Picariello Lucia, Fiorelli Gianna, Martineti Valentina, Tognarini Isabella, Pampaloni Barbara, Tonelli Francesco, Brandi Maria Luisa
Department of Clinical Physiopathology, University of Florence, Florence, Italy.
Anticancer Res. 2003 May-Jun;23(3B):2419-24.
The purpose of this study was to compare the "in vitro" effects of the selective estrogen receptor modulators, tamoxifen and raloxifene, on two human colon cancer cell lines.
Serial concentrations (0.1, 1, 5 and 10 microM) of tamoxifen and raloxifene were used and evaluated for cell proliferation, viability and apoptosis in HCT8 and HCT116 cells.
Micromolar doses of raloxifene significantly reduced HCT116 and HCT8 cell proliferation. Tamoxifen (5 microM) strongly reduced HCT8 cell growth with minor effects on HCT116 cells. Raloxifene (10 microM) was lethal on both cell lines, while 10 microM tamoxifen caused lethality only in HCT8 cells. Five microM raloxifene reduced cell viability in HCT8 and HCT116 cells, while 5 microM tamoxifen halved only HCT8 cell viability. Raloxifene and tamoxifen did not induce apoptosis in the two cell lines.
Tamoxifen, and even more raloxifene, were effective in reducing HCT8 and HCT116 cell proliferation and viability, suggesting their potential application in the prevention and therapy of colorectal cancer.
本研究的目的是比较选择性雌激素受体调节剂他莫昔芬和雷洛昔芬对两种人结肠癌细胞系的“体外”作用。
使用他莫昔芬和雷洛昔芬的系列浓度（0.1、1、5和10微摩尔），并评估其对HCT8和HCT116细胞增殖、活力和凋亡的影响。
微摩尔剂量的雷洛昔芬显著降低HCT116和HCT8细胞的增殖。他莫昔芬（5微摩尔）强烈降低HCT8细胞的生长，对HCT116细胞的影响较小。雷洛昔芬（10微摩尔）对两种细胞系均具有致死性，而10微摩尔他莫昔芬仅对HCT8细胞具有致死性。5微摩尔雷洛昔芬降低HCT8和HCT116细胞的活力，而5微摩尔他莫昔芬仅使HCT8细胞的活力减半。雷洛昔芬和他莫昔芬未诱导两种细胞系发生凋亡。
他莫昔芬，尤其是雷洛昔芬，在降低HCT8和HCT116细胞的增殖和活力方面有效，提示它们在结直肠癌预防和治疗中的潜在应用价值。
