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目的 从抗血管生成活性的角度 ,寻找新的抗肿瘤药物 ,研究Z2 4的体内抑瘤活性及其对血管内皮细胞的选择性抑制作用。方法 MTT法检测不同浓度的Z2 4作用 72h时对人肝癌细胞系BEL 74 0 2及正常人胚肺二倍体细胞 2BS的生长抑制作用 ,并从浓度 抑制率曲线求出IC50 ;台盼蓝拒染计数法检测不同浓度的Z2 4作用 72h时对人脐静脉内皮细胞 (HUVEC)的生长抑制作用 ,从浓度 抑制率曲线求出IC50 ;小鼠S180 ,H2 2和裸小鼠皮下移植性人肝癌BEL 74 0 2模型研究Z2 4的体内抑瘤作用。鸡胚尿囊膜 (CAM )血管生成模型检测Z2 4的血管生成抑制活性。结果 MTT法测得Z2 4对BEL 74 0 2生长抑制作用的IC50 为 10 6 μmol·L- 1,对 2BS生长抑制作用的IC50 为 116 μmol·L- 1。台盼蓝拒染计数法测得Z2 4对HUVEC生长抑制作用的IC50 为 6 .4 4μmol·L- 1。Z2 4可明显抑制鸡CAM新生血管的形成Z2 4 10 0mg·kg- 1可使S180 ,H2 2和裸小鼠人肝癌BEL 74 0 2模型的肿瘤重量较对照组分别下降 5 2 .5 %(n =10 ,P <0 .0 1) ,4 1.5 % (n =10 ,P <0 .0 1)和5 3.4 % (n =6 ,P <0 .0 1)。Z2 4可显著抑制CAM的血管生成。结论 Z2 4对多种肿瘤动物模型均具有显著的体内抑瘤活性 ,对血管内皮细胞有选择性抑制作用 ,并明显抑制CAM新生血管的生成?
Objective To search for new anti-tumor drugs from the perspective of anti-angiogenic activity and to study the antitumor activity of Z2 4 in vivo and its selective inhibitory effect on vascular endothelial cells. Methods MTT assay was used to detect the growth inhibition of human hepatocellular carcinoma cell line BEL 74 0 2 and normal human embryonic lung diploid cells 2BS at different concentrations of Z2 4 for 72 hours. IC50 was determined from concentration inhibition curve. Trypan blue The growth inhibition of human umbilical vein endothelial cells (HUVEC) treated with different concentrations of Z2 4 for 72h was detected by dye counting method. The IC50 was calculated from the concentration inhibition curve. S180, H2 2 and subcutaneous human hepatocellular carcinoma BEL 74 0 2 model to study the antitumor effect of Z2 4 in vivo. The chicken embryo allantoic membrane (CAM) angiogenesis model was tested for angiogenesis inhibitory activity of Z2 4. Results The IC50 of Z2 4 against BEL 74 0 2 was 106 micromol·L -1 and the IC50 of 2 ZS was 116 μmol·L -1. The IC50 of Z2 4 on the growth inhibition of HUVEC measured by trypan blue exclusion counting method was 6.44 μmol·L-1. Z2 4 could significantly inhibit the formation of chicken CAM angiogenesis Z2 4 10 0mg · kg-1 can make tumor weight of S180, H2 2 and BEL 74002 model of nude mice reduced by 52.5% n = 10, P <0.01), 4 1.5% (n = 10, P <0.01) and 5 3.4% (n = 6, P <0.01). Z2 4 significantly inhibited CAM angiogenesis. Conclusion Z2 4 has significant anti-tumor activity in vivo on a variety of tumor animal models and selectively inhibits vascular endothelial cells and significantly inhibits the formation of CAM neovascularization.