Planta Med 2006; 72(8): 754-756
DOI: 10.1055/s-2006-931596
Letter
© Georg Thieme Verlag KG Stuttgart · New York

In Vitro 12(S)-HETE and Leukotriene Metabolism Inhibitory Activity of Sesquiterpenes of Warburgia ugandensis

Abraham Abebe Wube1 , Simon Gibbons2 , Kaleab Asres3 , Bernhard Streit1 , Michael Adams1 , Rudolf Bauer1 , Franz Bucar1
  • 1Institute of Pharmaceutical Sciences, Department of Pharmacognosy, University of Graz, Graz, Austria
  • 2Centre for Pharmacognosy and Phytotherapy, The School of Pharmacy, University of London, London, U.K.
  • 3Department of Pharmacognosy, The School of Pharmacy, Addis Ababa University, Ethiopia
Further Information

Publication History

Received: December 9, 2005

Accepted: February 25, 2006

Publication Date:
29 May 2006 (online)

Abstract

Twelve drimane and coloratane sesquiterpenes, isolated from the stem bark of Ethiopian Warburgia ugandensis, were evaluated for inhibition of 12(S)-HETE using human platelets and of leukotriene B4 formation using activated human neutrophile granulocytes. Among the compounds examined for inhibition of 12-LOX, ugandensidial and muzigadial displayed potent inhibitory activity with IC50 values of 3.3 and 20.2 μM, respectively, in comparison to the positive control baicalein with an IC50 value of 20.0 μM. In the 5-LOX assay muzigadial and ugandensidial also exhibited a dose dependent and potent inhibitory effect on LTB4 biosynthesis with an IC50 value of 10.2 and 12.7 μM, respectively, compared to the well known 5-LOX inhibitor zileuton with an IC50 value of 10.4 μM. In contrast, none of the other sesquiterpenoids showed significant inhibition of either 12(S)-HETE or LTB4 metabolism.

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Ao. Univ.-Prof. Dr. Franz Bucar

Institute for Pharmaceutical Sciences

Department of Pharmacognosy

University of Graz

A-8010 Graz

Austria

Phone: +43-316-380-5531

Fax: +43-316-380-9860

Email: franz. bucar@uni-graz.at