RESUMEN
Marmin or 7-(6',7'-dihydroxygeranyl-oxy)coumarin is a compound isolated from Aegle marmelos Correa. In the study, we examined the effects of marmin on the contraction of guinea pig-isolated trachea stimulated by several inducers, namely histamine, metacholine, compound 48/80. We also evaluated its action against contraction induced by extracellular or intracellular calcium ion. The possibility of marmin to potentiate the relaxation effect of isoprenaline was also studied. Marmin added in the organ bath at 10 min prior to the agonist inhibited the contraction elicited by histamine and metacholine in a concentration-dependent manner. Moreover, marmin antagonized the histamine-induced contraction in competitive manner. Marmin mildly potentiated the relaxation effect of isoprenaline. In the study, marmin abrogated the contraction of tracheal smooth muscle induced by compound 48/80, an inducer of histamine release. Besides, marmin successfully inhibited CaCl(2)-induced contraction in Ca(2+)-free Krebs solution. Marmin also inhibited two phases of contraction which were consecutively induced by metacholine and CaCl(2) in Ca(2+)-free Krebs solution. Based on the results we concluded that marmin could inhibit contraction of the guinea-pig tracheal smooth muscle, especially by interfering histamine receptor, inhibiting the histamine release from mast, inhibiting intracellular Ca(2+) release from the intracellular store and the Ca(2+) influx through voltage-dependent Ca(2+) channels.
Asunto(s)
Aegle/química , Cumarinas/farmacología , Contracción Muscular/efectos de los fármacos , Músculo Liso/efectos de los fármacos , Tráquea/efectos de los fármacos , Animales , Cloruro de Calcio/farmacología , Cumarinas/aislamiento & purificación , Cobayas , Histamina/farmacología , Técnicas In Vitro , Isoproterenol/farmacología , Masculino , Cloruro de Metacolina/farmacología , Contracción Muscular/fisiología , Relajación Muscular/efectos de los fármacos , Relajación Muscular/fisiología , Músculo Liso/fisiología , Tráquea/fisiología , p-Metoxi-N-metilfenetilamina/farmacologíaRESUMEN
Aegeline or N-[2-hydroxy-2(4-methoxyphenyl) ethyl]-3-phenyl-2-propenamide is a main alkaloid isolated from Aegle marmelos Correa collected in Yogyakarta Indonesia. In our study, we investigated the effects of aegeline on the histamine release from mast cell. The study was performed by using (1) rat basophilic leukemia (RBL-2H3) cell line, and (2) rat peritoneal mast cells (RPMCs). DNP(24)-BSA, thapsigargin, ionomycin, compound 48/80 and PMA were used as inducers for histamine release from mast cell. In our study, aegeline inhibited the histamine release from RBL-2H3 cells induced by DNP(24)-BSA. Indeed, aegeline showed strong inhibition when RBL-2H3 cells induced by Ca(2+) stimulants such as thapsigargin and ionomycin. Aegeline is suggested to influence the intracellular Ca(2+) pool only since could not inhibit the (45)Ca(2+) influx into RBL-2H3 cells. Aegeline showed weak inhibitory effects on the histamine release from RPMCs, even though still succeed to inhibit when the histamine release induced by thapsigargin. These findings indicate that aegeline altered the signaling pathway related to the intracellular Ca(2+) pool in which thapsigargin acts. Based on the results, the inhibitory effects of aegeline on the histamine release from mast cells depended on the type of mast cell and also involved some mechanisms related to intracellular Ca(2+) signaling events via the same target of the action of thapsigargin or downstream process of intracellular Ca(2+) signaling in mast cells.
Asunto(s)
Aegle/química , Amidas/farmacología , Interacciones de Hierba-Droga , Liberación de Histamina/efectos de los fármacos , Mastocitos/efectos de los fármacos , Amidas/aislamiento & purificación , Animales , Calcio/metabolismo , Técnicas de Cultivo de Célula , Línea Celular Tumoral , Dinitrofenoles/antagonistas & inhibidores , Dinitrofenoles/farmacología , Ionomicina/antagonistas & inhibidores , Ionomicina/farmacología , Masculino , Mastocitos/metabolismo , Ratas , Ratas Wistar , Albúmina Sérica Bovina/antagonistas & inhibidores , Albúmina Sérica Bovina/farmacología , Acetato de Tetradecanoilforbol/antagonistas & inhibidores , Acetato de Tetradecanoilforbol/farmacología , Tapsigargina/antagonistas & inhibidores , Tapsigargina/farmacología , p-Metoxi-N-metilfenetilamina/antagonistas & inhibidores , p-Metoxi-N-metilfenetilamina/farmacologíaRESUMEN
Phytochemical studies on the rhizomes of Etlingera elatior have resulted in the isolation of 1,7-bis(4-hydroxyphenyl)-2,4,6-heptatrienone (1), demethoxycurcumin (2), 1,7-bis(4-hydroxyphenyl)-1,4,6-heptatrien-3-one (3), 16-hydroxylabda-8(17),11,13-trien-15,16-olide (4), stigmast-4-en-3-one, stigmast-4-ene-3,6-dione, stigmast-4-en-6beta-ol-3-one, and 5alpha,8alpha-epidioxyergosta-6,22-dien-3beta-ol. Compounds 1 and 4 are new, and their structures were elucidated by analysis of spectroscopic data. Diarylheptanoids 1-3 were found to inhibit lipid peroxidation in a more potent manner than alpha-tocopherol.