苯并异硒唑酮磺酰胺类化合物的抗炎作用

THE ANTI-INFLAMMATORY ACTIONS OF BENZOISOSELENOTHIAZOLIDONESULFONAMIDE DERIVATIVES

目的 研究苯并异硒唑酮磺酰胺类化合物A和B抗炎作用。方法 Boyden小室法测定中性粒细胞趋化 ;紫外分光光度法测定髓过氧化物酶活性 ;染色法测定肥大细胞脱颗粒。结果 化合物A和B均可抑制fMLPP诱导的兔外周血中性粒细胞趋化反应 ;外涂给药均可抑制巴豆油引起的小鼠髓过氧化物酶的升高。在 10 -7～ 10 -5mol·L-1浓度下可抑制化合物 48/ 80诱导的肥大细胞脱颗粒 ,并与浓度呈正相关。

AIM To study the anti inflammatory effects of benzoisoselenothiazolidonesulfonamide derivatives, compounds A and B. METHODS Boyden chamber was used to examine the chemotaxis of polymorphonuclear leukocyte. Myeloperoxidase activity was assayed by spectrophotometry. Dying method was used to study degranulation of mastocytes. RESULTS Compounds A and B were shown to inhibit the chemotaxis of polymorphonuclear leukocyte stimulated by fMLPP with IC 50 of 1 3×10 -8 mol·L -1 and 1 19×10 -10 mol·L -1 , respectively. In the model of mouse ear edema induced by croton oil, the rates of inhibition of myeloperoxidase activity after compounds A and B applied to the dorsal surface of mouse ear were 49% for compound A at the dose of 1 mg/mouse, 37% and 51% for compound B at the doses of 0 1 mg/mouse and 1 mg/mouse, respectively. Compounds A and B(10 -7 ～10 -5 mol·L -1 ) showed dose dependent inhibitory activity relationship with respect to the degranulation of mastocytes response to compound 48/80. CONCLUSION Benzoisoselenothiazolidonesulfonamide derivatives compound A and compound B showed obvious anti inflammatory effects.