The phenoxazine derivative Phx-1 suppresses IgE-mediated degranulation in rat basophilic leukemia RBL-2H3 cells
The phenoxazine derivative Phx-1 suppresses IgE-mediated degranulation in rat basophilic leukemia RBL-2H3 cells
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DOI：
10.1254/jphs.94.329
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发表时间：
2004-03-01
影响因子：
3.5
通讯作者：
Yamamura, H
中科院分区：
文献类型：
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作者：
Enoki, E;Sada, K;Yamamura, H
抗原诱导的高亲和力IgE受体（Fc ε RI）在肥大细胞上的聚集诱导脱粒以释放化学介质，导致急性过敏性炎症。我们已经证明，用吩恶嗪衍生物Phx-1（2-氨基-4，4 α-二氢-4 α，7-二甲基-3H-吩恶嗪-3-酮）处理大鼠肥大细胞RBL-2 H3可抑制抗原诱导的脱粒。生化分析表明，通过Gab 2和Akt的互补信号通路被该化合物抑制在肥大细胞中。这些发现表明，吩恶嗪衍生物可能具有通过抑制肥大细胞脱粒治疗过敏性疾病的潜力。
Antigen-induced aggregation of the high affinity IgE receptor (FcepsilonRI) on mast cells induces degranulation to release chemical mediators, leading to acute allergic inflammation. We have demonstrated that the treatment of rat mast cells, RBL-2H3, with a phenoxazine derivative Phx-1 (2-amino-4,4alpha-dihydro-4alpha,7-dimethyl-3H-phenoxazine-3-one) suppresses the antigen-induced degranulation. Biochemical analysis reveals that the complementary signaling pathway through Gab2 and Akt is inhibited by this compound in mast cells. These findings suggest that phenoxazine derivatives may have a therapeutic potential for allergic diseases by inhibiting mast cell degranulation.