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Inflammation Research

, Volume 52, Issue 6, pp 246–257 | Cite as

1-(2,3,4-trimethoxyphenyl)-3-(3-(2-chloroquinolinyl))-2-propen-1-one, a chalcone derivative with analgesic, anti-inflammatory and immunomodulatory properties

  • E. J. De León
  • M. J. Alcaraz
  • J. N. Dominguez
  • J. Charris
  • M. C. Terencio
Regular paper

Abstract:

Objetive and Design: The synthetic chalcone derivative 1-(2,3,4-trimethoxyphenyl)-3-(3-(2-chloroquinolinyl))-2-propen-1-one (TQ) was evaluated for its immunomodulatory and anti-inflammatory efficacy in vitro and in vivo. Material and Subjets: Human neutrophils and lymphocytes from healthy volunteers and RAW 264.7 murine macrophages. Swiss mice and Lewis rats were randomly divided into groups of six animals. Treatment: TQ was orally administered in all in vivo assays (10–30 mg/kg). Methods: Elastase, superoxide and LTB4 release were assayed in human neutrophils, NO/PGE2 production and NF-κB activation in RAW 264.7, and 3H thymidine incorporation in human lymphocytes. Zymosan-stimulated air pouches, DNFB-DTH, PBQ-induced writhings and formalin-induced pain were assayed in mice. Adjuvant-induced arthritis was tested in rats. Dunnett's t-test was employed for statistical analysis. Results: Human T-cell proliferation, neutrophil functions and NO/PGE2 production in murine macrophages were inhibited by TQ (IC50 in the μM range), which showed anti-inflammatory, immunomodulatory and analgesic effects. Conclusions: Our findings indicate the potential interest of TQ in the modulation of some immune and inflammatory responses probably by NF-κB inhibition.

Key words:Chalcone – Leukocyte – Arthritis – Air pouch – Analgesia. 

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Copyright information

© Birkhäuser Verlag, 2003

Authors and Affiliations

  • E. J. De León
    • 1
  • M. J. Alcaraz
    • 1
  • J. N. Dominguez
    • 2
  • J. Charris
    • 2
  • M. C. Terencio
    • 1
  1. 1.Department of Pharmacology, University of Valencia, Faculty of Pharmacy, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain, Fax: ++34 96 3544 292, e-mail: Carmen.Terencio@uv.es ES
  2. 2.Laboratory of Organic Synthesis, Faculty of Pharmacy, Central University of Venezuela, Caracas 1051, Venezuela VE

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