In Vitro Vasoactivity of Zerumbone from Zingiber zerumbet

Abstract

The sesquiterpene zerumbone, isolated from the rhizome of Zingiber zerumbet Sm., besides its widespread use as a food flavouring and appetiser, is also recommended in traditional medicine for the treatment of several ailments. It has attracted great attention recently for its effective chemopreventive and therapeutic effects observed in various models of cancer. To assess the zerumbone safety profile, a pharmacology study designed to flag any potential adverse effect on vasculature was performed. Zerumbone was tested for vasorelaxing activity on rat aorta rings and for L-type Ba²⁺ current blocking activity on single myocytes isolated from the rat-tail artery. The spasmolytic effect of zerumbone was more marked on rings stimulated with 60 mM than with 30 mM K⁺ (IC₅₀ values of 16 µM and 102 µM, respectively). In the presence of 60 mM K⁺, zerumbone concentration-dependently inhibited the contraction induced by the cumulative additions of Ca²⁺, this inhibition being inversely related to the Ca²⁺ concentration. Phenylephrine-induced contraction was inhibited by the drug, though less efficiently and independently of the presence of an intact endothelium, without affecting Ca²⁺ release from the intracellular stores. Zerumbone inhibited the L-type Ba²⁺ current (estimated IC₅₀ value of 458.7 µM) and accelerated the kinetics of current decay. In conclusion, zerumbone showed an overall weak in vitro vasodilating activity, partly attributable to the blocking of the L-type Ca²⁺ channel, which does not seem to represent, however, a serious threat to its widespread use.

Key words

Zingiber zerumbet - Zingiberaceae - zerumbone - L-type Ca²⁺ channel - whole-cell patch-clamp - vascular smooth muscle

• References

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