5-甲基水杨醛缩对氨基水杨酸希夫碱铜配合物合成表征与体外抗肿瘤活性研究  

Copper complex of 5-methyl-amino salicylic acid salicylaldehyde Schiff base: synthesis, characterization and antitumor activity in vitro

作　　者：郭永胜[1] 陈红林[1] 刘文[2] 孙体健[2] 

机构地区：[1]山西省肿瘤医院放疗科,太原030013 [2]山西医科大学基础医学院医学化学教研室

出　　处：《中国药物与临床》2016年第7期940-942,I0001,共4页Chinese Remedies & Clinics

基　　金：山西省自然科学基金(2013011060-3)

摘　　要：目的合成5-甲基水杨醛缩对氨基水杨酸希夫碱铜配合物药物并研究其体外抗肿瘤作用。方法采用常规加热回流法合成目标化合物,利用紫外吸收、元素分析和红外光谱等方法对其进行表征研究。采用四甲基偶氮唑盐(MTT)法考察药物对人宫颈癌细胞Si Ha和He La增殖的抑制作用,并采用吖啶橙/溴乙锭(AO/EB)双染色荧光显微镜观察药物对Si Ha细胞形态的变化。结果目标化合物的组成为[C30H24N2O8Na2Cu]·2H2O;对Si Ha和He La细胞都有不同程度的抑制作用,呈现良好的剂量-效应关系,对Si Ha的活性优于He La;并且可使肿瘤细胞的形态发生显著变化,引起细胞株的凋亡或坏死。结论 5-甲基水杨醛缩对氨基水杨酸希夫碱铜配合物能抑制人宫颈癌细胞Si Ha和He La的增殖,在体外有良好的抗肿瘤活性。Objective To synthesize the copper complex of 5-methyl-amino salicylic acid Schiff base and determine its anti-tumor effect in vitro. Methods The conventional heating under reflux method was used for synthesis of the target compound. Ultraviolet absorption, elemental analysis and infrared spectroscopy were employed to charac-terize the synthesized product. MTT assay was used to investigate the inhibitory effect of the copper complex against proliferation of human cervical cancer Si Ha and He La cell lines. AO/EB double staining fluorescence microscopy was used to study the change in Si Ha cell morphology as induced by the copper complex. Results The molecular formula of the target compound was found to be [C30H24N2O8Na2Cu]·2H2O. The copper complex exhibited varying degrees of inhibitory effects on Si Ha and He La cell lines in a significant dose-response manner. The anti-tumor effect was more active against Si Ha than He La cells. The compound was found to induce obvious changes in tumor cell morphology,apoptosis or necrosis of the tumor cell lines. Conclusion The copper complex of 5-methyl-aminosalicylic acid Schiff base may inhibit the proliferation of He La and Si Ha cell lines of cervical cancer, and thereby shows satisfactory anti-tumor activity in vitro.

关 键 词：希夫碱类 HELA细胞 铜配合物 抗肿瘤活性 Si Ha细胞 

分 类 号：R96[医药卫生—药理学]