Kato T, Takamoto S, Mizutani M, Hato M, Ota K
Gan To Kagaku Ryoho. 1984 Nov;11(11):2393-9.
The antitumor activities and the mechanisms of action of harringtonine and homoharringtonine, alkaloids isolated from cephalotaxus hainanensis Li, were compared to those of vincristine. The results obtained were as follows: Harringtonine and homoharringtonine Significantly inhibited the growth of L1210 cells in culture. The IC50 values were similar to that of vincristine. Harringtonine and homoharringtonine had little effects on changes in the DNA histograms of FL cells at any concentrations, which suggesting that these drugs prolong the duration of each phase of the cell cycle evenly. Harringtonine and homoharringtonine had only a minor effect in arresting P388 cells in mitosis. Harringtonine significantly inhibited the DNA synthesis of P388 leukemia cells in culture, while vincristine weakly inhibited RNA and DNA synthesis. The successive treatment with harringtonine and homoharringtonine were as effective as the successive treatment with vincristine against P388 and L1210 leukemia, while both drugs were ineffective against Lewis lung carcinoma.
对从海南粗榧中分离得到的生物碱三尖杉酯碱和高三尖杉酯碱的抗肿瘤活性及其作用机制与长春新碱进行了比较。得到的结果如下:三尖杉酯碱和高三尖杉酯碱显著抑制培养的L1210细胞的生长。其半数抑制浓度(IC50)值与长春新碱相似。三尖杉酯碱和高三尖杉酯碱在任何浓度下对FL细胞的DNA直方图变化影响很小,这表明这些药物均匀地延长了细胞周期各阶段的持续时间。三尖杉酯碱和高三尖杉酯碱在使P388细胞停滞于有丝分裂方面作用较小。三尖杉酯碱显著抑制培养的P388白血病细胞的DNA合成,而长春新碱对RNA和DNA合成的抑制作用较弱。三尖杉酯碱和高三尖杉酯碱连续给药对P388和L1210白血病的疗效与长春新碱连续给药相同,而两种药物对Lewis肺癌均无效。