Modulation of inflammatory responses by diterpene acids from Helianthus annuus L

Fractionation of a petroleum ether extract of Helianthus annuus L. led to the isolation of three diterpene acids: grandiflorolic, kaurenoic and trachylobanoic acids. These compounds were studied for potential anti-inflammatory activity on the generation of inflammatory mediators in lipopolysaccharid...

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Bibliographic Details
Published in:Biochemical and biophysical research communications 2008-05, Vol.369 (2), p.761-766
Main Authors: Díaz-Viciedo, Rodrigo, Hortelano, Sonsoles, Girón, Natalia, Massó, Jose M., Rodriguez, Benjamín, Villar, Angel, de las Heras, Beatriz
Format: Article
Language:English
Subjects:
Animals
Anti-inflammatory activity
Anti-Inflammatory Agents - administration & dosage
Cell Line
Cyclooxygenase-2
Cytokines - immunology
Diterpene acids
Diterpenes - administration & dosage
Dose-Response Relationship, Radiation
Helianthus
Helianthus - metabolism
Helianthus annuus
Helianthus annuus L
Immunologic Factors - immunology
Macrophages
Macrophages - drug effects
Macrophages - immunology
Mice
Nitric oxide
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Summary:Fractionation of a petroleum ether extract of Helianthus annuus L. led to the isolation of three diterpene acids: grandiflorolic, kaurenoic and trachylobanoic acids. These compounds were studied for potential anti-inflammatory activity on the generation of inflammatory mediators in lipopolysaccharide (LPS)-activated RAW 264.7 macrophages. At non-toxic concentrations, these compounds reduced, in a concentration-dependent manner nitric oxide (NO), prostaglandin E 2 (PGE 2) and tumor necrosis factor (TNF-α) production, as well as expression of inducible nitric oxide synthase (NOS-2) and cyclooxygenase-2 (COX-2). All diterpenoids displayed significant in vivo anti-inflammatory activity and suppressed the 12- O-tetradecanoylphorbol-13-acetate (TPA)-mouse ear edema. In addition, inhibition of myeloperoxidase (MPO) activity, an index of cellular infiltration, was observed. In summary, our results suggest that the inhibition of the expression of NOS-2, COX-2 and the release of inflammatory cytokines, is responsible for the anti-inflammatory effects of the diterpenoids isolated from H. annuus L. which likely contributes to the pharmacological action of sunflower.
ISSN:0006-291X
1090-2104
DOI:10.1016/j.bbrc.2008.02.104