In vitro 12(S)-HETE and leukotriene metabolism inhibitory activity of sesquiterpenes of Warburgia ugandensis

Abraham Wube; Simon Gibbons; Kaleab Asres; Bernhard Streit; Michael Adams; Rudolf Bauer; Franz Bucar

doi:10.1055/s-2006-931596

In vitro 12(S)-HETE and leukotriene metabolism inhibitory activity of sesquiterpenes of Warburgia ugandensis

Abraham Wube, Simon Gibbons, Kaleab Asres, Bernhard Streit, Michael Adams, Rudolf Bauer, Franz Bucar

Research output: Contribution to journal › Article › peer-review

9 Citations (Scopus)

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.

Original language	English
Pages (from-to)	754-756
Number of pages	3
Journal	Planta Medica
Volume	72
Issue number	08
DOIs	https://doi.org/10.1055/s-2006-931596
Publication status	Published - 1 May 2006

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@article{6bc1654d0b0847a486b92cc82cecbe01,

title = "In vitro 12(S)-HETE and leukotriene metabolism inhibitory activity of sesquiterpenes of Warburgia ugandensis",

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.",

author = "Abraham Wube and Simon Gibbons and Kaleab Asres and Bernhard Streit and Michael Adams and Rudolf Bauer and Franz Bucar",

year = "2006",

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doi = "10.1055/s-2006-931596",

language = "English",

volume = "72",

pages = "754--756",

journal = "Planta Medica",

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TY - JOUR

T1 - In vitro 12(S)-HETE and leukotriene metabolism inhibitory activity of sesquiterpenes of Warburgia ugandensis

AU - Wube, Abraham

AU - Gibbons, Simon

AU - Asres, Kaleab

AU - Streit, Bernhard

AU - Adams, Michael

AU - Bauer, Rudolf

AU - Bucar, Franz

PY - 2006/5/1

Y1 - 2006/5/1

N2 - 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.

AB - 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.

U2 - 10.1055/s-2006-931596

DO - 10.1055/s-2006-931596

M3 - Article

VL - 72

SP - 754

EP - 756

JO - Planta Medica

JF - Planta Medica

SN - 0032-0943

IS - 08

ER -