新型Schiff碱与DNA相互作用及其抗肿瘤活性研究  

Study on the interaction of novel Schiff base and DNA and its antitumor activities

作　　者：余英琳 廖向文[1] 潘伟健[1] 何荣伟[1] 应鹏[1] 陆家政[1] 

机构地区：[1]广东药学院药科学院,广州510006

出　　处：《山西医科大学学报》2013年第11期864-868,共5页Journal of Shanxi Medical University

基　　金：广东省大学生实验创新基金资助项目(1057310014);广东省科技计划基金资助项目(2012B031800431)

摘　　要：目的设计合成4种新型Schiff碱2-羟基-1-萘甲醛缩氨基硫脲、水杨醛缩氨基硫脲、2-羟基-1-萘甲醛缩异烟肼和水杨醛缩异烟肼并评价其体外抗肿瘤活性。方法紫外-可见分光光度法测定4种新型Schiff碱与小牛胸腺DNA的相互作用,采用MTT法研究它们对肿瘤细胞的抑制作用。结果 4种新型Schiff碱都能与CT-DNA通过插入方式进行结合,同时它们都对肿瘤细胞表现出很好的抑制作用。结论 Schiff碱具有良好的抗肿瘤活性,且Schiff碱的抗肿瘤活性可能与其DNA作用有相关性。Objective To synthesize four novel Schiff bases 2-hydroxy-l-naphthaldehyde thiosemicarbazone（I-INTD）, salicylaldehyde thiosemicarbazone （ SATS ）, 4-pyridinecarboxyhic acid, 2-[ （ 2-hydroxy ） -1 -napthalenylene ] hydrazide （ PAHN ）, and 4-pyridinecarboxyhic acid,2-[ （2-hydroxy）-1-phenyl ] methylene thydrazide （PAH）, and to investigate their antitumor activities. Methods The antitumor activities of the four novel Schiff bases against tumor cells were evaluated by MTI methods and their binding effects with calf thymus DNA were investigated using UV-Vis absorption. Results The results showed that these four Schiff bases exhibited considerable inhibitory activities against tumor cells and interacted with CT-DNA through intercalative modes. Conclusion All four Schiff bases have considerable inhibitory activities against tumor cells ,which are most likely to be associated with their structures.

关 键 词：SCHIFF碱 抗肿瘤活性 CT—DNA 

分 类 号：R962[医药卫生—药理学]