Antispasmodic effects of essential oil of Pterodon polygalaeflorus and its main constituent beta-caryophyllene on rat isolated ileum

作者:Leonhardt Valeria; Leal Cardoso Jose H; Lahlou Saad; Albuquerque Aline A C; Porto Romulo S; Celedonio Natalia R; Oliveira Ariclecio C; Pereira Renalison F; Silva Leidiane P; Garcia Teofilo Taylena M N; Silva Anna P F S; Magalhaes Pedro J C; Duarte Gloria P; Coelho de Souza Andrelina N*
来源:Fundamental & Clinical Pharmacology, 2010, 24(6): 749-758.
DOI:10.1111/j.1472-8206.2009.00800.x

摘要

This study investigates the effects of essential oil of Pterodon polygalaeflorus (EOPP) and beta-caryophyllene (beta-CAR). EOPP and beta-CAR relaxed the basal tone of ileum smooth muscle in a concentration-dependent manner (IC(50)s = 394.35 +/- 62.12 and 68.65 +/- 9.51 mu g/mL respectively), an effect that was unaltered by hexamethonium, L-nitroarginine methyl ester or indomethacin. Both EOPP and beta-CAR evoked a concentration-dependent relaxation of ileum pre-contracted with KCl with an IC(50) value of 107.78 +/- 10.47 and 17.35 +/- 0.75 mu g/mL, respectively. EOPP and beta-CAR inhibited the contractions induced by acetylcholine (ACh) and by KCl. In ileal preparations, the CaCl(2)-induced contractions were reduced by EOPP (300 mu g/mL) and beta-CAR (100 mu g/mL). Furthermore, CaCl(2)-induced contractions were also reduced by EOPP (300 mu g/mL) and beta-CAR (100 mu g/mL) in ileal preparations pretreated with ACh under Ca2+-free condition and in the presence of verapamil. EOPP (100 and 300 mu g/mL) and beta-CAR (30 and 100 mu g/mL) reduced the ACh-induced contractions of isolated rat ileum under Ca2+-free conditions. In the presence of high KCl and Ca2+-free conditions, EOPP (300 mu g/mL) and beta-CAR (100 mu g/mL) reduced the contractions induced by barium. A similar effect was also observed with verapamil. It is concluded that (i) beta-CAR is an important constituent involved in the myorelaxant and antispasmodic effects induced by EOPP; (ii) the inhibitory effect on intestinal contractility is myogenic and seems mainly mediated through an intracellular mechanism. However, the ability of EOPP and beta-CAR to decrease Ca2+ influx through cytoplasmic membrane could not be discounted.

  • 出版日期2010-12