Inhibitory effects of Mannich bases of heterocyclic chalcones on NO production by activated RAW 264.7 macrophages and superoxide anion generation and elastase release by activated human neutrophils
- Bioorg Med Chem. 2011 Apr 15;19(8):2751-6. doi: 10.1016/j.bmc.2011.02.038.
- 1. Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC.
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.