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