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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)。
Using matrine as raw material, N, N-benzyl-tocotrienol was obtained through the reaction of hydrolysis, benzylation and reduction. Coupled with furazan oxynitride through different types of linking groups, 14 N-benzyl The structure of the base of ginseng alcohol-phenylsulfonylfurzanone was confirmed by IR, MS and 1H NMR. The inhibitory activity of the target compound on the proliferation of various liver cancer cells was tested by MTT assay. The results showed that most of the compounds had a strong inhibitory effect on the proliferation of different liver cancer cells, and their activity was stronger than that of the positive control fluorouracil (5-FU) Among them, compounds 8a ~ 8h, 8j had the strongest inhibitory effect on Hep G2 cells with IC50 values of 0.12 ~ 0.93μmol·L-1.