Tominaga T, Yoshida Y, Matsumoto A, Hayashi K, Kosaki G
Department of Surgery, Tokyo Metropolitan Komagome Hospital, Japan.
Anticancer Res. 1993 May-Jun;13(3):661-5.
The growth inhibitory activity and influences on cell-cycle progression of tamoxifen (TAM) and its derivatives [toremifene(NK), droloxifene (FK) and TAT-59 (TAT) against MCF-7, cells, an estrogen respondent human breast cancer cell line were investigated. TAM and its derivatives exhibited a dose-dependent growth inhibitory activity against MCF-7 cells in the order of TAT > FK > TAM > NK at 48 and 120 hours in vitro. 10(-6) M TAT reduced growth of MCF-7 to 25% of that of control after 120 hours incubation in the presence of 10(-8) M estradiol; however, in the case of TAM the growth of MCF-7 was 73%. FACS analysis showed that 82.7% of the cells were accumulated at G0/1 phase after 120 hours incubation with TAT and its accumulative activity was higher than that of TAM. Moreover, when TAT was used in combination with 5-FU, the accumulative effect was significantly increased. Thus it is suggested that TAT or TAT in combination with 5-FU may be a useful adjuvant treatment against breast cancer.
研究了他莫昔芬（TAM）及其衍生物[托瑞米芬（NK）、屈洛昔芬（FK）和TAT-59（TAT）]对雌激素反应性人乳腺癌细胞系MCF-7细胞的生长抑制活性及其对细胞周期进程的影响。在体外48小时和120小时时，TAM及其衍生物对MCF-7细胞呈现出剂量依赖性生长抑制活性，其活性顺序为TAT>FK>TAM>NK。在10^(-8) M雌二醇存在的情况下，10^(-6) M TAT孵育120小时后，MCF-7细胞的生长降至对照组的25%；然而，对于TAM，MCF-7细胞的生长为73%。流式细胞术分析显示，与TAT孵育120小时后，82.7%的细胞积聚在G0/1期，其积聚活性高于TAM。此外，当TAT与5-氟尿嘧啶联合使用时，积聚效应显著增加。因此，提示TAT或TAT与5-氟尿嘧啶联合使用可能是一种有效的乳腺癌辅助治疗方法。
