Hypotensive effect of butein via the inhibition of angiotensin converting enzyme

Abstract

Butein (3,4,2′,4′-tetrahydroxychalcone), a plant polyphenol, has been known to elucidate endothelium-dependent vasodilation. In the present study, the hypotensive effect of butein and its possible mechanism, especially an angiotensin converting enzyme (ACE) inhibitory effect, were investigated. Intravenous injection of butein lowered the arterial blood pressure of anesthetized rats in a dose-dependent manner. The plasma ACE activities were significantly inhibited by the addition of butein in a dose-dependent manner, the IC50 value of which was 198 μg/ml (730 μM). Moreover, angiotensin I-induced contraction was markedly attenuated by prior exposure of endothelium-intact aortic rings to butein, but angiotensin II-induced contraction was not altered. These results suggest that butein has a hypotensive effect, at least in part, via the inhibition of angiotensin converting enzyme. © 2003 Pharmaceutical Society of Japan.