葛根素衍生物抗炎作用及对环氧化酶活性的影响

张毅; 李恒华; 江兵; 张莉; 周志; 陈国庆; 蒋渝; 杨大坚

引用本文:	张毅,李恒华,江兵,张莉,周志,陈国庆,蒋渝,杨大坚.葛根素衍生物抗炎作用及对环氧化酶活性的影响[J].中国现代应用药学,2011,28(1):8-10.
	ZHANG Yi,LI Henghua,JIANG Bing,ZHANG Li,ZHOU Zhi,CHEN Guoqing,JIANG Yu,YANG Dajian.Affects on Cyclooxygenase Activities and Anti-inflammations Effects of Tetra-acetylated Puerarin[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(1):8-10.

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葛根素衍生物抗炎作用及对环氧化酶活性的影响
张毅,李恒华,江兵,张莉,周志,陈国庆,蒋渝,杨大坚
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

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52.9 μmol·L^-1，与吲哚美辛相比，无统计学差异(P>0.05)。

关键词: 四乙酰葛根素抗炎环氧化酶

DOI：

分类号:

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

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

ZHANG Yi^1,2, LI Henghua^1,3, JIANG Bing^1,3, ZHANG Li^1,3, ZHOU Zhi¹, CHEN Guoqing^1,4, JIANG Yu¹, YANG Dajian^5,4

1.Chongqing Academy of Chinese Materia Medica, Chongqing 400065，China;2.Chongqing Western China Open Laboratory of Chinese Materia Medica, Chongqing 400065，China;3.Chongqing Center of Durg safty Evaluation, Chongqing 400065, China;4.2.Chongqing Western China Open Laboratory of Chinese Materia Medica, Chongqing 400065, China;5.1.Chongqing Academy of Chinese Materia Medica, Chongqing 400065, China

Abstract:

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(P>0.05). And the 50% inhibitory concentration (IC_{50-1. CONCLUSION Tetra-acetylated puerarin has significant anti-inflammatory activity and selective inhibition effect on the COX-2, and it has a good application prospects.}

Key words: tetra-acetylated puerarin anti-inflammatory cyclooxygenase