title: 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.
abstract: 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.
authors: Department of Chemistry, National Cheng Kung University, Tainan, Taiwan, ROC.
authors: M Vijaya Bhaskar
authors: MV
authors: Reddy
authors: Tsong-Long
authors: TL
authors: Hwang
authors: Yann-Lii
authors: YL
authors: Leu
authors: Wen-Fei
authors: WF
authors: Chiou
authors: Tian-Shung
authors: TS
authors: Wu
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology*; D006571:Heterocyclic Compounds; D006801:Humans; D008262:Macrophage Activation; D008264:Macrophages / Q000378:metabolism*; D051379:Mice; D009504:Neutrophils / Q000378:metabolism*; D009569:Nitric Oxide / Q000096:biosynthesis*; D010196:Pancreatic Elastase / Q000378:metabolism*; D013329:Structure-Activity Relationship; D013481:Superoxides / Q000378:metabolism*
chemical_list: D000893:Anti-Inflammatory Agents; D047188:Chalcones; D006571:Heterocyclic Compounds; D013481:Superoxides; D009569:Nitric Oxide; D010196:Pancreatic Elastase