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目的探讨新型氮芥衍生物N-[4-(二氯乙基)丁胺]-1,8-萘酰亚胺(XHH)对K562细胞的抗肿瘤作用及其机制。方法采用MTT法检测XHH对K562细胞增殖的影响;用Annexin V-FITC/Hoechst33342、PI/Hoechst33342和Rh123/Hoechst33342双染法高内涵观察细胞的形态学变化、凋亡率及线粒体膜电位;用分光光度法检测caspase-3、caspase-9的活性。结果在一定浓度范围内,XHH能抑制K562细胞的增殖且抗肿瘤活性优于美法仑,呈剂量和时间依赖性地诱导细胞凋亡、降低线粒体膜电位、活化caspase-3和caspase-9。结论 XHH具有较好的抗肿瘤活性,可通过线粒体/caspase-9/caspase-3途径诱导K562细胞凋亡。
Objective To investigate the antitumor effect of a novel nitrogen mustard derivative N- [4- (dichloroethyl) butylamine] -1,8-naphthalimide (XHH) on K562 cells and its mechanism. Methods MTT assay was used to detect the effect of XHH on the proliferation of K562 cells. Morphological changes, apoptosis rate and mitochondrial membrane potential were observed by Annexin V-FITC / Hoechst33342, PI / Hoechst33342 and Rh123 / Hoechst33342 double staining. The activity of caspase-3 and caspase-9 were detected by spectrophotometry. Results In a certain concentration range, XHH could inhibit the proliferation of K562 cells and the anti-tumor activity was better than that of melphalan. XHH induced apoptosis in dose and time-dependent manner, decreased mitochondrial membrane potential and activated caspase-3 and caspase-9. Conclusion XHH has good anti-tumor activity and can induce apoptosis of K562 cells through mitochondrial / caspase-9 / caspase-3 pathway.