Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC.
Bioorg Med Chem. 2011 Apr 15;19(8):2751-6. doi: 10.1016/j.bmc.2011.02.038. Epub 2011 Mar 8.
Some chalcones exert potent anti-inflammatory activities. Mannich bases of heterocyclic chalcones inhibited nitric oxide (NO) production in lipopolysaccharide and interferon-γ stimulated RAW 264.7 macrophages. Also Formyl-Met-Leu-Phe and cytochalasin B induced superoxide anion generation (O2·-) and elastase release in human neutrophils. Mannich bases of heterocyclic chalcone analogs exhibited potent inhibitory effects on NO production with IC(50) values ranges between 10.5 and 0.018 μM, O2·- generation (IC(50) 39.87-0.68 μM) and elastase release (IC(50) 39.74-0.95 μM). Compound 29 (IC(50) 0.055 μM) and 34 (IC(50) 0.018 μM) were showed excellent inhibition on NO production. On the other hand, compounds 2 and 8 showed potent inhibition on O2·- generation and elastase release. Therefore, these four compounds may be new leads for development of anti-inflammatory activities. The structure-activity relationships are also discussed.
一些查耳酮具有很强的抗炎活性。杂环查耳酮的曼尼希碱抑制脂多糖和干扰素-γ刺激的 RAW 264.7 巨噬细胞中一氧化氮（NO）的产生。同时，甲酰-Met-Leu-Phe 和细胞松弛素 B 诱导人嗜中性粒细胞中超氧阴离子（O2·-）的产生和弹性蛋白酶的释放。杂环查尔酮类似物的曼尼希碱对 NO 产生具有很强的抑制作用，IC（50）值在 10.5 和 0.018 μM 之间，O2·-生成（IC（50）39.87-0.68 μM）和弹性蛋白酶释放（IC（50）39.74-0.95 μM）。化合物 29（IC（50）0.055 μM）和 34（IC（50）0.018 μM）对 NO 产生具有极好的抑制作用。另一方面，化合物 2 和 8 对 O2·-生成和弹性蛋白酶释放具有很强的抑制作用。因此，这四种化合物可能是开发抗炎活性的新先导化合物。还讨论了构效关系。
