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目的：选用黄花夹竹桃甙（ＴＳ）作为Ｎａ~＋－Ｋ~＋－ＡＴＰ酶的抑制剂，观察其对体外培养的Ｋ５６２细胞的杀伤作用，初步探讨其作用机制。方法：台盼蓝排染法测定ＴＳ对Ｋ５６２细胞的杀伤作用；８６Ｒｂ示踪法测定ＴＳ对Ｋ５６２细胞Ｎａ~＋－Ｋ~＋－ＡＴＰ酶活性的抑制作用；透射电镜观察ＴＳ对Ｋ５６２细胞形态学的改变。结果：低剂量的ＴＳ（０．００１～０．ｌμｇ／ｍｌ）在体外能够显著杀伤Ｋ５６２细胞，并有剂量依赖性。此种作用需经ＴＳ持续作用８ｈ以上才表现出来，并迅速增强。经０．１μｇ／ｍｌＴＳ处理１２ｈ的Ｋ５６２细胞，其生长受到显著的抑制。体外杀伤细胞浓度的ＴＳ作用１ｈ，对Ｋ５６２细胞的Ｎａ~＋Ｋ~＋－ＡＴＰ酶有明显的抑制作用。电镜观察发现，ＴＳ作用２４ｈ后，Ｋ５６２细胞出现非特异性的形态学改变，并发生溶解性坏死。结论：ＴＳ对Ｋ５６２细胞表现出很强的杀伤作用，其机制可能是抑制膜上Ｎａ~＋－Ｋ~＋－ＡＴＰ酶的活性，引起水盐代谢紊乱和营养物质摄取障碍。
OBJECTIVE: To investigate the cytotoxicity of oleander (TS) as an inhibitor of Na ~ + -K ~ + -ATPase in K562 cells in vitro and its possible mechanism. Methods: The killing effect of TS on K562 cells was determined by trypan blue exclusion. The inhibitory effect of TS on the activity of Na ~ + -K ~ + -ATPase of K562 cells was determined by 86Rb tracer method. The effect of TS on the morphology of K562 cells was observed by transmission electron microscopy Change. Results: Low doses of TS (0.001 ~ 0.lμg / ml) could kill K562 cells in vitro in a dose-dependent manner. This effect needs to be sustained by the role of TS more than 8h before manifested, and rapidly increased. K562 cells treated with 0.1μg / ml TS for 12h significantly inhibited the growth of K562 cells. In vitro K562 cells treated with TS for 1 h had a significant inhibitory effect on Na ~ + K ~ + -ATPase in K562 cells. Electron microscopy showed that after treated with TS for 24 h, nonspecific morphological changes occurred in K562 cells and lytic necrosis occurred. Conclusion: TS has a strong killing effect on K562 cells. The mechanism may be that it inhibits the activity of Na ~ + -K ~ + -ATPase on the membrane, causing disorder of water and salt metabolism and nutrient uptake.