抗菌氟喹诺酮类及其萘衍生物的光氧化剂性质研究。

Studies of the photooxidant properties of antibacterial fluoroquinolones and their naphthalene derivatives.

作者信息

Vargas F, Zoltan T, Ramirez A H, Cordero T, Chavez V, Izzo C, López V, Cárdenas Y M, Fernández A, Hincapie L, Fuentes A

机构信息

Laboratorio de Fotoquímica, Centro de Química, Instituto Venezolano de Investigaciones Científicas I.V.I.C., Carretera Panamericana Klm. 11, Apartado 20632, Caracas 1020-A, Venezuela.

出版信息

Pharmazie. 2009 Feb;64(2):116-22.

PMID:19320285

Abstract

We synthesized and determined the production of reactive oxygen species (ROS) as 1O2, *-O2, *OH, H2O2 during the photolysis with UV-A light of three antibacterial quinolones and their naphthyl ester derivatives. Singlet oxygen and ROS dose-dependant generation from norfloxacin (1), enoxacin (2), ciprofloxacin (3) and their respective naphthyl ester derivatives 4-6 were detecting in cell-free systems by the histidine assay and by luminol-enhanced chemiluminescence (LCL). Both the electronic absorption and emission spectra were quantified and their photostability determined. The antibacterial activity in darkness and under irradiation of compounds 4, 5 and 6 was tested on E. coli and compared with their parent drugs.

摘要

我们合成并测定了三种抗菌喹诺酮及其萘酯衍生物在紫外-A光光解过程中作为单线态氧（¹O₂）、超氧阴离子自由基（·O₂⁻）、羟基自由基（·OH）、过氧化氢（H₂O₂）的活性氧（ROS）生成情况。通过组氨酸测定法和鲁米诺增强化学发光法（LCL）在无细胞体系中检测了诺氟沙星（1）、依诺沙星（2）、环丙沙星（3）及其各自的萘酯衍生物4 - 6产生的单线态氧和ROS剂量依赖性生成情况。对电子吸收光谱和发射光谱进行了定量，并测定了它们的光稳定性。在黑暗和光照条件下测试了化合物4、5和6对大肠杆菌的抗菌活性，并与它们的母体药物进行了比较。