赖氨酰谷氨酸二肽的抗肿瘤活性研究

目的研究二肽Lys-Glu(Vilon)的抗肿瘤活性。方法用液相法人工合成了抗肿瘤二肽Vilon,分子量为275.3。用细胞计数法和MTT法测定Vilon对人肠癌LOVO,人胃癌MKN45和人肝癌QGY77033种肿瘤细胞生长的抑制作用,以及对人体正常细胞生长的影响;并对其进行了体内实验。结果Vilon对体外培养的LOVO,MKN45和QGY7703细胞具有剂量依赖性抑制作用,但对人正常白细胞无明显抑制作用。体内抑瘤实验表明,Vilon对小鼠肝癌H22的生长有抑制作用,有效剂量为15mg.kg-1,当使用高剂量30mg.kg-1时,对小鼠移植性肿瘤肝癌H22的抑瘤率达0.60以上,且具有剂效关系。结论Vilon具有明显的体外、体内抗肿瘤活性。

Antitumor activity of Vilon dipeptide Lys-Glu

Aim To study the antitumor activity of Dipeptide Lys-Glu (Vilon). Methods Dipeptide Vilon, which molecular weight is 275.3, was synthetized by the liquid-phase synthetic method. Proliferation inhibition of human intestines tumor cell of LOVO, human stomach tumor cell MKN-45 and human liver tumor cell QGY7703 assays were examined by cell accounting and MTT method, and test the influence of healthy human normal leucocytes. Experiments in vivo were tested by treatment on tumor mice. Results Vilon exerted strong dose-dependent inhibition on the proliferation of three tumor cell lines, but not human normal leucocytes. Treatments on tumor mice showed that effectively inhibited tumor growth of mice H22 hepatoma with apparently dose-dependent effect. The most minimum efficient dose was 15 mg·kg-1. When higher dose (30 mg·kg-1) was used, the inhibition rate of mice H22 hepatoma reached above 60%. Conclusion Vilon has apparent antitumor activity in vitro and vivo.