Herencia F, Ferrándiz M L, Ubeda A, Guillén I, Dominguez J N, Charris J E, Lobo G M, Alcaraz M J
Department of Pharmacology, University of Valencia, Burjassot, Spain.
FEBS Lett. 1999 Jun 18;453(1-2):129-34. doi: 10.1016/s0014-5793(99)00707-3.
In a previous work, we tested a series of chalcone derivatives as possible anti-inflammatory compounds. We now investigate the effects of three of those compounds, CHI, CH8 and CH12, on nitric oxide and prostanoid generation in mouse peritoneal macrophages stimulated with lipopolysaccharide and in the mouse air pouch injected with zymosan, where they showed a dose-dependent inhibition with inhibitory concentration 50% values in the microM range. This effect was not the consequence of a direct inhibitory action on enzyme activities. Our results demonstrated that chalcone derivatives inhibited de novo inducible nitric oxide synthase and cyclooxygenase-2 synthesis, being a novel therapeutic approach for inflammatory diseases.
在之前的一项研究中，我们测试了一系列查尔酮衍生物作为潜在的抗炎化合物。我们现在研究其中三种化合物CHI、CH8和CH12，对脂多糖刺激的小鼠腹腔巨噬细胞以及注射酵母聚糖的小鼠气囊肿中一氧化氮和前列腺素生成的影响，结果显示它们具有剂量依赖性抑制作用，半数抑制浓度值在微摩尔范围内。这种作用并非对酶活性的直接抑制作用所致。我们的结果表明，查尔酮衍生物可抑制从头诱导型一氧化氮合酶和环氧化酶-2的合成，这是一种针对炎症性疾病的新型治疗方法。
