Planta Med 1998; 64(7): 588-593
DOI: 10.1055/s-2006-957527
Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Study of Three Sesquiterpene Lactones from Tithonia diversifolia on their Anti-Inflammatory Activity Using the Transcription Factor NF-κB and Enzymes of the Arachidonic Acid Pathway as Targets

Peter Rüngeler1 , 4 , Guido Lyß1 , Victor Castro2 , Gerardo Mora2 , Heike L. Pahl3 , Irmgard Merfort1
  • 1Institut für Pharmazeutische Biologie, Universität Freiburg, Freiburg, Germany
  • 2Universidad de Costa Rica, Escuela de Quimica and CIPRONA, San José, Costa Rica
  • 3Department of Experimental Anaesthesiology, University Hospital, Freiburg, Germany
  • 4Part of the thesis
Further Information

Publication History

1997

1998

Publication Date:
04 January 2007 (online)

Abstract

In Central America leaf extracts from the Asteraceae Tithonia diversifolia are used externally for the treatment of haematomas and wounds. Therefore, the main sesquiterpene lactones (Sls) of this species growing in Costa Rica, diversifolin (1), diversifolin methyl ether (2), and tirotundin (3), were studied for their anti-inflammatory activity. We determined whether these compounds inhibit cyclooxygenase-l, phospholipase A2, or the transcription factor NF-κB. Here we show that these Sls do not influence the enzymes of the arachidonic acid pathway, but inhibit the activation of NF-κB. Thereby, the synthesis of inflammatory mediators such as cytokines and chemokines is reduced. Our results indicate that the inhibitory activity of compounds 1-3 is due to alkylation of cysteine residues, which are probably located in the DNA binding domain of NF-κB. The Sls were also studied for their antibacterial activity, but only Sl 1 was moderatly active against Bacillus subtilis in the agar plate diffusion test.

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