姜黄素类化合物体外抗氧化作用及其构-效关系研究  

In Vitro Antioxidant Activity and Structure-activity Relationships of Curcuminoids

作　　者：宋立敏[1] 张迪[2] 张杰[2] 许卉[2] 杨昕[1] SONG Li-min;ZHANG Di;ZHANG Jie;XU Hui;YANG Xin(School of Chemistry and Chemical Engineering,Yantai University,Yantai 264005,China;School of Pharmacy,Yantai University,Yantai 264005,China)

机构地区：[1]烟台大学化学化工学院,山东烟台264005 [2]烟台大学药学院,山东烟台264005

出　　处：《烟台大学学报（自然科学与工程版）》2018年第2期121-126,共6页Journal of Yantai University(Natural Science and Engineering Edition)

基　　金：国家十二五"重大新药创制"科技重大专项课题(2014ZX09301306-006);烟台大学2017年研究生科技创新基金项目(YDYB1725)

摘　　要：本文以抗坏血酸为阳性对照药物,通过系列体外抗氧化模型,系统评价姜黄素及其结构类似物单脱甲氧基姜黄素(DMC)、双脱甲氧基姜黄素(BDMC)、二甲氧基姜黄素(BIMC)和双环戊二酮衍生物(CURC)的自由基清除及还原能力,在此基础上探索分析这类化合物抗氧化作用的构-效关系.结果表明,实验考察的姜黄素类似物具有不同程度的还原能力,并能剂量依赖地清除DPPH·、O_2^-·、·OH、ROO·和ABTS·^+自由基,酚羟基、苯环上的甲氧基以及庚二烯-3,5二酮长链共轭结构共同影响这类成分的抗氧化活性,且对不同抗氧化模型的影响存在差异.In the present study,several in vitro experiments are carried out to investigate antioxidant activities of curcumin and its diverse structural analogues,including demethoxycurcumin(DMC),bisdemethoxycurcumin(BDMC),dimethoxycurcumin(BIMC),and its dicyclopentanedione derivative(CURC).Vitamine C(Vc)is used as a positive control,thus the scavenging ability on free radicals of DPPH·,O 2-·,·OH,ROO·,and ABTS·+and ferric-reducing antioxidant power(FRAP)are evaluated by spectrophotometric assays.The potency is quantitatively investigated according to half effective concentration(EC 50)or the relative ratio to Vc calculated from dose-response curve.Moreover,the relationship between antioxidant activities and chemical structure of these curcuminoids is explored.The results indicate that all the test curcuminoids show obvious dose-dependent antioxidant activity,and the potency varies with both assay models and chemical structure of the test compounds,which results from the combined effects of the phenolic hydroxyl and methoxyl groups and the conjugate chain structure of heptadiene-3,5-dione.

关 键 词：姜黄素 化学结构类似物 抗氧化活性 自由基清除 还原能力 构-效关系 

分 类 号：R917[医药卫生—药物分析学]