1. Academic Validation
  2. Selective antiproliferative activity of caffeic acid phenethyl ester analogues on highly liver-metastatic murine colon 26-L5 carcinoma cell line

Selective antiproliferative activity of caffeic acid phenethyl ester analogues on highly liver-metastatic murine colon 26-L5 carcinoma cell line

  • Bioorg Med Chem. 2002 Oct;10(10):3351-9. doi: 10.1016/s0968-0896(02)00138-4.
Takema Nagaoka 1 Arjun H Banskota Yasuhiro Tezuka Ikuo Saiki Shigetoshi Kadota
Affiliations

Affiliation

  • 1 Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630-Sugitani, Toyama, Japan.
Abstract

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.

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