Methanolic extract and two purified compounds (brazilin and hematoxylin) fr
om Caesalpinia sappan were examined for their relaxant effects in isolated
rat thoracic aorta. The methanolic extract significantly and dose-dependent
ly relaxed the alpha (1)-receptor agonist phenylephrine-precontracted aorti
c rings, without affecting passive tension of these vessels. Removal of the
vascular endothelium, inhibition of nitric oxide (NO) synthase with 0.1 mM
N-omega-nitro-L-arginine and of cGMP biosynthesis with 10 muM methylene bl
ue abolished the vasorelaxant effects of the herbal extract at doses up to
30 mug/ml. Similar vasorelaxant effects were observed with brazilin and hem
atoxylin. Therefore, these results suggest that brazilin and hematoxylin ma
y be responsible for the vascular relaxant effects of C. sappan, via endoge
nous NO and subsequent cGMP formation. The vascular relaxant effects of the
plant may contribute to its therapeutic actions. (C) 2000 Elsevier Science
Inc. All rights reserved.