摘要
在酸性条件下,分别合成了四氯合钯(Ⅱ)离子与2种喹诺酮(诺氟沙星,NFLX=C16H18N3O3F;环丙沙星,CPLX=C17H18N3O3F)离子形成的配合物(NFLXH)2[PdCl4]·2H2O(1)和(CPLXH)2[PdCl4]·2H2O(2).用元素分析、IR、UV以及摩尔电导测定等方法对其进行了表征.配合物1的晶体结构经X射线单晶衍射确定,结构参数:三斜晶系,P-1空间群,a=0.84561(17)nm,b=0.94191(19)nm,c=1.2832(3)nm;α=111.26(3)°,β=97.23(3)°,γ=96.38(3)°,V=0.9312(4)nm3,Z=1,最后吻合因子R=0.040,wR=0.088.利用紫外光谱法、荧光光谱法对配合物与小牛胸腺DNA(ct-DNA)的作用进行了研究,研究表明,配合物对DNA的作用模式为插入作用,与DNA的结合常数Kb分别为:Kb(1)=2.06×104,Kb(2)=2.43×104.其后测试了配合物对体外肿瘤细胞的抗增殖活性.经采用四甲基偶氮唑蓝分析法(MTT法)测试后发现配合物1和2对人肺腺癌A549细胞、人原髓细胞白血病HL-60细胞的增殖抑制作用显著强于相应的喹诺酮分子本身,其中配合物2对人肺腺癌A549细胞增殖有明显的抑制作用,抑制率可高达(95.4±3.7)%,半数抑制浓度(IC50,72h)为(124.5±10.3)μmol·L-1.
The complexes of norfloxacin （NFLX=C16H18FN3O3）, ciprofloxacin （CPLX=C17H18FN3O3） with palladium ion [（NFLXH）2[PdCl4]·2H2O （1）, （CPLXH）2[PdCl4]·2H2O （2）] were synthesized under an acidic condition. Complex 1 is orange crystal and complex 2 is brown powder. By means of elemental analysis, IR, UV and molar conductance, the structures of the complexes were characterized. The structure of 1 was determined by single crystal X-ray crystallography, which is of triclinic space group P-1 with a= 0.84561（17） nm, b=0.94191（19） nm, c= 1.2832（3） nm; α= 111.26（3）°, β=97.23（3）°, γ=96.38（3）°, V= 0.9312（4） nm^3, Z= 1, R=0.040 and wR=0.088. The interactions between the complexes and ct-DNA were studied by ultraviolet absorption spectroscopy and fluorescence spectroscopy, indicating that the binding mode is intercalation and the binding constants （Kb） of the complexes with DNA respectively is： 2.06 × 10^4 （1）, 2.43 × 10^4 （2）. Antiproliferative activities of the complexes to tumors in vitro were tested by using an 3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide （MTT） method, showing that the complexes have more powerful inhibition effects on A549 cells and on HL-60 cells growth than quinolone itself. 2 has obvious inhibition effect on A549 cells growth： inhibition ratio on A549 cells reached （95.4 ±3.7）% and its IC50（72 h） on A549 cells was （124.5± 10.3） μmol,L^-1.
出处
《化学学报》
SCIE
CAS
CSCD
北大核心
2009年第14期1573-1578,共6页
Acta Chimica Sinica
基金
国家自然科学基金(No.20173050)资助项目
