Lee Ya-Ting, Don Ming-Jaw, Hung Pei-Shih, Shen Yuh-Chiang, Lo Yin-Shen, Chang Kuo-Wei, Chen Chieh-Fu, Ho Li-Kang
Department of Pharmacology, School of Medicine, National Yang-Ming University, 155, Sec. 2, Li-Nung St. Peitou, Taipei 112, Taiwan, ROC.
Cancer Lett. 2005 Jun 1;223(1):19-25. doi: 10.1016/j.canlet.2004.09.048. Epub 2004 Nov 5.
Many phenolic acid phenethyl esters possess diverse biological effects including anti-cancer activity. A series of 14 derivatives were synthesized for the evaluation of their cytotoxic effect on oral cancer cells. These derivatives were tested by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) colorimetric and trypan blue dye exclusion assay on the growth of oral squamous cell carcinoma (SAS), oral epidermoid carcinoma-Meng 1 (OEC-M1), and normal human oral fibroblast (NHOF) cells, respectively. Caffeic acid phenethyl esters, 3a (CAPE), and 3b, 3c, and 3d showed cytotoxic effects on the SAS and OEC-M1 cell lines, but not the NHOF cell line at a 5-100 microM dose range. Flow cytometric analysis showed that 3c caused OEC-M1 cell arrest at G2/M phase. Such differential effects on representative cancer and normal cells suggested these compounds might be useful in oral cancer chemotherapy.
许多酚酸苯乙酯具有多种生物活性，包括抗癌活性。合成了一系列14种衍生物，以评估它们对口腔癌细胞的细胞毒性作用。分别通过3-(4,5-二甲基噻唑-2-基)-2,5-二苯基四氮唑溴盐（MTT）比色法和台盼蓝染料排斥试验，对这些衍生物在口腔鳞状细胞癌（SAS）、口腔表皮样癌-Meng 1（OEC-M1）和正常人口腔成纤维细胞（NHOF）细胞生长上进行了测试。咖啡酸苯乙酯3a（CAPE）以及3b、3c和3d在5-100微摩尔剂量范围内，对SAS和OEC-M1细胞系显示出细胞毒性作用，但对NHOF细胞系无此作用。流式细胞术分析表明，3c导致OEC-M1细胞在G2/M期停滞。这些化合物对代表性癌细胞和正常细胞的不同作用表明，它们可能在口腔癌化疗中有用。
