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Effect of Dehydroleucodine on Intestinal Transit: Structural Basis of the Interaction With the α(2)-adrenergic Receptor

Effect of Dehydroleucodine on Intestinal Transit: Structural Basis of the Interaction With the α(2)-adrenergic Receptor

Graciela Haydée Wendel, Alejandra Olivia María, Carlos Fernando Aguilar, Lilian Eugenia Pelzer

Eur Biophys J. 2011 Aug;40(8):981-6.

PMID: 21671152

Abstract:

The activity of dehydroleucodine, a sesquiterpene lactone obtained from Artemisia douglasiana, was studied in mice small intestinal transit. Its mechanism was evaluated in the presence of several adrenergic and cholinergic antagonist drugs and one opioid antagonist. Docking of dehydroleucodine into the homology model of the α2-adrenergic receptor allowed us to analyze the structural basis of their interactions. The experiments showed that dehydroleucodine delayed intestinal transit. The docking of dehydroleucodine showed a unique binding site, equivalent to the binding site of carozolol in the β-adrenergic receptor. The results suggested that dehydroleucodine produced an inhibitory effect on intestinal transit. Its action could be mediated, at least in part, through the α2-adrenergic receptor.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP36150079	Dehydroleucodine		36150-07-9	Price

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