Department of Natural Products Chemistry, Shenyang Pharmaceutical University, Shenyang 110016, People's Republic of China.
Bioorg Med Chem Lett. 2013 May 1;23(9):2500-4. doi: 10.1016/j.bmcl.2013.03.025. Epub 2013 Mar 15.
Four new daphnane-type diterpenes, genkwadanes A-D (1-4), together with 19 known ones, were isolated from ethanol extract of the flower buds of Daphne genkwa. Their structures were determined on the basis of extensive spectroscopic data. Among them, daphnane-type diterpene with a 1,10-double bond (1) was isolated from this plant for the first time. The cytotoxicity of all compounds 1-23 against the 10 selected human cancer cell lines was assayed. A number of compounds exhibited significant activities against the 10 cancer cell lines (IC50<9.56 μM). and most interestingly, all the compounds revealed preferred cytotoxicities on the HT-1080 cell line and displayed much stronger inhibitory activities (IC50<29.94 μM) compared with positive control 5-fluorouracil (IC50=35.62 μM), particularly, compounds 9-11, 13, 16 and 19 exhibited the strongest cytotoxicity activities against the HT-1080 cell line (IC50<0.1 μM).
从芫花花蕾的乙醇提取物中分离得到了 4 个新的瑞香烷型二萜，分别命名为 genkwadanes A-D（1-4），加上之前已知的 19 个化合物，共分离得到 23 个化合物。根据广泛的光谱数据分析确定了它们的结构。其中，化合物 1 是一种具有 1,10-双键的瑞香烷型二萜，首次从该植物中分离得到。所有化合物 1-23 对 10 种选定的人类癌细胞系的细胞毒性进行了检测。许多化合物对 10 种癌细胞系表现出显著的活性（IC50<9.56 μM）。有趣的是，与阳性对照 5-氟尿嘧啶（IC50=35.62 μM）相比，所有化合物在 HT-1080 细胞系上都表现出更好的细胞毒性，且显示出更强的抑制活性（IC50<29.94 μM），特别是化合物 9-11、13、16 和 19 对 HT-1080 细胞系的细胞毒性最强（IC50<0.1 μM）。
