TY - JOUR
T1 - Antispasmodic effects of essential oil of Pterodon polygalaeflorus and its main constituent β-caryophyllene on rat isolated ileum
AU - Leonhardt, Valeria
AU - Leal-Cardoso, José H.
AU - Lahlou, Saad
AU - Albuquerque, Aline A.C.
AU - Porto, Romulo S.
AU - Celedônio, Natalia R.
AU - Oliveira, Ariclecio C.
AU - Pereira, Renalison F.
AU - Silva, Leidiane P.
AU - Garcia-Teófilo, Taylena M.N.
AU - Silva, Anna P.F.S.
AU - Magalhães, Pedro J.C.
AU - Duarte, Gloria P.
AU - Coelho-De-Souza, Andrelina N.
PY - 2010/12
Y1 - 2010/12
N2 - This study investigates the effects of essential oil of Pterodon polygalaeflorus (EOPP) and β-caryophyllene (β-CAR). EOPP and β-CAR relaxed the basal tone of ileum smooth muscle in a concentration-dependent manner (IC50s = 394.35 ± 62.12 and 68.65 ± 9.51 μg/mL respectively), an effect that was unaltered by hexamethonium, L-nitroarginine methyl ester or indomethacin. Both EOPP and β-CAR evoked a concentration-dependent relaxation of ileum pre-contracted with KCl with an IC50 value of 107.78 ± 10.47 and 17.35 ± 0.75 μg/mL, respectively. EOPP and β-CAR inhibited the contractions induced by acetylcholine (ACh) and by KCl. In ileal preparations, the CaCl2-induced contractions were reduced by EOPP (300 μg/mL) and β-CAR (100 μg/mL). Furthermore, CaCl2-induced contractions were also reduced by EOPP (300 μg/mL) and β-CAR (100 μg/mL) in ileal preparations pretreated with ACh under Ca2+-free condition and in the presence of verapamil. EOPP (100 and 300 μg/mL) and β-CAR (30 and 100 μg/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 μg/mL) and β-CAR (100 μg/mL) reduced the contractions induced by barium. A similar effect was also observed with verapamil. It is concluded that (i) β-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 β-CAR to decrease Ca2+ influx through cytoplasmic membrane could not be discounted.
AB - This study investigates the effects of essential oil of Pterodon polygalaeflorus (EOPP) and β-caryophyllene (β-CAR). EOPP and β-CAR relaxed the basal tone of ileum smooth muscle in a concentration-dependent manner (IC50s = 394.35 ± 62.12 and 68.65 ± 9.51 μg/mL respectively), an effect that was unaltered by hexamethonium, L-nitroarginine methyl ester or indomethacin. Both EOPP and β-CAR evoked a concentration-dependent relaxation of ileum pre-contracted with KCl with an IC50 value of 107.78 ± 10.47 and 17.35 ± 0.75 μg/mL, respectively. EOPP and β-CAR inhibited the contractions induced by acetylcholine (ACh) and by KCl. In ileal preparations, the CaCl2-induced contractions were reduced by EOPP (300 μg/mL) and β-CAR (100 μg/mL). Furthermore, CaCl2-induced contractions were also reduced by EOPP (300 μg/mL) and β-CAR (100 μg/mL) in ileal preparations pretreated with ACh under Ca2+-free condition and in the presence of verapamil. EOPP (100 and 300 μg/mL) and β-CAR (30 and 100 μg/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 μg/mL) and β-CAR (100 μg/mL) reduced the contractions induced by barium. A similar effect was also observed with verapamil. It is concluded that (i) β-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 β-CAR to decrease Ca2+ influx through cytoplasmic membrane could not be discounted.
KW - β-caryophyllene
KW - Antispasmodic effect
KW - Essential oil
KW - Ileal smooth muscle
KW - Pterodon polygalaeflorus
UR - http://www.scopus.com/inward/record.url?scp=78349267226&partnerID=8YFLogxK
U2 - 10.1111/j.1472-8206.2009.00800.x
DO - 10.1111/j.1472-8206.2009.00800.x
M3 - Article
C2 - 20015227
AN - SCOPUS:78349267226
SN - 0767-3981
VL - 24
SP - 749
EP - 758
JO - Fundamental and Clinical Pharmacology
JF - Fundamental and Clinical Pharmacology
IS - 6
ER -