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9-O-肉桂酸小檗红碱酯的合成及抗炎活性

发表时间:2017-06-15  浏览量:147  下载量:10
全部作者: 贺芬,刘艳飞,张姗姗,王晓红,李宜褰,谢雄,刘珍宝
作者单位: 中南大学化学化工学院;中南大学湘雅药学院
摘 要: 以小檗碱和肉桂酸为原料,通过去甲基化、乙酰化、成酯反应合成小檗碱衍生物9-O-肉桂酸小檗红碱酯,采用二甲苯致小鼠耳肿胀模型,观察致炎后9-O-肉桂酸小檗红碱酯对小鼠耳肿胀程度及血清中炎症因子白细胞介素-6(interleukin-6,IL-6)、肿瘤坏死因子-α(tumor necrosis factor-α,TNF-α)的影响,考察其抗炎活性。通过傅里叶变换红外光谱(Fourier transform infrared spectroscopy,FTIR)、核磁共振氢谱(1H nuclear magnetic resonance,1H NMR)和碳谱(13C NMR)及质谱确认了产物化学结构。小鼠耳肿胀结果显示,合成的目标产物9-O-肉桂酸小檗红碱酯能降低耳肿胀及抑制IL-6、TNF-α水平的升高,且呈剂量依赖性,说明其具有抗炎活性。
关 键 词: 药物化学;小檗碱;9-O-肉桂酸小檗红碱酯;药物合成;抗炎活性
Title: Synthesis and anti-inflammatory activity of 9-O-cinnamicberberine
Author: HE Fen, LIU Yanfei, ZHANG Shanshan, WANG Xiaohong, LI Yiqian, XIE Xiong, LIU Zhenbao
Organization: School of Chemistry and Chemical Engineering, Central South University; Xiangya School of Pharmaceutical Sciences, Central South University
Abstract: 9-O-cinnamicberberine was synthesized from berberine and cinnamic acid via demethylation, acetylation and esterification, and its anti-inflammatory activity was evaluated using the xylene-induced ear swelling mice model. The ear swelling extent and the related inflammatory factors such as interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) in serum were observed. The structure of the target compound was confirmed by Fourier transform infrared spectroscopy (FTIR), 1H nuclear magnetic resonance (1H NMR), 13C NMR and mass spectrum. The target compound has lowered the ear swelling extent and inhibited the serum levers of IL-6 and TNF-α in a dose dependent manner, which indicating this compound has anti-inflammatory activity.
Key words: medicinal chemistry; berberine; 9-O-cinnamicberberine; pharmaceutical synthesis; anti-inflammatory activity
发表期数: 2017年6月第11期
引用格式: 贺芬,刘艳飞,张姗姗,等. 9-O-肉桂酸小檗红碱酯的合成及抗炎活性[J]. 中国科技论文在线精品论文,2017,10(11):1237-1243.
 
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