Inhibition of NF-κB activation and expression of inflammatory mediators by polyacetylene spiroketals from Plagius flosculosus

Marco A. Calzado, Katharina Schmid Lüdi, Bernd Fiebich, Yinon Ben-Neriah, Susanne Bacher, Eduardo Munoz, Mauro Ballero, Simona Prosperini, Giovanni Appendino, M. Lienhard Schmitz*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

18 Scopus citations

Abstract

Transcription factor NF-κB plays a key role for the inducible expression of genes mediating proinflammatory effects and is thus an important target for the development of antiinflammatory drugs. Here, we show that extracts from the plant Plagius flosculosus (L.) Alavi and Heyw. can inhibit the induction of NF-κB activity, and we describe the identification of three spiroketal compounds. Of those, only compound 1 could inhibit the phosphorylation and proteasomal degradation of IκB, thus preventing the nuclear import and DNA binding of NF-κB. Accordingly, compound 1, which is also found in the widely used medicinal herb chamomile, interfered with the LPS-induced production of IL-1, IL-6, TNF, and PGE2 in primary human monocytes.

Original languageEnglish
Pages (from-to)88-93
Number of pages6
JournalBiochimica et Biophysica Acta - Gene Structure and Expression
Volume1729
Issue number2
DOIs
StatePublished - 30 Jun 2005

Bibliographical note

Funding Information:
This work was supported by a EU grant (AINP, contract QLK3-CT-2000-00463).

Keywords

  • Cytokine
  • Inducible transcription
  • Inflammation
  • NF-κB

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