白藜芦醇衍生物的制备及其抗炎活性研究  

Synthesis and anti-inflammatory activity of resveratrol derivatives

作　　者：匡洪涛 温授惠 曹健康 徐梦彤 安琪 牟晓凤 赵烽[1] KUANG Hongtao;WEN Shouhui;CAO Jiankang;XU Mengtong;AN Qi;MOU Xiaofeng;ZHAO Feng(Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,Key Laboratory of Ministry of Educationof Molecular Pharmacology and Drug Evaluation,Yantai University,Yantai 264005,Shandong,P.R.China)

机构地区：[1]烟台大学新型制剂与生物技术药物研究山东省高校协同创新中心,分子药理和药物评价教育部重点实验室,山东烟台264005

出　　处：《滨州医学院学报》2020年第2期136-139,共4页Journal of Binzhou Medical University

基　　金：山东省大学生创新创业训练计划项目(S201911066006)。

摘　　要：目的对天然白藜芦醇进行衍生物制备及抗炎活性研究,以期获得抗炎活性更好的药物先导化合物。方法以白藜芦醇为研究对象,进行结构修饰与改造,设计合成6个白藜芦醇衍生物,包括1个甲基化产物、4个酯化产物和1个酰胺类衍生物。所有化合物结构都通过1H NMR、ESIMS鉴定。采用Griess法检测白藜芦醇衍生物对LPS诱导巨噬细胞释放炎症介质NO的抑制活性。结果白藜芦醇的酰胺类衍生物显示出较好的NO抑制活性且未显示细胞毒性,具有一定的应用价值。结论对白藜芦醇衍生物潜在抗炎活性的研究可以为寻找新型抗炎先导化合物提供物质基础。Objective To obtain better drug lead compounds with anti-inflammatory activity from derivatives of natural product resveratrol.Methods Resveratrol was used as a lead compound for structural modification and 6 derivatives were designed and synthesized,including one methylation product,four esterification products and one amide analogue.The structures of all derivatives were characterized by 1H-NMR,and MS spectra.The inhibition on NO production of resveratrol derivatives in LPS-stimulated RAW 264.7 cells were tested by Griess method.Results The results indicated that amide derivative 6 possessed some application potential with good anti-inflammatory activities and no cytotoxity.Conclusion Research on the potential anti-inflammatory activity of resveratrol derivatives can provide a material basis for the research of new anti-inflammatory drug lead compounds.

关 键 词：白藜芦醇 结构修饰 酰化反应 酰胺类衍生物 抗炎活性 

分 类 号：R914.5[医药卫生—药物化学]