烟台大学学报（自然科学与工程版）2017，Vol.30Issue(2)：111-116,6.DOI:10.13951/j.cnki.37-1213/n.2017.02.006
6-取代青藤碱衍生物的合成及体外抗炎活性研究
Synthesis and in vitro Anti-inflammatory Activity of6-Substituted Sinomenine Derivatives
摘要
Abstract
In order to search for novel compounds with excellent and safe anti-inflammation activity, ten novel 6-substituted sinomenine derivatives C1-C10 have been designed and synthesized via reduction of carbonyl, chiral separation and esterification of (S)-configuration isomer from sinomenine.The structures of target compounds are confirmed by 1H NMR and MS techniques.The biological evaluation results show that C1-C10 exhibit good inhibitory effect on NF-κB transfection in vitro induced by lipopolysaccharide, which are higher than sinomenine.It is indicated that the introduction of lipophilic substituted cinnamic acid can enhance the anti-inflammatory activity of sinomenine via regulating lipid water distribution coefficient.关键词
青藤碱/合成/抗炎活性/NF-κBKey words
sinomenine/synthesis/anti-inflammatory/NF-κB分类
医药卫生引用本文复制引用
李新利,赵风兰,管忠俊,蔡艺,柴晓云,吴秋业,孟庆国..6-取代青藤碱衍生物的合成及体外抗炎活性研究[J].烟台大学学报（自然科学与工程版）,2017,30(2):111-116,6.基金项目
国家自然科学基金资助项目(81473104). （81473104）
