摘要
目的:对14个合成的丹参水溶性单体类似物进行抗肿瘤活性筛选,并研究其抗肿瘤相关机制。方法:MTT法检测化合物的抗肿瘤细胞增殖活性;流式细胞术检测目标化合物对细胞周期的影响;Gi-emsa染色观察化合物对细胞有丝分裂的影响;Western Blot检测化合物对细胞周期蛋白表达的影响。结果:14个化合物中,化合物ERJT-12对多种人肿瘤细胞株均有生长抑制作用,ERJT-12使人乳腺癌细胞株MCF-7阻滞于G2/M期,并使其有丝分裂指数明显提高;ERJT-12作用下,MCF-7细胞中G2/M期相关蛋白质CDK1的活性下降,CyclinB1蛋白表达下调。结论:化合物ERJT-12能抑制肿瘤细胞的生长并引起细胞周期改变,具有较好的抗肿瘤活性。
Objective：To screen antineoplastic compounds from 14 synthesized analogs of the salvia miltiorrhiza monomers,and explore the action mechanisms.Methods：The antiproliferative activity of these compounds was determined by MTT method.Cell-cycle distribution was detected by flow cytometry.Mitotic index of cells was determined by Wright-Giemsa staining.The expression of cell cycle proteins were detected by Western blot.Results：Among 14 compounds screened,compound ERJT-12 showed a significant antiproliferative activity in a variety of human tumor cell lines.ERJT-12 arrested cell cycle in G2/M phase and increased the mitotic index in MCF-7 cells.It also suppressed activity of CDK1 protein and down-regulated the expression of cyclin B1.Conclusion：ERJT-12 can inhibit the growth of tumor cells and arrest cell cycle.It shows relatively potent antineoplastic activity and is valuable for further investigation.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2011年第16期1563-1568,共6页
Chinese Journal of New Drugs
基金
广西教育厅科研资助项目(201012MS048)
关键词
丹参
抗肿瘤活性
细胞周期
MCF-7细胞
salvia miltiorrhiza
antineoplastic activity
cell cycle
MCF-7 cell
