Journal of Pharmacological Sciences (Jan 2004)

The Phenoxazine Derivative Phx-1 Suppresses IgE-Mediated Degranulation in Rat Basophilic Leukemia RBL-2H3 Cells

  • Eisuke Enoki,
  • Kiyonao Sada,
  • Xiujuan Qu,
  • Shinkou Kyo,
  • S.M. Shahjahan Miah,
  • Tomoko Hatani,
  • Akio Tomoda,
  • Hirohei Yamamura

Journal volume & issue
Vol. 94, no. 3
pp. 329 – 333

Abstract

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Antigen-induced aggregation of the high affinity IgE receptor (FcεRI) 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-4,4α-dihydro-4α,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. Keywords:: phenoxazine derivative, mast cell, degranulation