Vasorelaxant Effect of and Its Active Ingredients on an Isolated Coronary Artery.

Cardiovascular diseases are a major cause of death in developed countries. The regulation of vascular tone is a major approach to prevent and ameliorate vascular diseases. As part of our ongoing screening for cardioprotective natural compounds, we investigated the vasorelaxant effect of rhizomes from (L.) Mansf. [ (Roxb.) Schltr.] used as a spice and herbal medicine in Asian countries. The methanol extract of rhizomes (BRE) exhibited significant vasorelaxation effects ex vivo at EC values of 13.4 ± 6.1 μg/mL and 40.9 ± 7.9 μg/mL, respectively, with and without endothelium in the porcine coronary artery ring. The intrinsic mechanism was evaluated by treating with specific inhibitors or activators that typically affect vascular reactivity. The results suggested that BRE induced relaxation in the coronary artery rings via an endothelium-dependent pathway involving NO-cGMP, and also via an endothelium-independent pathway involving the blockade of Ca channels. Vasorelaxant principles in BRE were identified by subsequent chromatographic methods, which revealed that flavonoids regulate vasorelaxant activity in BRE. One of the flavonoids was a Diels-Alder type adduct, 4-hydroxypanduratin A, which showed the most potent vasorelaxant effect on porcine coronary artery with an EC of 17.8 ± 2.5 μM. Our results suggest that rhizomes of might be of interest as herbal medicine against cardiovascular diseases.