Licochalcones suppress degranulation by decreasing the intracellular Ca2+ level and tyrosine phosphorylation of ERK in RBL-2H3 cells
Autor: | Eriko Aizu-Yokota, Hideo Inoue, Yoshiko Sonoda, Megumi Funakoshi-Tago, Tadashi Kasahara, Shota Tanifuji |
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Rok vydání: | 2010 |
Předmět: |
MAPK/ERK pathway
Licochalcone A Immunology Anti-Inflammatory Agents Intracellular Space Plant Roots Cell Degranulation Allergic inflammation Structure-Activity Relationship chemistry.chemical_compound Chalcones Cell Line Tumor Glycyrrhiza Extracellular Animals Immunology and Allergy Phosphorylation Extracellular Signal-Regulated MAP Kinases Pharmacology Degranulation Tyrosine phosphorylation Basophils Rats Cell biology chemistry Cytoprotection Tyrosine Calcium Histamine Intracellular Phytotherapy Signal Transduction |
Zdroj: | International Immunopharmacology. 10:769-776 |
ISSN: | 1567-5769 |
DOI: | 10.1016/j.intimp.2010.04.007 |
Popis: | Mast cells play a key role in allergic inflammation by releasing various mediators, such as histamine, serotonin, leukotrienes and cytokines. A signaling cascade of events activated by stimulation with antigens contributes to the regulation of mast cell degranulation. While various anti-inflammatory and anti-allergic drugs have been developed that inhibit degranulation of mast cells, the inhibitory mechanism has been poorly understood. Licochalcone A (Lico A) is a retrochalcone isolated from the root of Xinjiang liquorice and has been reported to exhibit various biological activities such as anti-inflammatory activity. We examined the effects of Lico A and related chalcones on degranulation in a rat basophilic leukemia cell line, RBL-2H3. Whereas Lico A and licochalcone C (Lico C) exhibited inhibitory activity with cytotoxicity, licochalcone D (Lico D) significantly inhibited the degranulation in RBL-2H3 cells with low cytotoxicity. Moreover, Lico D significantly inhibited the Ca2+ influx and phosphorylation of extracellular signal regulated kinase (ERK) and MEK. These results suggest that Lico D inhibits mast cell degranulation via the inhibition of both extracellular Ca2+ influx and activation of the MEK-ERK pathway. |
Databáze: | OpenAIRE |
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