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

M. Vijaya Bhaskar Reddy, Tsong Long Hwang, Yann Lii Leu, Wen Fei Chiou, Tian Shung Wu

Research output: Contribution to journalArticle

19 Citations (Scopus)

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 IC50 values ranges between 10.5 and 0.018 μM, O2·- generation (IC50 39.87-0.68 μM) and elastase release (IC50 39.74-0.95 μM). Compound 29 (IC50 0.055 μM) and 34 (IC50 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.

Original languageEnglish
Pages (from-to)2751-2756
Number of pages6
JournalBioorganic and Medicinal Chemistry
Volume19
Issue number8
DOIs
Publication statusPublished - 2011 Apr 15

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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