Article

Anti-inflammatory profile of dehydrocostic acid, a novel sesquiterpene acid with a pharmacophoric conjugated diene.

Departament de Farmacologia, Facultat de Farmàcia, Universitat de València, Av. Vicent Andrés Estellés s/n, 46100 Burjassot, Spain.
European Journal of Pharmaceutical Sciences (impact factor: 3.21). 11/2005; 26(2):162-9. DOI:10.1016/j.ejps.2005.05.007 pp.162-9
Source: PubMed

ABSTRACT Sesquiterpene acids are natural products that, in contrast with the thoroughly studied sesquiterpene lactones, have received little pharmacological attention. A good source of this class of compounds is Inula viscosa (Asteraceae), a plant with documented anti-inflammatory effects. The present paper gives the results of our investigations on the biochemical mechanisms involved in the anti-inflammatory activity of one such compound, dehydrocostic acid. The most salient findings were that in vitro dehydrocostic acid inhibits leukotriene B(4) production (IC(50)=22 microM), elastase activity (IC(50)=43 microM) and bee venom phospholipase A(2) activity (IC(50)=17 microM). Furthermore, this sesquiterpenoid was effective on some models of acute edema induced by PLA(2) and 12-O-tetradecanoylphorbol 13-acetate (TPA) Comparison of these data with that known for ilicic acid firmly suggests that the presence of a semiplanar ring A is essential for an improved inhibitory activity on inflammatory mediators.

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Keywords

12-O-tetradecanoylphorbol 13-acetate
 
acute edema induced
 
anti-inflammatory activity
 
bee venom phospholipase A(2)
 
biochemical mechanisms
 
dehydrocostic acid
 
documented anti-inflammatory effects
 
elastase activity
 
improved inhibitory activity
 
inflammatory mediators
 
pharmacological attention
 
salient findings
 
Sesquiterpene acids
 
sesquiterpenoid
 
studied sesquiterpene lactones
 
vitro dehydrocostic acid inhibits leukotriene B(4)
 

V Hernández