Flavonoids Inhibit Histamine Release and Expression of Proinflamma-tory Cytokines in Mast Cells

Hyo-Hyun ParkSoyoung LeeHee-Young SonSeung-Bin ParkMi-Sun KimEun-Ju ChoiThoudam S.K. SinghJeoung-Hee HaMaan-Gee LeeJung-Eun KimMyung Chul HyunTaeg Kyu KwonYeo Hyang KimSang-Hyun Kim
Dept. of Immunology (면역학); Dept. of Pediatrics (소아청소년학)
Issue Date
Archives of Pharmacal Research, Vol.31(10) : 1303-1311, 2008
Mast cells participate in allergy and inflammation by secreting inflammatory mediators such as histamine and proinflammatory cytokines. Flavonoids are naturally occurring molecules with antioxidant, cytoprotective, and antiinflammatory actions. However, effect of flavonoids on the release of histamine and proinflammatory mediator, and their comparative mechanism of action in mast cells were not well defined. Here, we compared the effect of six flavonoids (astragalin, fisetin, kaempferol, myricetin, quercetin, and rutin) on the mast cell-mediated allergic inflammation. Fisetin, kaempferol, myricetin, quercetin, and rutin inhibited IgE or phorbol-12-myristate 13-acetate and calcium ionophore A23187 (PMACI)-mediated histamine release in RBL-2H3 cells. These five flavonoids also inhibited elevation of intracellular calcium. Gene expressions and secretion of proinflammatory cytokines such as tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, and IL-8 were assessed in PMACI-stimulated human mast cells (HMC-1). Fisetin, quercetin, and rutin decreased gene expression and production of all the proinflammatory cytokines after PMACI stimulation. Myricetin attenuated TNF-α and IL-6 but not IL-1β and IL-8. Fisetin, myricetin, and rutin suppressed activation of NF-κB indicated by inhibition of nuclear translocation of NF-κB, NF-κB/DNA binding, and NF-κB-dependent gene reporter assay. The pharmacological actions of these flavonoids suggest their potential activity for treatment of allergic inflammatory diseases through the down-regulation of mast cell activation.
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1. Journal Papers (연구논문) > 1. School of Medicine (의과대학) > Dept. of Immunology (면역학)
1. Journal Papers (연구논문) > 1. School of Medicine (의과대학) > Dept. of Pediatrics (소아청소년학)
Keimyung Author(s)
권택규; 김여향
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