香豆素-希夫碱衍生物的体外抗肿瘤活性研究

In vitro antitumor activity of coumarin-schiff base derivatives

目的:探讨香豆素-希夫碱衍生物的体外抗肿瘤作用。方法:通过MTT法测试香豆素-希夫碱衍生物对4种人癌细胞株和1种人正常细胞株的抑制作用,并通过流式细胞仪对代表性化合物5k的作用机制进行了研究。结果:化合物4b、5b、5e、5f、5g、5k、5l、5n对某些肿瘤细胞株的抑制活性明显优于常用抗癌药物5-氟脲嘧定(5-FU),且它们对人肝正常细胞HL-7702的毒性显著小于5-FU;化合物5k可诱导人胃癌细胞MGC-803凋亡,并主要将MGC-803细胞阻滞在G1期。结论:香豆素-希夫碱衍生物对某些人癌细胞株具有良好的体外抑制作用。

Objective： To investigate the in vitro antitumor activities of some coumarin-schiff base derivatives. Methods： The in vitro antitumor activities of coumarin-schiff base derivatives against four cancer cell lines and a normal cell line were then determined by MTT method. Moreover,apoptosis and cycle arrest mechanism of the representative compound 5k was then performed. Results： Compounds 4b,5b,5e,5f,5g,5k,5l and 5n exhibited better antiproliferative activity than the commercial anticancer drug（ 5-FU） against some cancer cell lines,they also showed lower cytotoxicity than that of 5-FU against human normal liver cell line HL-7702. In addition,the result also demonstrated that compound 5k could induce human gastric carcinoma cell MGC-803 and arrest it in G1 stage. Conclusion： Coumarin-schiff base derivatives exhibits good in vitro antitumor activities against some human cancer cell lines.