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1.
Pakistan Journal of Pharmaceutical Sciences. 2011; 24 (4): 427-433
in English | IMEMR | ID: emr-137540

ABSTRACT

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


elaxation 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


Subject(s)
Animals, Laboratory , Male , Aegle/chemistry , Coumarins/isolation & purification , Trachea/drug effects , p-Methoxy-N-methylphenethylamine/pharmacology , Muscle, Smooth/drug effects , Muscle Relaxation/drug effects , Muscle Contraction/drug effects , Guinea Pigs
2.
Pakistan Journal of Pharmaceutical Sciences. 2011; 24 (3): 359-367
in English | IMEMR | ID: emr-129863

ABSTRACT

Aegeline or 7V-[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[2]4-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 DNP24-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 ofaegeYme 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


Subject(s)
Animals, Laboratory , Male , Histamine Release/drug effects , Mast Cells/drug effects , Amides/pharmacology , Herb-Drug Interactions , Rats, Wistar , Cell Line, Tumor , Dinitrophenols/pharmacology , Ionomycin/pharmacology , Mast Cells/metabolism , Thapsigargin/pharmacology
3.
Journal of Basic and Applied Sciences. 2010; 6 (2): 141-148
in English | IMEMR | ID: emr-105348

ABSTRACT

Skimmianine is a quinoline alkaloid isolated from the roots of Aegle marmelos Correa. In the study, we studied the effects of skimmianine on the histamine release from rat mast cells. The study was performed by using two cell lines, rat basophilic leukemia [RBL-2H3] cell line, and rat peritoneal mast cells [RPMCs]. DNP[24]-BSA, thapsigargin, ionomycin, compound 48/80 and PMA were used as inducers for histamine release from rat mast cell. Skimmianine markedly inhibited the histamine release from RBL-2H3 cells induced by DNP[24]-BSA, thapsigargin and ionomycin. The effect suggested is related to Ca[2+] signaling since skimmianine showed strong effects when the histamine release induced by Ca[2+] signal stimulants [thapsigargin and ionomycin]. It is supported that skimmianine altered the influx of [45] Ca[2+] into the cells. In RPMCs experiment, skimmianine also suppressed the histamine release induced by Ca[2+] stimulants, and phorbol myristate acetate [PMA]. However, skimmianine had no effect on the histamine release induced by compound 48/80. Based on the results, the inhibitory effects of skimmianine on the histamine release from mast cells might involve some mechanisms related to intracellular Ca[2+] signaling events and protein kinase C signaling possessing a main role in granule exocytotic processes


Subject(s)
Animals, Laboratory , Plant Roots , Mast Cells , Quinolines , Histamine , Histamine Release , Plants, Medicinal , Rats , Histamine Antagonists
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