白杨素衍生物的合成及其抗癌活性研究  

Synthesis and Anticancer Activities of Derivatives Chrysin Derivatives

作　　者：赵子淏 敖宝学 魏云[1] 刘运美[1] 谢志忠[1] 曹轩[1] 郑兴[1] 唐国涛[1] 

机构地区：[1]南华大学药物药理研究所湖南省药物蛋白质组学重点实验室,湖南衡阳421001

出　　处：《肿瘤药学》2015年第5期344-347,共4页Anti-Tumor Pharmacy

基　　金：国家自然科学基金项目(81273537)

摘　　要：目的合成一系列白杨素衍生物并研究其体外抗肿瘤活性。方法以白杨素为起始原料,通过醚化反应引入5-溴水杨酸酯,合成6个白杨素衍生物。然后采用MTT法检测白杨素衍生物对人胃癌MGC-803细胞、人肝癌Hep G2细胞的体外抗肿瘤活性。结果化合物3a、3b、4b抑制Hep G2的IC50值高于白杨素,化合物2a、2b、4a抑制Hep G2的IC50值低于白杨素,其中化合物2a、4a的IC50值低于阳性对照药5-氟尿嘧啶。化合物3a抑制MGC-803细胞的IC50值低于白杨素和阳性对照药5-氟尿嘧啶。结论合成的白杨素衍生物均经过1H NMR,MS确证。目标化合物2a对Hep G2细胞具有较强抑制作用,化合物3a对MGC-803细胞具有较好的抑制作用,抑制作用均较阳性对照药物5-氟尿嘧啶强。Objective To synthetize a variety of chrysin derivatives and identify their antitumor activity in vitro. Methods Chry-sin was applied as main raw materials and the 5-Bromosalicylic acid ester was added to the reaction system to synthesize chrysin derivatives in the etherification reaction. Then the MTT method was used to detect the anticancer activities of chrysin derivatives on human gastric cell line MGC-803 and human hepatocellular carcimoma cell HepG2. Results The 50%inhibiting concentrations of compounds2a,2band4aonHepG2cellswerelowerthanthatofchrysinin vitro.Meanwhile,the50%inhibitingconcentrationsof compounds 2a and 4a on HepG2 cells were lower than that of positive control component 5-FU. The 50%inhibiting concentration of compound 3a on MGC-803 cells were also lower than that of chaysin and 5-FU. Conclusions The chemical structures of these compounds were confirmed by 1H NMR, MS method. The antitumor activity of compound 2a against HepG2 cell and compound 3a against MGC-803 cell were better than 5-fluorouracil.

关 键 词：白杨素 衍生物 抗肿瘤 合成 

分 类 号：R969.1[医药卫生—药理学]