目的 研究芫花Daphne genkwa中的瑞香烷型二萜原酸酯類成分及其腫瘤細(xì)胞毒活性。方法 采用色譜分離技術(shù)進(jìn)行分離和純化，并根據(jù)譜學(xué)數(shù)據(jù)確定化合物的結(jié)構(gòu)，采用MTT法評價(jià)化合物對NCI-H1975肺癌細(xì)胞株和SK-BR-3乳腺癌細(xì)胞株的細(xì)胞毒活性。結(jié)果 從芫花中分離得到6個(gè)化合物，分別鑒定為異芫花酯甲（1）、芫花酯甲（2）、芫花酯?。?b>3）、芫花酯庚（4）、異芫花酯乙（5）、芫花酯乙（6）。結(jié)論 化合物1為新化合物?；衔?b>1～6對人乳腺癌SK-BR-3細(xì)胞株顯示了較強(qiáng)的細(xì)胞毒活性，IC₅₀值分別為217.1、172.6、170.2、809.4、83.7、61.6 nmol/L，而對肺癌NCI-H1975細(xì)胞株未顯示細(xì)胞毒活性。

Abstract: 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 cells 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.

國家重大新藥創(chuàng)新專項(xiàng)（2011ZX09401-009）