N-苄基苦参醇-苯磺酰呋咱杂合物的合成及其抗肝癌活性  

Novel hybrids of(phenylsulfonyl)furoxan and N-benzyl matrinol as anti-hepatocellular carcinoma agents

作　　者：何黎琴[1] 杨琦[1] 吴亚先[1] 王效山[1] 

机构地区：[1]安徽中医药大学药学院,安徽合肥230031

出　　处：《药学学报》2015年第5期574-578,共5页Acta Pharmaceutica Sinica

基　　金：安徽省教育厅自然科学重点科研项目(KJ2013A168)

摘　　要：以苦参碱为原料,经水解、苄基化、还原等反应得到N-苄基苦参醇,通过不同类型的连接基团,将其与呋咱氮氧化物偶联得到14个N-苄基苦参醇-苯磺酰呋咱杂合物,其结构经IR、MS、1H NMR确证。采用MTT法测试了目标化合物对多种肝癌细胞的体外增殖抑制活性,结果显示,大多数化合物对不同肝癌细胞增殖均具有较强的抑制作用,且活性强于阳性对照药氟尿嘧啶(5-FU),其中化合物8a^8h、8j抑制肝癌细胞Hep G2的活性最强,IC50值达亚微摩尔浓度(0.12~0.93μmol·L-1)。N-Benzyl matrinol was obtained by hydrolysis, benzylation and reduction reaction from matrine. A series of hybrids （8a-8n） from （phenylsulfonyl）furoxan and N-benzyl matrinol were synthesized and biologically evaluated as anti-hepatocellular carcinoma agents. All target compounds were evaluated for anti- proliferative activity against human hepatocellular Bel-7402, SMMC-7721, Bel-7404, and HepG2 cells in vitro by MTT method. The results indicated that all of these compounds had potent anti-proliferative activity which were more potent than their parent compound and 5-FU, especially 8a-8h and 8j showed the strongest anti-HCC HepG2 cell activity with IC50 values of 0.12-0.93 μmol.L-1.

关 键 词：苦参碱 呋咱氮氧化物 抗肝癌活性 

分 类 号：R916[医药卫生—药学]