左氧氟沙星铜(Ⅱ)配合物的合成及生物活性研究

Study on the synthesis and biological activities of copper(Ⅱ)complexes with levofloxacin

合成了四个新左氧氟沙星铜(Ⅱ)配合物:[Cu(Lvfx)(Bipy)(H2O)]Cl.4H2O(1),[Cu(Lvfx)(Phen)(H2O)]Cl.5H2O(2),[Cu(Lvfx)(Tatp)(H2O)]Cl.5H2O(3),[Cu(Lvfx)(Dppz)(H2O)]Cl.4.5H2O(4){Lvfx=左氧氟沙星,Bipy=2,2’-联吡啶,Phen=1,10-邻菲罗啉,Tatp=1,4,8,9-四氮三联苯,Dppz=二吡啶并[3,2-a:2’,3’-c]吩嗪},并通过红外光谱法、紫外-可见光谱法、元素分析、原子吸收光谱法、摩尔电导率分析和差热-热重分析对配合物进行了表征。用滤纸片扩散法和试管二倍稀释法分别测试了配合物及配体对大肠杆菌、金黄色葡萄球菌的抗菌活性,结果显示配合物(3)对大肠杆菌具有最佳的抑菌效果。采用荧光光谱法初步研究了配合物与BSA的相互作用。结果表明,四个配合物均对BSA的荧光有较强的猝灭作用,且发生了能量转移,其与BSA的结合常数(K)分别为4.7×102、5.7×103、5.0×103和1.7×103L.mol-1,结合位点n分别为0.59、0.83、0.81和0.69。

Four new copper（II） complexes with levofloxacin： [ Cu （Lvfx） （Bipy） （ H2O） ] Cl· 4H2O （ 1 ）, [ Cu （Lvfx） （Phen） （ H2O） ]Cl· 5H2O（2）, [ Cu（Lvfx） （Tatp） （H2O） ] Cl· 5H2O（3） and[ Cu（Lvfx） （Dppz） （H2O） ] Cl·4. 5H2O（4） （ Lvfx = Levo- fioxacin, Bipy = 2,2＂-bipyridine, Phen = 1,10 -phenanthroline, Tatp = 1,4,8,9 -tetraazatriphenylene, Dppz = dipyrido [ 3,2 -a： 2＂, 3 ＂-c ] phenazine）were synthesized and characterized by IR, UV-visible spectrometry, elemental analysis, atomic absorption spectrometry, molar conductivity and DTA-TG. The antibacterial activity of complexes and ligands were assayed against E. coli and Staphylococcus aureus using the filter paper diffusion and the double dilution method, and complex 3 showed the best inhibitory effect against E. co- li. The interaction between the complexes and BSA was investigated by fluorescence spectroscopy. The results showed that complexes could strongly quench fluorescence of BSA, accompanying energy transfer. The binding constants （K）were calculated as 4. 7 ×102, 5.7×103 ,5.0×103 and 1.7×103 L · mo1-1 for complexes 1-4 ,and binding sites n were 0. 59,0. 83,0. 81 and 0. 69 ,respectively.