摘要
目的:检测角叉菜诱导的大鼠胸膜炎渗出细胞中COX2的存在并观察NS398对其活性的影响。方法:用SDSPAGE和Westernblot分析及PGHS1和PGHS2抗血清,识别并检测胸膜炎渗出细胞中的COX2。酶活性用TLC法测定。结果:致炎后5h,PGHS2出现,19h时消失,而PGHS1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PGHS1,未检测到PGHS2。新的非甾体抗炎药NS398,可明显抑制COX2活性(IC50=45μmol·L-1)。结论:COX2仅存在于角叉菜诱导的炎症部位;NS398可选择性抑制COX2,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