葛根素衍生物抗炎作用及对环氧化酶活性的影响  

Affects on Cyclooxygenase Activities and Anti-inflammations Effects of Tetra-acetylated Puerarin

作　　者：张毅[1,2] 李恒华[1,3] 江兵[1,3] 张莉[1,3] 周志[1] 陈国庆[1,2] 蒋渝[1] 杨大坚[1,2] 

机构地区：[1]重庆市中药研究院,重庆400065 [2]重庆市西部中药学开放实验室,重庆400065 [3]重庆市药物安全评价中心,重庆400065

出　　处：《中国现代应用药学》2011年第1期8-10,共3页Chinese Journal of Modern Applied Pharmacy

基　　金：重庆市科技攻关项目(2007AB5051);国家科技部重大新药创制(2009ZX09103-150)

摘　　要：目的探讨四乙酰葛根素(4Ac)的抗炎作用以及对环氧化酶(COX)的抑制作用。方法采用角叉菜胶诱发的大鼠急性足肿胀模型进行抗炎作用研究,并对环氧化酶的选择性进行了研究。结果 4Ac(40 mg.kg-1)对模型大鼠的足肿胀均有明显的抑制作用;4Ac对COX-2活性的半数抑制浓度(IC50)约为52.9μmol.L-1,与吲哚美辛相比,无统计学差异(P>0.05)。结论 4Ac有明显的抗炎作用,对COX-2具有选择性抑制作用,具有良好的应用前景。OBJECTIVE To investigate anti-inflammatory effects and cyclooxygenase-inhibitory effects of tetra-acetylated puerarin.METHODS The anti-inflammatory effect of tetra-acetylated puerarin was observed by using the rat inflammation model induced by Carrageenan,and the cyclooxygenase activity of tetra-acetylated puerarin was observed by radioimmunoassay（RIA）.RESULTS Tetra-acetylated puerarin（40 mg·kg-1） can significantly decrease the rat paw edema for the inhibition effects on foot edema.Compared with indomethacin,the effect on COX-2 of puerarin derivatives showed no significant difference（P0.05）.And the 50% inhibitory concentration（IC50） of it was about 52.9 μmol-L-1.CONCLUSION Tetra-acetylated puerarin has significant anti-inflammatory activity and selective inhibition effect on the COX-2,and it has a good application prospects.

关 键 词：四乙酰葛根素 抗炎 环氧化酶 

分 类 号：R285.5[医药卫生—中药学]