The development of new-type quinine derivatives regulating calcium channel

从小叶Ehretia microphylla分离得到的微叶虫素在μM浓度下对RBL-2H3细胞的胞吐有抑制作用。测定了一种新型抗过敏化合物微叶黄的理化和生物学特性。微叶黄酮在不同刺激下抑制RBL-2H3细胞、大鼠肥大细胞和人嗜碱性细胞的胞外分泌。微叶黄酮通过刺激抑制细胞内钙离子浓度的增加，这是由于抑制钙通过钙释放活化钙（CRAC）通道流入。在以下过敏模型中也测定了微叶黄酮的作用：微叶黄酮抑制被动皮肤过敏反应和蛔虫诱导的双相皮肤过敏反应的即时期。另一方面，微叶龙素对晚期蛔虫诱导的双相皮肤过敏反应和恶唑酮诱导的接触型延迟性皮肤反应等iv型过敏模式无影响。微叶黄酮是一种新型抗过敏药和/或新型抗过敏药的先导化合物，用于治疗急性过敏反应。

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.