姚卫蓉^1，*， 汪泓^1，， 崔艳丽^2，

（  1、江南大学食品学院，无锡，214122；       2、浙江大学化学系，杭州，310027；  ）

摘要： [目的] 高效快速地合成岩藻聚糖硫酸酯，研究其对肿瘤细胞的体外抑制作用。[方法] 以全TMS保护的岩藻糖基碘作为糖给体，以三乙胺作为反应促进剂，合成了以单一的α-糖苷键结合的三糖。对新合成的岩藻聚糖进行硫酸化处理得到岩藻聚糖硫酸酯，采用 MTT法进行体外抗细胞增殖活性实验，检测合成的岩藻聚糖硫酸酯对肝癌细胞Huh7、胰腺癌细胞BxPC-3、胃癌细胞BGC-823的生长抑制作用。[结果] 通过改进已有的糖苷化反应方法，高效快速地合成了岩藻聚糖硫酸酯，得到的产物对肝癌细胞Huh7、胰腺癌细胞BxPC-3、胃癌细胞BGC-823均有抑制作用，其中对胃癌细胞BGC-823的抑制效果最好，当样品的处理浓度为0.1 mg/mL时，细胞的存活率已经低于20%，其它两种细胞的存活率也已低于30%。[结论] 新合成的岩藻聚糖硫酸酯具有较好的体外抗肿瘤作用。
关键词： 寡糖合成；岩藻聚糖硫酸酯；抗癌活性

Yao Weirong^1,*， Wang Hong^1,， Cui Yanli^2,

（  1、School of Food Science & Technology, Jiangnan University, Wuxi 214122, China；       2、Department of Chemistry, Zhejiang University, Hangzhou 310027, China；  ）

Abstract： [Objective] The paper was focused on the efficient, quick synthesis and antitumor effects of fucoidan. [Method] Per-O-trimethylsilylated fucosyl iodide as a sugar donor, triethylamine as a reaction promoter, we successfully synthesized trisaccharidein by a single α-glycosidic bond. The synthetic trisaccharidein were treated with sulfur trioxide triethylamine complex to get fucoidan, then the growth inhibition activity of hepatoma cell Huh7, pancreatic cancer cell BxPC-3, gastric carcinoma cell BGC-823 were carried out by MTT test in vitro. [Result] we provided a new method which improved the existing glycosylation reaction process to synthesize fucoidan. The product inhibited the growth of hepatoma cell Huh7, pancreatic cancer cell BxPC-3, gastric carcinoma cell BGC-823, among them, gastric carcinoma cell BGC-823 was the most sensitive, the survival rate was below 20% when product's concentration was 0.1 mg/mL, and the other two tumour cell were below 30%. [Conclusion] The synthetic fucoidan has excellent antitumor effect in vitro.
Keywords： Oligosaccharide synthesis; Fucoidan; Biological activity

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