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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 Yi1,2, LI Henghua1,3, JIANG Bing1,3, ZHANG Li1,3, ZHOU Zhi1, CHEN Guoqing1,4, JIANG Yu1, YANG Dajian5,4
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 (IC50-1. 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
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