Nagaoka Takema, Banskota Arjun H, Tezuka Yasuhiro, Saiki Ikuo, Kadota Shigetoshi
Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630-Sugitani, Toyama, Japan.
Bioorg Med Chem. 2002 Oct;10(10):3351-9. doi: 10.1016/s0968-0896(02)00138-4.
Caffeic acid phenethyl ester (CAPE, 2) and its twenty analogues (1, 3-21) were prepared. These esters were tested by MTT assay on growth of murine colon 26-L5 carcinoma, murine B16-BL6 malonoma, murine Lewis lung carcinoma, human HT-1080 fibrosarcoma, human lung A549 adenocarcinoma, and human cervix HeLa adenocarcinoma cell lines. It was found that CAPE analogues possessed selective antiproliferative activity toward highly liver-metastatic murine colon 26-L5 carcinoma cell line. Among them, 4-phenylbutyl caffeate (4), (Z)-8-phenyl-7-octenyl (10a) and (E)-8-phenyl-7-octenyl (10b) caffeate showed the most potent antiproliferative activity (EC50 value, 0.02 microM). In addition, CAPE (2) induced DNA fragmentation at concentrations of 1 to 10 microg/mL towards murine colon 26-L5 carcinoma cells.
制备了咖啡酸苯乙酯（CAPE，2）及其二十种类似物（1, 3 - 21）。通过MTT法对这些酯类化合物针对小鼠结肠26 - L5癌、小鼠B16 - BL6黑色素瘤、小鼠Lewis肺癌、人HT - 1080纤维肉瘤、人肺A549腺癌和人宫颈HeLa腺癌细胞系的生长进行了测试。发现CAPE类似物对高肝转移性小鼠结肠26 - L5癌细胞系具有选择性抗增殖活性。其中，4 - 苯基丁基咖啡酸酯（4）、（Z）- 8 - 苯基 - 7 - 辛烯基（10a）和（E）- 8 - 苯基 - 7 - 辛烯基（10b）咖啡酸酯表现出最强的抗增殖活性（EC50值，0.02 microM）。此外，CAPE（2）在浓度为1至10微克/毫升时可诱导小鼠结肠26 - L5癌细胞发生DNA片段化。
