芫花中瑞香烷型二萜原酸酯类化合物及其肿瘤细胞毒活性  

Daphnane diterpene esters from flower buds of Daphne genkwa and their cytotoxic effects on cancer cells

作　　者：邵泽艳[1,2] 商倩[1] 赵娜夏[1] 张士俊[1] 夏广萍[1] 白秀秀[1,2] 董虹玲[1,2] 韩英梅[1] 

机构地区：[1]天津药物研究院天津市新药设计与发现重点实验室,天津300193 [2]天津中医药大学,天津300193

出　　处：《中草药》2013年第2期128-132,共5页Chinese Traditional and Herbal Drugs

基　　金：国家重大新药创新专项(2011ZX09401-009)

摘　　要：目的研究芫花Daphne genkwa中的瑞香烷型二萜原酸酯类成分及其肿瘤细胞毒活性。方法采用色谱分离技术进行分离和纯化,并根据谱学数据确定化合物的结构,采用MTT法评价化合物对NCI-H1975肺癌细胞株和SK-BR-3乳腺癌细胞株的细胞毒活性。结果从芫花中分离得到6个化合物,分别鉴定为异芫花酯甲(1)、芫花酯甲(2)、芫花酯丁(3)、芫花酯庚(4)、异芫花酯乙(5)、芫花酯乙(6)。结论化合物1为新化合物。化合物1～6对人乳腺癌SK-BR-3细胞株显示了较强的细胞毒活性,IC50值分别为217.1、172.6、170.2、809.4、83.7、61.6 nmol/L,而对肺癌NCI-H1975细胞株未显示细胞毒活性。Objective To study daphnane diterpene esters from the flower buds of Daphne genkwa and to evaluate their cytotoxicity against tumor cells. Methods The compounds were isolated and purified by means of chromatographic techniques and their structures were identified on the basis of spectral features. Cytotoxic activity against NCI-H1975 lung cancer cells and SK-BR-3 breast cancer cells were assessed for all the compounds by MTT method. Results Six compounds were isolated and identified as isoyuanhuacin （1）, yuanhuacin （2）, yuanhuatin （3）, yuanhuagin （4）, isoyuanhuadin （5）, and yuanhuadin （6）. Conclusion Compound 1 is a new compound. Compounds 1--6 exhibit the strong cytotoxicity on SK-BR-3 human breast cancer ceils with the IC50 values of 217.1, 172.6, 170.2, 809.4, 83.7, and 61.6 nmol/L, respectively, but show no effect on NCI-H1975 human lung cancer cells.

关 键 词：芫花 二萜原酸酯类 细胞毒活性 异芫花酯甲 芫花酯丁 

分 类 号：R284.1[医药卫生—中药学]