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角叉菜诱导大鼠胸膜炎中环氧酶-2的生成及NS-398对其选择性抑制作用 被引量:2

INDUCTION OF CYCLOOXYGENASE 2 IN RAT CARRAGEENIN INDUCED PLEURISY AND ITS SELECTIVE INHIBITION BY NS 398
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摘要 目的:检测角叉菜诱导的大鼠胸膜炎渗出细胞中COX2的存在并观察NS398对其活性的影响。方法:用SDSPAGE和Westernblot分析及PGHS1和PGHS2抗血清,识别并检测胸膜炎渗出细胞中的COX2。酶活性用TLC法测定。结果:致炎后5h,PGHS2出现,19h时消失,而PGHS1在注射角叉菜前后均出现。此外,在胸膜炎大鼠和正常大鼠的肺、胃、肾微粒体中,只检测到PGHS1,未检测到PGHS2。新的非甾体抗炎药NS398,可明显抑制COX2活性(IC50=45μmol·L-1)。结论:COX2仅存在于角叉菜诱导的炎症部位;NS398可选择性抑制COX2,并呈剂量依赖性。 AIM: To detect cyclooxygenase 2(COX 2)/prostaglandin H synthase 2(PGHS 2) in cells of pleural exudate and investigate the effect of NS 398 on its activity. METHODS: COX 2 was tested by SDS PAGE and Western blot in cells of the pleural exudate induced in rats by intrapleural injection of 0 2 ml of 2% carrageenin. TLC was used to analyze the activity of COX 2. RESULTS: The examination using PGHS 1 or PGHS 2 antiserum showed that PGHS 2 appeared at the 5th hour after carrageenin injection, and vanished at the 19th hour. While, PGHS 1 appeared in cells before and after carrageenin injection. Furthermore, only PGHS 1, but not PGHS 2, was detected in the microsomal fraction of the lung, stomach and kidney of pleurisy affected and normal control rats. NS 398,a novel nonsteroidal anti inflammatory agent, suppressed the activity of COX 2 with IC 50 =4 5 μmol·L -1 . CONCLUSION: COX 2 is only present in inflammatory site induced by carrageenin. NS 398 may selectively inhibit COX 2 activity in a dose dependent manner.
出处 《药学学报》 CAS CSCD 北大核心 1999年第3期181-184,共4页 Acta Pharmaceutica Sinica
关键词 环氧酶-2 胸膜炎 NS-398 角叉菜 大鼠 cyclooxygenase 2(prostaglandin H synthase 2) pleurisy Western blot N (2 cyclohexyloxy 4 nitrophenyl) methane sulfonamide
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