Zullies Ikawati, Elizabeth Wallgard, Kazutaka Maeyama


The dual effects of the flavonoid quercetin on rat basophilic leukemia cells (RBL-2H3), tumor analog mast cells, was studied. Quercetin is known as an anti-inflammatory drug that inhibits mast cell secretion of histamine. This study aims to investigate the consequences of varying incubation times with quercetin on 2H3 cells to histamine release inhibitory action and the effects of long time incubation to the morphology of the cells. The effect of quercetin on histamine synthesis was also observed. The histamine release from the cells was inhibited by quercetin as expected, but the ability of secretion was rapidly recovered when quercetin was removed before challenging. Incubation up to 6 hours decreased the inhibitory action, but longer than 6 hours increased the inhibitory activity. In long time incubation, the cells exhibited cell damage, decreased cell growth, morphological changes, and detachment from the underlying surface in proportion with the concentration of quercetin. The instant and reversible inhibitory effects of quercetin appear to represent a first phase of actions, while reduced cell growth, elevated cell damage and morphological changes seem to be connected to a second phase. Consequently, quercetin could be considered as a compound that acts dually on RBL-2H3 cells.

Key words : quercetin, histamine, RBL-2H3 cells

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Barsumian, E.L., Isersky, C., Petrino, M.G., Siraganian, R.P., 1981. IgE-induced Histamine Release from Rat Basophilic Leukemia Cell Line: Isolation of Releasing and Nonreleasing Clones. Eur. J. Immunol., 11, 317-323

Dale, M.M., and Foreman, J.C.; 1994, Histamine as a Mediator of Allergic and Inflammatory Reactions, in Textbook of Immunopharmacology (M.Dale, J.C.Foreman, F.Tai-Ping, Eds.), 3rd Ed., Blackwell Scientific Publications, Oxford. 123-131

Ferriola, P.C., Cody, V., Middleton, E.Jr., 1989. Protein Kinase C Inhibition by Plant Flavonoids, Kinetic Mechanism and Structure-activity Relationships. Biochem. Pharmacol., 38, 1617-1624

Fewtrell, C.M., and Gomperts, B.D., 1977. Quercetin: a Novel Inhibitor of Ca2+ Influx and Exocytosis in Rat Peritoneal Mast Cells. Biochem. Biophys. Acta, 469, 52-60

Foreman, J.; 1994, Mast Cells and Basophils Leucocyte, in Textbook of Immunopharmacology (M.Dale, J.C.Foreman, F.Tai-Ping, Eds.), 3rd Ed., Blackwell Scientific Publications, Oxford. 21-23

Formica, J.V., and Regelson, W., 1995. Review of the Biology of Quercetin and Related Biflavonoids. Food Chem. Toxicol., 33, 1061-1080

Maeyama, K., Yagi, S., Watanabe, T., 1992. Histamine Release from Rat Basophilic Leukemia Cells (RBL-2H3). Ann. Psychiatry, 3, 67-77

Middleton, E.Jr., Kandaswami, C., Theoharides, T.C., 2000. The Effect of Plant Flavonoids on Mammalian Cells: Implications for Inflammation, Heart Disease, and Cancer. Pharmacol. Rev., 52, 673-751

Richter, M., Ebermann, R., Marian, B., 1999. Quercetin-induced Apoptosis in Colorectal Tumor Cells: Possible Role of EGF Receptor Signaling. Nutr Cancer, 34, 88-89

Senyshyn, J., Baumgartner, R.A., Beaven, M.A., 1998. Quercetin Sensitizes RBL-2H3 to Polybasic Mast Cell Secretagogue through Increased Expression of GTP-binding Protein Linked to a Phospholipase C Signaling Pathway. J. Immunol., 160, 5136-5144

Shoshan, V., Shahak, Y., Shavit, N., 1980. Quercetin Interaction with the Chloroplast ATPase Complex. Biochem Biophys Acta, 59, 421-433

Watanabe, T., Taguchi, K., Maeyama, K., Wada, H., 1991. Formation of Histamine: Histidine Decarboxylase, in Handbook of Experimental Pharmacology, (B. Uvnas, Ed.), Vol 97, Springer-Verlag, Berlin, 145-163

Yamatodani, A., Fukuda, H., Iwaeda, T, Watanabe, T., Wada, H., 1985. HPLC Determination of Plasma and Brain Histamine without Previous Purification of Biological Samples: Cation Exchange Chromatography Coupled with Post-column Derivatization Fluorometry. J. Chromatogr., 244, 115-123

Yoshida, M., Sakai, T., Ninoshino, H., Aoike, A., Kawai, K., Nagata, K., 1990. Flavonoids Inhibit the Expression of Heat Shock Proteins. Cell Struct.Funct., 15, 393-401

DOI: http://dx.doi.org/10.14499/indonesianjpharm0iss0pp55-64


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