氧氟沙星金属配合物的光谱与抗肿瘤活性

Synthesis,Spectral Analysis,Antibacterial and Antitumor Activities of Co(Ⅱ) and Ni(Ⅱ) Ofloxacin Complexes

合成了以氧氟沙星为配体的钴(Ⅱ)、镍(Ⅱ)配合物M(ofo)2·4H2O(M=Co,Ni;ofo=ofloxacin,Ⅰ),通过元素分析、红外光谱和热分析等方法对配合物的结构进行了表征,钴(Ⅱ)、镍(Ⅱ)分别为中心原子,与氧氟沙星配体3位羧基的一个氧原子和4位酮基氧原子配位,推测了配合物的可能结构,讨论了配合物的荧光光谱性质,利用液体稀释法测定了药物配体和配合物对两种革兰氏阳性菌和两种革兰氏阴性菌的体外抑制活性,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,结果表明配合物与药物配体的抗菌活性和抗菌谱相同,配合物对BEL-7402细胞没有抑制作用,对HL-60细胞在较高浓度时有一定的抑制作用。

The interactions of cobalt sulphate and nickel acetate with ofloxacin （ofo, Ⅰ ）, a 4-quinoline derivative, were studied. The hydrothermal technique was adopted in this work. The isolated solid complexes were characterized by elemental analysis, infrared spectra, electronic spectra, fluorescence spectra and thermal analysis. The results support the formation of complexes of the formula Co（ofo）2 · 4H2O （ Ⅱ ） and Ni（ofo）2· 4H2O （ Ⅲ ）. The infrared spectra of the isolated solid complexes suggested that ofo acts as bidentate ligands through one of the oxygen atoms of the earboxylic group and the ring earbonyl oxygen atom. Thermogravimetric （TG） and its differential （DTG） were carried out for the complexes. The data obtained indicated that the thermal decomposition of the two complexes in inert atmosphere proceeded approximately with two main degradation steps. Ⅰ showed a intense fluorescence in solid state at λex/λem = 365 nm/461 nm, and two complexes displayed weakly similar emission maximum at 470 nm in the powder samples at ambient temperature, while the emission of Ⅱ and Ⅲ may be mainly originated from the intraligand excited states of Ⅰ,Ⅰ, Ⅱ and Ⅲ were assayed against two kinds of gram-positive and two kinds of gramnegative bacteria by in vitro doubling dilutions method. The results indicated that Ⅱ and Ⅲ have the similar minimal inhibitory concentration （MIC）as the Ⅰ against S. Aureus, M. Lutens, E. ColiandP. Aeruginosa. The inhibitory effect of Ⅰ, Ⅱ and Ⅲ on leukemia HL-60 cell line has been measured by using MTT （Methyl-Thiazol-Tetrozolium） method and that on liver cancer BEL-7402 cell line measured by SRB （Sulphurhodamin B） method. The results indicated that the complexes in the high concentration have inhibitory effect on HL-60 cell line.