Comoë L, Jeannesson P, Trentesaux C, Desoize B, Jardillier J C
Leuk Res. 1987;11(5):445-51. doi: 10.1016/0145-2126(87)90076-2.
In view of new antitumor compounds which could exert their therapeutic effect through a combination of cell growth inhibition and cell maturation, we describe here the effects of a novel antileukemic alkaloid, fagaronine, on the growth and the induction of hemoglobin synthesis in the K 562 cell line. We found that fagaronine, after 3 days, reduces in a concentration dependent relationship the cell growth rate without lethality and this effect on the cell growth is irreversible. Reducing the cell growth rate by 50% (IC50 = 3 X 10(-6)M) is sufficient to induce an optimal amount of hemoglobin synthesis (75% benzidine-positive cells, 13-15 pg hemoglobin/cell) after 4 days of culture. Considering the variation of the total intracellular protein content during the response, it appears that fagaronine stimulated mainly hemoglobin synthesis, and to a lesser extent non-hemoglobin proteins. These results suggest that the novel antileukemic alkaloid, fagaronine, can be considered as a potent inducer of differentiated-associated properties in the human K 562 leukemic cells.
鉴于新的抗肿瘤化合物可通过抑制细胞生长和促进细胞成熟相结合来发挥治疗作用，我们在此描述一种新型抗白血病生物碱——白屈菜红碱，对K562细胞系生长及血红蛋白合成诱导的影响。我们发现，3天后白屈菜红碱以浓度依赖关系降低细胞生长速率且无致死性，这种对细胞生长的影响是不可逆的。在培养4天后，将细胞生长速率降低50%（IC50 = 3×10⁻⁶M）足以诱导出最佳量的血红蛋白合成（75%联苯胺阳性细胞，13 - 15 pg血红蛋白/细胞）。考虑到反应过程中细胞内总蛋白含量的变化，似乎白屈菜红碱主要刺激血红蛋白合成，对非血红蛋白蛋白的刺激程度较小。这些结果表明，新型抗白血病生物碱白屈菜红碱可被视为人类K562白血病细胞中分化相关特性的有效诱导剂。
