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The development of new-type quinine derivatives regulating calcium channel

新型钙通道调节奎宁衍生物的研制

基本信息

批准号：
14380289
负责人：
OHTANI Kazuhiro
金额：
$ 7.04万
依托单位：
Kochi University (2003-2004)Hiroshima University (2002)
依托单位国家：
日本
项目类别：
Grant-in-Aid for Scientific Research (B)
财政年份：
2002
资助国家：
日本
起止时间：
2002 至 2004
项目状态：
已结题

项目摘要

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.

从小叶厚壳中分离得到的小叶酮在μM浓度下对RBL-2 H3细胞的胞吐有抑制作用。对一种新型抗过敏化合物小叶乙酮的理化性质和生物学特性进行了研究。小叶绿酮抑制RBL-2 H3细胞、大鼠肥大细胞和人嗜碱性粒细胞的胞吐作用。小叶绿酮抑制刺激引起的细胞内钙离子浓度的增加，这是由于抑制通过钙释放激活的钙（CRAC）通道的钙流入。在以下过敏模型中也测定了叶绿酮的作用：叶绿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相。另一方面，叶绿酮对IV型变态反应模式如蛔虫诱导的双相皮肤变态反应的晚期和恶唑酮诱导的接触型迟发性皮肤反应没有影响。小叶绿酮被认为是一种新型的抗过敏药物和/或一类新型抗过敏药物的先导化合物。