PARP抑制剂WZ-8体内外抗肿瘤作用研究

Study of the Poly(ADP-ribose) Polymerase Inhibitor WZ-8 for Cancer Therapy in Vitro and in Vivo

目的研究PARP抑制剂WZ-8对人源性肿瘤细胞增殖及裸鼠移植人结肠癌(HCT116)生长的抑制作用。方法 SRB染色法和裸小鼠移植瘤模型研究WZ-8在体内外抗肿瘤作用。结果体外WZ-8对多种人肿瘤细胞增殖有明显抑制作用,其中对结肠癌细胞HCT116的半数抑制浓度IC-50为(0.21±0.01)-g·mL1。体内研究表明WZ-8(20 mg·kg-1)对小鼠移植HCT116肿瘤生长有一定抑制效果,其体内外抗肿瘤活性均高于同类化合物Iniparib。结论 WZ-8在体外对人源性肿瘤细胞增殖有明显抑制作用,在体内可抑制裸鼠移植人结肠癌细胞HCT116的生长。

OBJECTIVE To investigate the effect of poly（ADP-ribose） polymerase inhibitor WZ-8 on proliferation and growth of human colonic carcinoma HCT116 cells in vitro and in vivo. METHODS SRB assay and xenografted model were performed to detect proliferation inhibition effect of WZ-8 on cancer cells. RESULTS WZ-8 obviously inhibited the growth of 10 different human cancer cells in vitro. The IC50 of WZ-8 on HCT116 cells was lower than other cancer cells. WZ-8 also exhibited higher anti-tumor activity of HCT116 xenografted mice than Iniparib in vivo. CONCLUSION WZ-8 exertes a significant inhibition on proliferation and growth of HCT116 cancer cells both in vitro and in vivo.