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

Fingerprint

Nitric Oxide Synthase Type II
Cyclooxygenase 2
Dinoprostone
Biflavonoids
Anti-Inflammatory Agents
Hydroxyl Radical
Inhibitory Concentration 50
Lipopolysaccharides
Macrophages
Cell Line
Substitution reactions
Cells
Derivatives
Molecules
RAW 264.7 Cells

All Science Journal Classification (ASJC) codes

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

Cite this

Che, Haiyan ; Park, Byung Kyu ; Lim, Hyun ; Kim, Hyun Pyo ; Chang, Hyeun Wook ; Jeong, Jin Hyun ; Park, Haeil. / Synthesis of biflavones having a 6-O-7'' linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase. In: Bioorganic and Medicinal Chemistry Letters. 2009 ; Vol. 19, No. 1. pp. 74-76.
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Synthesis of biflavones having a 6-O-7'' linkage and effects on cyclooxygenase-2 and inducible nitric oxide synthase. / Che, Haiyan; Park, Byung Kyu; Lim, Hyun; Kim, Hyun Pyo; Chang, Hyeun Wook; Jeong, Jin Hyun; Park, Haeil.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 19, No. 1, 01.01.2009, p. 74-76.

Research output: Contribution to journalArticle

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