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Effects of luteolin, quercetin and baicalein on immunoglobulin E‐mediated mediator release from human cultured mast cells
Author(s) -
Masahiro Kimata,
Michitaka Shichijo,
Tsuyoshi Miura,
Isao Serizawa,
Nobuya Inagaki,
Hiroichi Nagai
Publication year - 2000
Publication title -
clinical and experimental allergy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.462
H-Index - 154
eISSN - 1365-2222
pISSN - 0954-7894
DOI - 10.1046/j.1365-2222.2000.00768.x
Subject(s) - luteolin , baicalein , histamine , immunoglobulin e , protein kinase c , mapk/erk pathway , p38 mitogen activated protein kinases , mast cell , chemistry , quercetin , allergic inflammation , kinase , signal transduction , pharmacology , jurkat cells , biochemistry , microbiology and biotechnology , biology , immunology , inflammation , antibody , t cell , antioxidant , immune system
Background Flavonoids have a variety of activities including anti‐allergic activities, and are known to inhibit histamine release from human basophils and murine mast cells. Objective The effects of luteolin, a flavone, on the immunoglobulin (Ig) E‐mediated allergic mediator release from human cultured mast cells (HCMCs) were investigated and compared with those of baicalein and quercetin. Methods HCMCs were sensitized with IgE, and then treated with flavonoids before challenge with antihuman IgE. The amount of released mediators was determined as was mobilization of intracellular Ca 2+ concentration, protein kinase C (PKC) translocation and phosphorylation of intracellular proteins were detected after anti‐IgE stimulation. Results Luteolin, baicalein and quercetin inhibited the release of histamine, leukotrienes (LTs), prostaglandin D 2 (PGD 2 ), and granulocyte macrophage‐colony stimulating factor (GM‐CSF) from HCMC in a concentration‐dependent manner. Additionally, the three flavonoids inhibited A23187‐induced histamine release. As concerns Ca 2+ signalling, luteolin and quercetin inhibited Ca 2+ influx strongly, although baicalein did slightly. With regard to PKC signalling, luteolin and quercetin inhibited PKC translocation and PKC activity strongly, although baicalein did slightly. The suppression of Ca 2+ and PKC signallings might contribute to the inhibition of mediator release. The activation of extracellular signal‐regulated kinases (ERKs) and c‐Jun NH2‐terminal kinase (JNK), that were activated just before the release of LTs and PGD 2 and GM‐CSF mRNA expression in IgE‐mediated signal transduction events, were clearly suppressed by luteolin and quercetin. In contrast, the flavonoids did not affect the activation of p38 mitogen‐activated protein kinase (p38 MAPK) pathway. Conclusion These results indicate that luteolin is a potent inhibitor of human mast cell activation through the inhibition of Ca 2+ influx and PKC activation.