头孢氨苄水解物的镍/锌单核配合物的合成、晶体结构及抗肿瘤活性  

Syntheses,Crystal Structures and Antitumor Activity of Ni(Ⅱ)/Zn(Ⅱ) Complexes Containing Cephalexin Hydrolysate

作　　者：杨晨 王国平[1] YANG Chen;WANG Guo-Ping(Department of Chemistry,Zhejicang University,Hangzhou 310027,China)

机构地区：[1]浙江大学化学系,杭州310027

出　　处：《无机化学学报》2018年第12期2172-2178,共7页Chinese Journal of Inorganic Chemistry

基　　金：浙江省教育厅科研基金(No.Y201122236)资助项目

摘　　要：以头孢氨苄(cephalexin)为原料合成锌和镍配合物,得到了2种新的单核配合物:[Ni(cepha)2]·6H2O (1)和[Zn(cepha)2]·6H2O(2)(cepha=cephalosporoate),通过元素分析、红外光谱、热重分析和X射线粉末衍射分析等方法表征1和2的结构,并通过X射线单晶衍射分析确定配合物的结构。配合物1和2均为正交晶系,空间群为P22121。头孢氨苄(cephalexin)在配位过程中发生水解产生头孢菌素中间体(cepha)并参与配位。金属离子与cepha形成六配位扭曲八面体几何构型,且通过分子间氢键将配合物进一步组装成三维网格结构。通过MTT法测定头孢氨苄、醋酸盐和配合物对乳腺癌细胞(MCF-7)和人肝癌细胞(HepG-2)的体外抗肿瘤活性,结果表明配合物1和2对MCF-7和HepG-2癌细胞均具有一定的抑制增殖活性。Two new mononuclear complexes,[Ni（cepha）2]·6H2O （1） and[Zn（cepha）2]·6H2O （2） （cepha=cephalo-sporoate） have been synthesized and characterized by elemental analysis, infrared spectroscopy, thermogravimetric analysis and X-ray powder diffraction analysis. The structures of complexes have also been determined by X-ray single crystal diffraction analysis, and the results show that the complexes 1 and 2 are both in orthorhombic system with space group P22121. The cephalexin hydrolyzes during the coordination process to produce cephalosporin intermediate, cephalosporoate （cepha）, which participates in coordination. Metal ion acts as six-coordinated center forming a distorted octahedral geometry, and the complexes are further extended to a three-dimensional network via intermolecular hydrogen bonds. The antitumor activity in vitro of cephalexin, metal acetate and complexes were carried out by MTT assay. The results reveal that complexes 1 and 2 have a certain inhibiting activity against MCF-7 and HepG-2 cell lines.

关 键 词：头孢氨苄 镍配合物 锌配合物 晶体结构 水解 抗肿瘤活性 

分 类 号：O614.813[理学—无机化学] O614.241[理学—化学]