The development of new-type quinine derivatives regulating calcium channel

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Microphyllone isolated from Ehretia microphylla has an inhibitory activity on exocytosis in RBL-2H3 cells at μM concentration. The physicochemical and biological characters of microphyllone as a novel anti-allergic compound were determined. Microphyllone inhibited exocytosis in RBL-2H3 cells, rat mast cells and human basophiles with various stimuli. Microphyllone inhibited an increase in concentration of intracellular calcium ion by stimulation, which is due to inhibition of calcium influx through the calcium release-activated calcium (CRAC) channel. The effects of microphyllone were also determined in the following allergic models : Microphyllone suppressed passive cutaneous anaphylaxis reaction and immediate phase of ascaris-induced biphasic skin allergic reaction. On the other hand, microphyllone has no effect on Type-IV allergic modes such as the late phase of ascaris-induced biphasic skin allergic reaction and oxazolone-induced contact type delayed cutaneous reaction. Microphyllone is proposed as a new type of anti-allergic and/or a lead compound for new class anti-allergies against acute allergic reactions.