钆(III)-喹诺酮配合物的合成、抗菌活性与抗肿瘤活性

Synthesis, characterization, antibacterial and antitumor activities of three gadolinium (III) complexes containing fluoroquinolones

合成了以喹诺酮药物分子(诺氟沙星、氧氟沙星和环丙沙星)为配体的钆(III)配合物Gd(L)3·6H2O(L为药物配体).通过红外光谱、摩尔电导率、元素分析和顺磁共振等方法对配合物进行了表征,推测了配合物的可能结构,并用液体稀释法测定了药物配体和配合物对2种革兰氏阳性菌和2种革兰氏阴性菌的体外抑制活性,结果表明配合物与药物配体的抗菌活性和抗菌谱相同;采用MTT比色法测定了配体及配合物对HL-60(人急性早幼粒白血病)细胞的抑制作用,采用SRB蛋白染色法测定了配体及配合物对BEL-7402(人肝细胞性肝癌)细胞的抑制作用,结果表明Gd(OFLX)3·6H2O对BEL-7402细胞有强效抑制作用,Gd(CPLX)3·6H2O对HL-60和BEL-7402细胞均有强效抑制作用.

Three novel Gadolinium complexes of fluoroquinolone, Gd(L)3·6H2O {L= Norfloxacin (NFLX), Ofoxacin (OFLX) and Ciprofloxacin (CPLX), respectively}, were synthesized. The compounds were characterized by FTIR, molar conductivity, elemental analysis and electron paramagnetic resonance (EPR) spectra. In all of the complexes, the ligand L is coordinated through Ocarbox and Oketo atoms. Both ligands and complexes were assayed against grampositive and gramnegative bacteria by in vitro doubling dilutions method, the complexes showed the same minimal inhibitory concentration (MIC) as the corresponding ligands against Staphylococcus Aureus, Micrococcus Lutens, Escherichia Coli and Pseudomonas Aeruginosa. The inhibitory effect of the ligands and complexes on leukemia HL60 cell line was measured by using MTT (MethylThiazolTetrozolium) assay method and liver cancer BEL7402 cell line measured by SRB (Sulphurhodamin B) method. The results indicated that the complex Gd(OFLX)3·6H2O has strong inhibitory effect on BEL7402 cell line, Gd(CPLX)3·6H2O has strong inhibitory effect on HL60 cell line and on BEL7402 cell line.