De León E J, Alcaraz M J, Dominguez J N, Charris J, Terencio M C
Department of Pharmacology, University of Valencia, Faculty of Pharmacy, Av Vicent Andrés Estellés s/n, 46100 Burjassot, Valencia, Spain.
Inflamm Res. 2003 Jun;52(6):246-57. doi: 10.1007/s00011-003-1164-x.
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.
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.
TQ was orally administered in all in vivo assays (10-30 mg/kg).
Elastase, superoxide and LTB(4) release were assayed in human neutrophils, NO/PGE(2) production and NF-kappaB activation in RAW 264.7, and (3)H 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.
Human T-cell proliferation, neutrophil functions and NO/PGE(2) production in murine macrophages were inhibited by TQ (IC(50) in the microM range), which showed anti-inflammatory, immunomodulatory and analgesic effects.
Our findings indicate the potential interest of TQ in the modulation of some immune and inflammatory responses probably by NF-kappaB inhibition.
评估合成查尔酮衍生物1-(2,3,4-三甲氧基苯基)-3-(3-(2-氯喹啉基))-2-丙烯-1-酮（TQ）在体外和体内的免疫调节及抗炎功效。
来自健康志愿者的人中性粒细胞和淋巴细胞以及RAW 264.7小鼠巨噬细胞。瑞士小鼠和Lewis大鼠被随机分成每组六只动物的组。
在所有体内试验中口服给予TQ（10 - 30毫克/千克）。
检测人中性粒细胞中的弹性蛋白酶、超氧化物和白三烯B4释放，RAW 264.7中的一氧化氮/前列腺素E2生成和核因子κB激活，以及人淋巴细胞中的3H胸苷掺入。检测小鼠中酵母聚糖刺激的气囊、二硝基氟苯诱导的迟发型超敏反应、苯醌诱导的扭体反应和福尔马林诱导的疼痛。在大鼠中测试佐剂诱导的关节炎。采用Dunnett t检验进行统计分析。
TQ抑制人T细胞增殖、中性粒细胞功能以及小鼠巨噬细胞中的一氧化氮/前列腺素E2生成（IC50在微摩尔范围内），显示出抗炎、免疫调节和镇痛作用。
我们的研究结果表明TQ可能通过抑制核因子κB对调节某些免疫和炎症反应具有潜在意义。
