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

Wube, Abraham, Gibbons, Simon, Asres, Kaleab, Streit, Bernhard, Adams, Michael, Bauer, Rudolf and Bucar, Franz (2006) In Vitro 12(S)-HETE and Leukotriene Metabolism Inhibitory Activity of Sesquiterpenes of Warburgia ugandensis. Planta Medica, 72 (08). pp. 754-756. ISSN 0032-0943

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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.

Item Type: Article
Faculty \ School: Faculty of Science > School of Pharmacy
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Depositing User: LivePure Connector
Date Deposited: 27 Jun 2020 00:02
Last Modified: 27 Jun 2020 00:02
URI: https://ueaeprints.uea.ac.uk/id/eprint/75799
DOI: 10.1055/s-2006-931596

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