蛇葡萄素的抗肿瘤作用研究

Antitumor Effects of Ampelopsin

目的:研究蛇葡萄素在体内外对肿瘤生长的抑制作用。方法:用MTT法测定蛇葡萄素对人鼻咽癌HK-1细胞和人乳腺癌MCF-7细胞的体外细胞毒实验;观察蛇葡萄素对C57BL/6小鼠移植性B16黑色素瘤的体内抑瘤作用;用流式细胞仪测定含药小鼠血清对B16细胞周期及细胞增殖的影响。结果:蛇葡萄素对人鼻咽癌HK-1细胞及人乳腺癌MCF-7细胞的IC50分别为50.0μg/ml及79.4μg/ml。在100mg/kg、150mg/kg及200mg/kg的剂量下,与生理盐水对照组比较,蛇葡萄素对C57BL/6小鼠移植性B16黑色素瘤的抑瘤率分别为25.54%(P<0.05)、32.03%(P<0.01)及54.55%(P<0.001);60mg/kg氮烯咪胺(阳性对照组)的抑瘤率为59.31%,与200mg/kg的药物组比较无显著性差异(P>0.05);在150mg/kg及200mg/kg蛇葡萄素腹腔给药后10min的小鼠含药血清的作用下,B16细胞的G1期和G2/M期细胞数增高,S期细胞数减少,分裂增殖指数分别降低19.1%及21.7%。结论:蛇葡萄素对体外肿瘤细胞HK-1和MCF-7的增殖,及体内小鼠移植性B16黑色素瘤的生长均具有显著的抑制作用。

Objective: This study was designed to investigate the inhibitory effects of ampelopsin on tumors in vivo and in vitro. Methods: The in vitro cytotoxicity of ampelopsin was assessed against human nasopharyngeal carcinoma HK 1 and mammary cancer MCF 7 cell lines by MTT assay. The in vivo anti tumor effect of ampelopsin was evaluated by observation of growth inhibition of B16 melanoma inoculated into C57BL/6 mice. B16 melanoma cells were treated with drug serum of mice that were administered by ampelopsin, then the cells cycle distribution were detected by flow cytometry. Results: Ampelopsin at the 100 mg/kg dose, 150 mg/kg dose, and 200 mg/kg dose of, the growth inhibition of the transplant tumor was 25.54%(P< 0.05), 32.03%(P< 0.01), and 54.55%(P< 0.001),respectively,by compare with the normal saline control. The 60 mg/kg dose of deticene resulted in 59.31% growth inhibition that was not significant different compared to that of the 200 mg/kg dose of ampelopsin (P >0.05).In the influence of ampelopsin sample serum of the mice administered intraperitoneally after 10 min, melanoma B16 cells treated with serum of the mice,which was received ampelopsin intraperitoneally 10 min after warks,showed that the Phase G1 and Phase G2/M cells increased and the Phase S cells decreased obviously. The cleavage and proliferation index number of B16 melanoma cells were reduced 19.1% and 21.7% at the doses of 150 mg/kg and 200 mg/kg of ampelopsin, respectively. The IC50 values for the in vitro cytotoxicity of ampelopsin on nasopharyngeal carcinoma HK 1 cells and mammary cancer MCF 7 cells ware 50.0 μg/ml and 79.4 μg/ml, respectively. Conclusion: Ampelopsin appears to be a potent anti tumor agent that was firstly discovered in the in vivo transplant B16 mouse melanoma and the in vitro human nasopharyngeal carcinoma HK 1 cell and mammary cancer MCF 7 cell.