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引用本文:陶雪芬,张如松.告达庭葡萄糖苷的合成及抗肿瘤活性研究[J].中国现代应用药学,2011,28(7):644-648.
TAO Xuefen,ZHANG Rusong.Synthesis of Caudatin Glucoside and Study on Its Antitumor Activity[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(7):644-648.
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告达庭葡萄糖苷的合成及抗肿瘤活性研究
陶雪芬, 张如松
浙江中医药大学药学院药物化学教研室,杭州 310053
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。
关键词:  告达庭  葡萄糖苷  合成  抗肿瘤活性
DOI:
分类号:
基金项目:白首乌C21甾体苷类化合物抗肿瘤活性的构效关系研究(Y200805461)
Synthesis of Caudatin Glucoside and Study on Its Antitumor Activity
TAO Xuefen, ZHANG Rusong
Department of Medicinal Chemistry, College of Pharmaceutical Science, Zhejiang Chinese Medicinal University, Hangzhou 310053, China
Abstract:
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-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-β-D-glucoside shows similar activity to caudatin.
Key words:  caudatin  glucoside  synthesis  antitumor activity
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