甘油糖醚Myrmekiosides A类似物的合成及初步活性研究  

The synthesis and anti-tumor activity of Myrmekiosides A analogs

作　　者：高翠翠 张君[1] 马海珍[1] 叶鑫 李春霞[1,2] GAO Cui-cui;ZHANG Jun;MA Hai-zhen;YE Xin;LI Chun-xia(Key Laboratory of Marine Drugs,Ministry of Education, Shandong Provincial Key Laboratory ofGlycoscience and Glycotechnology, School of Medicine and Pharmacy,Ocean University of China,Qingdao 266003,China;Laboratory for Marine Drugs and Bioproducts of QingdaoPilot National Laboratory for Marine Science and Technology, Qingdao 266237,China)

机构地区：[1]中国海洋大学海洋药物教育部重点实验室,山东省糖科学与糖工程重点实验室,医药学院,山东青岛266003 [2]青岛海洋科学与技术试点国家实验室海洋药物与生物制品功能试验室,山东青岛266237

出　　处：《中国海洋药物》2019年第4期1-10,共10页Chinese Journal of Marine Drugs

基　　金：国家重大新药创制专项(2018ZX09305004);山东省重大科技创新工程专项(2018SDKJ0404-2);国家自然科学基金-山东省联合基金项目(U1606403-1);山东省自然科学基金项目(ZR2017MH096)资助

摘　　要：通过改变天然产物甘油糖醚Myrmekiosides A的甘油骨架上连接的糖基类型和长链烷基,高效合成了5个类似物(Myrmekioside A-1~5)。5个类似物对非小细胞肺癌株A549抑制活性测试发现,甘油糖醚结构中的糖单元类型和烷基长链对抗肿瘤活性均有影响,其中Myrmekioside A-3具有最好的抑制活性,抑制率为71%。Five analogs(Myrmekioside A-1~5)were designed by changing the type of glycosyl and the long-chain alkyl groups attaching to the glycerol skeleton of natural glycolipid Myrmekiosides A,and the target compounds were obtained with high yields.The anti-tumor activities of five analogs against non-small cell lung cancer cell line A549 were evaluated.The results showed that both the type of glycosyl group and the alkyl chain had an effect on the tumor activity.Myrmekioside A-3 demonstrated the best cytotoxic activity against A549 with 71%inhibition.

关 键 词：甘油糖醚Myrmekiosides A 类似物 合成 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]