Anti-inflammatory activity of 5-O-demethylnobiletin, a polymethoxyflavone isolated from Sideritis tragoriganum

Esperanza Bas, M. Carmen Recio, Rosa M. Giner, Salvador Máñez, Miguel Cerdá-Nicolás, José Luis Ríos

Research output: Contribution to journalArticle

23 Scopus citations

Abstract

We have studied the effect of 5-O-demethylnobiletin (1) on both the inflammation of mouse ears induced by repeated application of 12-O-tetradecanoylphorbol 13-acetate (TPA) and the acute mouse paw oedemas induced by carrageenan and phospholipase A2 (PLA2), and determined its activity on 5-lipoxygenase (5-LOX) and elastase release/activity. Compound 1 reduced the oedema formation, cell infiltration, and tissue damage in the inflammation induced by TPA in mouse ears, along with the acute oedema induced by carrageenan in mouse paws and the acute PLA2-induced oedema in mouse paws. The flavone inhibited leukotriene B4 formation in rat neutrophils and elastase release in human neutrophils, but did not reduce the expression of cyclooxygenase-2 (COX-2) in murine RAW 264.7 macrophages. These experimental results suggest that 1 may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.

Original languageEnglish (US)
Pages (from-to)136-142
Number of pages7
JournalPlanta Medica
Volume72
Issue number2
DOIs
StatePublished - Feb 1 2006
Externally publishedYes

Keywords

  • 5-O-Demethylnobiletin
  • 5-lipoxygenase
  • Anti-inflammatory activity
  • Lamiaceae
  • Sideritis tragoriganum

ASJC Scopus subject areas

  • Analytical Chemistry
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine
  • Organic Chemistry

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