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化合物209是一个新合成的氨基二硫代甲酸酯类化合物,它在体外水平可以抑制肿瘤细胞的增殖,但是化合物209的体内抗肿瘤作用及其抗肿瘤机制并不明确。本文探究了化合物209对人结直肠癌细胞HT-29的作用并初步探讨了相关机制。体外研究表明,化合物209可以显著抑制HT-29细胞的增殖;体内研究结果表明,化合物209可以显著抑制裸鼠HT-29移植瘤的生长,但是对裸鼠体重和白细胞无影响。流式细胞分析实验结果表明,化合物209可将HT-29细胞阻滞于细胞周期的G1期。同时,化合物209能上调体外培养HT-29细胞中p27,cyclin E,CDK2,cyclin D1和CDK4的表达。在体内瘤组织中上述蛋白表达情况与体外实验结果一致。这些结果说明,化合物209具有较好的抗肿瘤活性,其抗肿瘤作用与细胞周期阻滞及其相关蛋白的表达变化有关。
Compound 209 is a newly synthesized aminodithiocarbamate compound which inhibits the proliferation of tumor cells in vitro. However, the anti-tumor effect of compound 209 in vivo and its antitumor mechanism are not clear. This article explored the effect of compound 209 on human colorectal cancer cells HT-29 and explored the underlying mechanisms. In vitro studies showed that Compound 209 significantly inhibited the proliferation of HT-29 cells. In vivo studies showed that compound 209 significantly inhibited the growth of HT-29 xenografts in nude mice but did not affect the body weight and white blood cells of nude mice. Flow cytometry results showed that compound 209 blocked HT-29 cells in the G1 phase of the cell cycle. Meanwhile, Compound 209 can up-regulate the expression of p27, cyclin E, CDK2, cyclin D1 and CDK4 in HT-29 cells cultured in vitro. The above protein expression in in vivo tumor tissue is consistent with in vitro experimental results. These results indicate that compound 209 has good antitumor activity, and its anti-tumor effect is related to the change of cell cycle arrest and the expression of related proteins.