PARP抑制剂WZ-8体内外抗肿瘤作用研究

朱勇; 王鸿; 何俏军

引用本文:	朱勇,王鸿,何俏军.PARP抑制剂WZ-8体内外抗肿瘤作用研究[J].中国现代应用药学,2014,31(6):682-686.
	ZHU Yong,WANG Hong,HE Qiaojun.Study of the Poly(ADP-ribose) Polymerase Inhibitor WZ-8 for Cancer Therapy in Vitro and in Vivo[J].Chin J Mod Appl Pharm(中国现代应用药学),2014,31(6):682-686.

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PARP抑制剂WZ-8体内外抗肿瘤作用研究
朱勇^1,2, 王鸿¹, 何俏军¹
1.浙江大学药学院药理毒理与生化药学研究所，杭州 310058;2.浙江省药品不良反应监测中心，杭州 310012

摘要:

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IC50为(0.21±0.01)mg·mL^-1。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。

关键词: PARP抑制剂 WZ-8 Iniparib 人结肠癌细胞HCT116

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

ZHU Yong^1,2, WANG Hong¹, HE Qiaojun¹

1.Institute of Pharmacology and Toxicology, School of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;2.Zhejiang Center for Adverse Drug Reaction Monitoring, Hangzhou 310012, China

Abstract:

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.

Key words: Poly(ADP-ribose) polymerase inhibitor WZ-8 Iniparib HCT116 cells