Synthesis of biflavones having a 6-O-7'' linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase

Haiyan Che, Byung Kyu Park, Hyun Lim, Hyun Pyo Kim, Hyeun Wook Chang, Jin Hyun Jeong, Haeil Park

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

In order to establish anti-inflammatory potential of biflavonoids, 17 biflavone derivatives having a 6-O-7″ linkage were synthesized and their effects on cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) were evaluated. The basic molecule (6-O-7″ biflavone) potently inhibited COX-2-mediated PGE2 production (IC50: < 2 μM), being less active on iNOS-mediated NO production (IC50: > 50 μM) from lipopolysaccharide-treated RAW 264.7 cells, a mouse macrophage cell line. Generally, the hydroxyl/methoxyl substitution(s) on the basic biflavone (6-O-7″) reduced the inhibitory activity of PGE2 production, while the effects on NO production were varied. It is suggested that the basic biflavone (6-O-7″) may have a potential for new anti-inflammatory agent.

Original languageEnglish
Pages (from-to)74-76
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number1
DOIs
Publication statusPublished - 2009 Jan 1

All Science Journal Classification (ASJC) codes

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

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