Imperatorin, a psoralen-type furanocoumarin, is a potent myorelaxant agent acting as a calcium antagonist on vascular smooth muscle. Its effects on other types of smooth muscle remain unknown. Therefore, the aim of this study was to investigate the hypothesized myorelaxant effect of imperatorin on gut motor activity and, possibly, to define the underlying mechanism of action. Imperatorin was made available for pharmacological studies from the fruits of the widely available Angelica officinalis through the application of high-performance countercurrent chromatography (HPCCC). Imperatorin generated reversible relaxation of jejunum strips dose-dependently (1-100 μM). At 25 and 50 μM, imperatorin caused relaxation comparable to the strength of the reaction induced by isoproterenol (Isop) at 0.1 μM. The observed response resulted neither from the activation of soluble guanylate cyclase, nor from β-adrenoreceptor involvement, nor from Ca(2+)-activated potassium channels. Imperatorin relaxed intestine strips precontracted with high potassium concentration, attenuated the force and duration of K(+)-induced contractions, and modulated the response of jejunum strips to acetylcholine. The results suggest that imperatorin probably interacts with various Ca(2+) influx pathways in intestine smooth muscle. The types of some calcium channels involved in the activity of imperatorin will be examined in a subsequent study.
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| http://dx.doi.org/10.1155/2015/614849 | DOI Listing |
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