, 1998, 287 (3) 969-974;
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