Abstract
Objective: Alpha-isocubebene (α-ICB) is a compound isolated from Schisandra chinensis fruit which is a well-known as a useful material in the preventive or treatment of cardiovascular symptoms in Korean. Design and method: In the present study, the vasoactivities of α-ICB were evaluated in the isolated thoracic aorta of mice (8-week-old male C57/BL6). Results: In isolated rings of aorta (about 2 mm in width), phenylephrine (0.1–3.0 μM), adrenergic α-receptor agonist, or norepinephrine (10–300 nM) induced vasocontraction in dose-dependent manners, which were markedly attenuated by α-ICB (1–10 μg/ml) in a concentration-dependent manner. However, α-ICB had no effects on vasodilation induced by acetylcholine (10–300 nM). These results suggested that α-ICB regulated vasocontraction via regulation of contractile machine including myosin light chain (MLC) on the vasculature. In the immunoblot analysis, α-ICB inhibited phosphorylation of MLC at the sites of Thr18 and Thr18/Ser19. The effects on Thr18 phosphorylation were more prominent than that at The18/Ser19 sites, suggesting a pivotal involvement of MLC phosphatase in the modulation of vasocontraction by α-ICB. Conclusions: Collectively, α-ICB attenuated vasocontraction induced by various agonists through inhibition of MLC phosphorylation via an increased activity of MLC phosphatase.
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