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1.
Asian Pacific Journal of Tropical Medicine ; (12): 1043-1046, 2017.
Article in Chinese | WPRIM | ID: wpr-972544

ABSTRACT

Objective To investigate the effects of friedelin (terpenoid) and 8-hydroxyisocapnolactone-2-3-diol (coumarin) with concentration 10 μM, 30 μM, and 100 μM on inhibiting mast cells (MCs) degranulation. Methods The investigation was performed in vitro by administering each compound into rat peritoneal MCs and rat basophilic leukemia-2H3 cells followed by activation with 50 μg/mL of compound 48/80 or 1 μM of ionomycin. The concentration of histamine released from each group was measured by a high-performance liquid chromatography-fluorometry system with post-column derivatization using o-phthalaldehyde. Results 8-Hydroxyisocapnolactone-2-3-diol inhibited degranulation of compound 48/80 activated-rat peritoneal MCs with the histamine release percentages of 74.57%, 72.21% and 51.79% when the 10 μM, 30 μM and 100 μM concentrations were used, respectively. Where as about 81% histamine was released by the control group. Degranulation inhibition ability was also observed in ionomycin-activated rat basophilic leukemia-2H3 cells. In contrast, friedelin failed to inhibit degranulation in either cell type. The inhibition of 8-hydroxyisocapnolactone-2-3-diol was not related to the depletion of histamine synthesis as implied by the total histamine measurement. Conclusions These results exhibit the promising of 8-hydroxyisocapnolactone-2-3-diol is a potential parent structure for developing a MCs stabilizer.

2.
Asian Pacific Journal of Tropical Medicine ; (12): 1043-1046, 2017.
Article in English | WPRIM | ID: wpr-819420

ABSTRACT

OBJECTIVE@#To investigate the effects of friedelin (terpenoid) and 8-hydroxyisocapnolactone-2-3-diol (coumarin) with concentration 10 μM, 30 μM, and 100 μM on inhibiting mast cells (MCs) degranulation.@*METHODS@#The investigation was performed in vitro by administering each compound into rat peritoneal MCs and rat basophilic leukemia-2H3 cells followed by activation with 50 μg/mL of compound 48/80 or 1 μM of ionomycin. The concentration of histamine released from each group was measured by a high-performance liquid chromatography-fluorometry system with post-column derivatization using o-phthalaldehyde.@*RESULTS@#8-Hydroxyisocapnolactone-2-3-diol inhibited degranulation of compound 48/80 activated-rat peritoneal MCs with the histamine release percentages of 74.57%, 72.21% and 51.79% when the 10 μM, 30 μM and 100 μM concentrations were used, respectively. Where as about 81% histamine was released by the control group. Degranulation inhibition ability was also observed in ionomycin-activated rat basophilic leukemia-2H3 cells. In contrast, friedelin failed to inhibit degranulation in either cell type. The inhibition of 8-hydroxyisocapnolactone-2-3-diol was not related to the depletion of histamine synthesis as implied by the total histamine measurement.@*CONCLUSIONS@#These results exhibit the promising of 8-hydroxyisocapnolactone-2-3-diol is a potential parent structure for developing a MCs stabilizer.

3.
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
4.
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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