告达庭葡萄糖苷的合成及抗肿瘤活性研究  

Synthesis of Caudatin Glucoside and Study on Its Antitumor Activity

作　　者：陶雪芬[1] 张如松[1] 

机构地区：[1]浙江中医药大学药学院药物化学教研室,杭州310053

出　　处：《中国现代应用药学》2011年第7期644-648,共5页Chinese Journal of Modern Applied Pharmacy

基　　金：白首乌C21甾体苷类化合物抗肿瘤活性的构效关系研究(Y200805461)

摘　　要：目的合成告达庭-β-D-葡萄糖苷并研究其抗肿瘤活性。方法以告达庭为原料在CdCO3催化下与溴活化的乙酰葡萄糖成苷,脱保护基得到目标产物,以MTT法考察其对肿瘤细胞的抑制作用。结果合成了告达庭-β-D-葡萄糖苷,结构经1H-NMR和13C-NMR鉴定。结论初步药理实验表明乙酰葡萄糖苷对大鼠胶质瘤细胞C6的抑制作用较强,而告达庭-β-D-葡萄糖苷对C6细胞的抑制作用与原料告达庭相当。OBJECTIVE To synthesize caudatin-β-D-glucoside and determine its antitumor activity. METHODS The target compound caudatin-β-D-glucoside was synthesized from caudatin by reaction with tetra-O-actyl-D-glucosyl bromide catalyzed by CdCO3 and then deprotection in CH3ONa/CH3OH. The antitumor activity was studied by MTT method. RESULTS Caudatin-fl-β-D-glucoside was synthesized and characterized by 1H-NMR and 13C-NMR spetra. CONCLUSION Preliminary pharmacological result shows that the inhibitory effect of caudatin-tetra-O-actyl-D-glucoside on rat glioma cell C6 is higher than that of caudatin while caudatin-fl-D-glucoside shows similar activity to caudatin.

关 键 词：告达庭 葡萄糖苷 合成 抗肿瘤活性 

分 类 号：R916.696[医药卫生—药学]