【摘要】 为寻找能特异性诱导肿瘤细胞凋亡的小分子诱导剂,研究了二异丙氧基磷酰化亮赖叉肽甲酯((DIPP-L-Leu)2-L-Lys-OCH3)对K562细胞的促凋亡作用。合成了(DIPP-L-Leu)2-L-Lys-OCH3,通过质谱、磷谱、氢谱和碳谱进行结构鉴定。通过MTT比色实验得到:该样品对K562细胞的半抑制浓度为22.66μmol.L-1。AO荧光染色、DNA琼脂糖凝胶电泳和Annexin -FITC/PI双染实验表明:该样品对K562细胞的增殖抑制作用是通过诱导细胞凋亡实现的。Caspase活性分析实验证明该样品是通过线粒体途径启动细胞凋亡。更多还原

【Abstract】 This paper studies the apoptosis of K562 cells in diisopropylphosphoryl leucyl-lysine methyl ester （（DIPP-L-Leu）₂- L-Lys-OCH₃） to investigate special induces in tumor cells. （DIPP-L-Leu）₂-L-Lys-OCH₃ was synthesized, then verified by ESI-MS, ³1P NMR, ¹H NMR and ¹3C NMR. The apoptosis was investigated using MTT assays, fluorescence microscopy, and AnnexinV-FITC flow cytometry analysis. The results show that （DIPP-L-Leu）₂-L-Lys-OCH₃ can induce apoptosis of K562 cells with an IC₅0 of 22.66 μmol·L^-1. Specific caspase assays show that （DIPP-L-Leu）₂-L-Lys-OCH₃ induces apoptosis in K562 cells through the mitochondrial pathway.更多还原