Orallo F, Lamela M, Camiña M, Uriarte E, Calleja J M
Departamento de Farmacología, Facultad de Farmacia, Universidad de Santiago de Compostela, Spain.
Planta Med. 1998 Mar;64(2):116-9. doi: 10.1055/s-2006-957386.
In this work, the potential vasorelaxant activity of centaurein and centaureidin, two flavonoids from Centaurea corcubionensis, were studied for the first time in rat aorta. Centaureidin (10 microM-0.1 mM) totally relaxed, in a concentration-dependent manner and with almost equal effectiveness, the contractions induced by NA (IC50 = 16.7 +/- 1.9 microM) or by a high K+ concentration (IC50 = 16.1 +/- 3.1 microM) in intact rat aortic rings. Mechanical removal of endothelium did not significantly modify the vasoralexant effects of this flavone (IC50 = 20.8 +/- 2.4 microM for NA; IC50 = 21 +/- 2.9 microM for K+). On the other hand, centaurein (1 microM-0.1 mM) had no effect on NA- and high K(+)-induced contractions in rubbed and intact rat aortic rings. These results indicate that substitution by glucose in the chemical structure of centaureidin leads to the loss of its vasodilator activity.