常春藤糖苷衍生物的合成及体外抗胃癌细胞活性  

Synthesis and in Vitro Anti-gastric Cancer Cells Activities of Hederagenin Glucoside Derivatives

作　　者：洪开文 宋伦 陈懿[1] 郑重 董登祥 HONG Kai-wen;SONG Lun;CHEN Yi;ZHENG Zhong;DONG Deng-xiang(Applied Medical Department,Vocational and Technical College of Anshun,Guizhou Anshun 561000;College of Pharmacy,Guizhou College of Traditional Chinese Medicine,Guizhou Guiyang 550025,China)

机构地区：[1]安顺职业技术学院应用医药系,贵州安顺561000 [2]贵州中医药大学药学院,贵州贵阳550025

出　　处：《广州化工》2021年第15期32-36,92,共6页GuangZhou Chemical Industry

基　　金：黔合院士工作站[(2014)4013];黔中民族药资源开发创新团队项目[B202001];黔中民族药(苗药)资源开发与产业化协同创新中心基金资助项目。

摘　　要：以常春藤皂苷元为起始物,进行甲基化、乙酰化保护,通过糖化学结构修饰,合成了4种常春藤糖苷衍生物(7~10),其结构经^(1)H NMR,^(13)C NMR等表征。采用MTT法研究其体外抗胃癌细胞活性。4个新型目标化合物对上述胃癌细胞都有抑制作用,在药物浓度1×10^(-3) mmol/L时,化合物7对BGC803和SGC7901的抑制率分别为50.04%±4.61%、29.83%±3.5%,明显强于母药常春藤皂苷元对肿瘤细胞的抑制率17.08%±5.18%和10.58%±3.61%。该合成方法可以为前导药物研究提供参考。Using Hederagenin as starting material,through methylation and acetylation protection respectively,four novel hedragenin derivatives(7~10)were synthesized by performing modification.The structures were characterized by ^(1)H NMR and ^(13)C NMR.The in vitro anti-gastric cancer cellsactivities of the compounds were determined by MTT method.The synthesis of 4 new target compounds had an inhibitory effect on the above gastric cancer cells.At a drug concentration of 1×10^(-3) mmol/L,the inhibition rates of Compound 7 on BGC803 and SGC7901 were(50.04±4.61)%and(29.83±3.5)%respectively,Which was significantly stronger than the parent drug hederagenin(17.08±5.18)%and(10.58±3.61)%.This synthetic method can provide a reference for the study of lead drugs.

关 键 词：常春藤皂苷元 胃癌细胞 结构修饰 MTT法 

分 类 号：O624.3[理学—有机化学] O624.5[理学—化学]