Anti-allergic activity of emodin on IgE-mediated activation in RBL-2H3 cells

Abstract

BackgroundEmodin (1,3,8-trihydroxy-6-methylanthraquinone) is a Chinese herbal anthraquinone derivative from the rhizome of rhubarb (Rheum palmatum L.) that exhibits numerous biological activities, such as antitumor, antibacterial, antiinflammatory, and immunosuppressive. In the present studies, the anti-allergic activities of emodin were investigated to elucidate the underlying active mechanisms. MethodsThe inhibitory effects of emodin on the IgE-mediated allergic response in rat basophilic leukemia (RBL-2H3) cells were evaluated by measuring the release of granules and cytokines. The Ca2+ mobilization in RBL-2H3 cells loaded with the Ca2+-reactive fluorescent probe Fluo-4 AM was also measured by laser scanning confocal microscope. ResultsEmodin inhibited the release of β-hexosaminidase (β-HEX; IC50=5.5μM) and tumor necrosis factor (TNF)-α (IC50=11.5μM) from RBL-2H3 cells induced by 2,4-dinitrophenylated bovine serum albumin (DNP-BSA) and displayed stronger inhibition of β-HEX release than ketotifen fumarate salt (IC50=63.8μM). Emodin at a concentration of 12.5μM also inhibited the DNP-BSA-induced influx of extracellular Ca2+ in RBL-2H3 cells. ConclusionsThese results suggested that emodin likely exhibits anti-allergic activities via increasing the stability of the cell membrane and inhibiting extracellular Ca2+ influx.