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在体外研究发现酰亚胺类G-四链体配体Tel03能够诱导K562白血病细胞凋亡。本研究进一步用动物实验探讨Tel03的体内抗白血病瘤体细胞作用。建立裸鼠K562白血病瘤体模型,将实验用小鼠随机分为实验组和对照组,实验组分别腹腔注射等体积(300μl)含有不同剂量(5mg/kg和15mg/kg)Tel03药液的2组动物,对照组注射等量灭菌PBS,每周2次,连续4周。观察各组瘤体体积和动物体重,采用缺口末端标记技术(TUNEL法)检测瘤体细胞凋亡,Western blot检测Bcl-2和Bax的表达。结果表明:Tel03显著抑制动物白血病瘤体细胞的生长,实验组与对照组相比,瘤体均显著缩小,并且在小剂量组(5mg/kg Tel03)中Tel03诱导瘤体细胞凋亡的同时对动物不产生明显毒性作用。蛋白水平分析证实,Tel03抑制bcl-2表达同时诱导bax表达。结论:G-四链体配体Tel03具有诱导白血病瘤体细胞凋亡的作用,有用于白血病治疗的可能性。
In vitro studies showed that imide G-quadruplex ligand Tel03 was able to induce apoptosis in K562 leukemia cells. In this study, animal experiments were further used to investigate the in vivo anti-leukemia tumor cell effect of Tel03. The nude mice model of K562 leukemia was established. The experimental mice were randomly divided into experimental group and control group. The experimental groups were injected intraperitoneally with equal volume (300μl) of Tel03 solution containing different doses (5mg / kg and 15mg / kg) The animals in the control group were injected with the same amount of sterile PBS twice a week for 4 weeks. Tumor volume and body weight were observed in each group. TUNEL method was used to detect the apoptosis of tumor cells. Western blot was used to detect the expression of Bcl-2 and Bax. The results showed that: Tel03 significantly inhibited the growth of somatic cells in animal leukemia, the experimental group compared with the control group, the tumor was significantly reduced, and in a small dose (5mg / kg Tel03) Tel03 induced tumor cell apoptosis at the same time Animals do not produce significant toxic effects. Protein level analysis confirmed Tel03 inhibited bcl-2 expression while inducing bax expression. Conclusion: Tel-04, a G-quadruplex ligand, has the potential to induce apoptosis in leukemia tumor cells and is potentially useful in the treatment of leukemia.