氟喹诺酮类药物与蛋白质相互作用的研究(英文)

A study of the interaction between fluoroquinolone antibiotics and proteins by fluorescence quenching measurements

运用荧光淬灭机理研究了氟喹诺酮类药物洛美沙星,氧氟沙星,衣诺沙星与3种蛋白质(牛血清蛋白,免疫球蛋白,胰蛋白酶)之间的相互作用,计算了两者之间的结合常数和结合位点数,根据实验当中所得的热力学参数确定了它们之间的作用类型,氟喹诺酮类药物的含量与其荧光强度呈现良好的线性关系,在此实验条件下测定了胶囊及人工合成样中洛美沙星和衣诺沙星的含量,其浓度范围分别为0.018～0.878和0.030～3.171μg/mL。

The results from the fluorescence spectra studies showed the binding characteristics of fluoroquinolone antibiotics including lomefioxacin(Lome), ofloxacin(OF) and enoxacin(Enox) with three proteins, bovine serum albumin(BSA), human immunoglobulin G(IgG) and trypsin. The binding constant K and the number of binding sites n were also calculated. Meanwhile, the determination method for the fiuoroquinolones in the capsule and the artificial synthetic samples were studied due to their intense fluorescence related to the macrocyclic-aromatic structures. The results showed a good linear relationship between fluorescence intensities and the concentrations of fluoroquinolones. The concentration ranges of Lome and Enox are 0.018～0.878μg/mL and 0.030～3.171 μg/mL, respectively.