Abstract
The present study used isometric tension recording to investigate the vasorelaxant effect of limonene (LM), carveol (CV), and perillyl alcohol (POH) on contractility parameters of the rat aorta, focusing in particular on the structure-activity relationship. LM, CV, and POH showed a reversible inhibitory effect on the contraction induced by electromechanical and pharmacomechanical coupling. In the case of LM, but not CV and POH, this effect was influenced by preservation of the endothelium. POH and CV but not LM exhibited greater pharmacological potency on BayK-8644-induced contraction and on electromechanical coupling than on pharmacomechanical coupling. In endothelium-denuded preparations, the order of pharmacological potency on electrochemical coupling was LM < CV < POH. These compounds inhibited also, with grossly similar pharmacological potency, the contraction induced by phorbol ester dibutyrate. The present results suggest that LM, CV and POH induced relaxant effect on vascular smooth muscle by means of different mechanisms likely to include inhibition of PKC and IP3 pathway. For CV and POH, hydroxylated compounds, it was in electromechanical coupling that the greater pharmacological potency was observed, thus suggesting a relative specificity for a mechanism likely to be important in electromechanical coupling, for example, blockade of voltage-dependent calcium channel.
Highlights
Monoterpenes and monoterpenoids, the major chemical components of essential oils, are made of two isoprene units [1,2]
Results are shown as means ± standard error of the mean (SEM). * indicates a*
Our main finding indicates that perillyl alcohol (POH), CV, and LM had a relaxant effect on several types of contraction
Summary
Monoterpenes and monoterpenoids, the major chemical components of essential oils, are made of two isoprene units [1,2]. They have shown several pharmacological activities such as antioxidant, anti-inflammatory, antiedematogenic, gastroprotective, and anti-hypertensive [3,4,5,6,7]. Thymol, eugenol, methyleugenol, 1,8-cineole, and terpinen-4-ol are small monoterpenoids, which exhibited vasorelaxant effects on isolated rat aorta [9,10,11,12,13,14]. 1,8-cineole and citronellol have been reported to elicit hypotension in normotensive rats [15,16].
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