氟喹诺酮类药物的光化学性质及其光敏毒性机理  

Photochemistry and Phototoxicity of Fluoroquinolones

作　　者：张鹏[1,2] 李海霞[1,2] 刘艳成[1,2] 王文锋[1] 

机构地区：[1]中国科学院上海应用物理研究所,上海201800 [2]中国科学院研究生院,北京100049

出　　处：《生物物理学报》2010年第11期1015-1024,共10页Acta Biophysica Sinica

基　　金：国家自然科学基金项目(10675158)~~

摘　　要：氟喹诺酮类药物(fluoroquinolones,FQs)是目前得到广泛应用的广谱、高效的合成抗菌素。本文通过对FQs光化学研究进展的介绍,详述了具有代表性的FQs的光物理、光化学性质及光化学反应途径,以及其对生物分子的光敏损伤机理等。FQs具有较高的三重激发态产额,其激发态能够发生多种光化学反应,此类反应极易受到溶剂性质和某些盐类的影响,其光敏毒性与其分子结构有着密切的联系,尤其受8位取代基的影响非常大。对该类药物光化学性质和光敏毒性机理的研究,将会对此类药物的合理使用和新一代药物的研发提供很好的理论依据。Fluoroquinolones are widely used as broad-spectrum antimicrobials.In the past decade,these drugs have been the object of increasing interest due to the finding of their phototoxic and photocarcinogenic properties.The mechanisms underlying the phototoxic reactions are not known exactly,and one prerequisite for a deeper understanding is the exact knowledge of photochemistry of these drugs.The photophysical and photochemical properites of a series of structurally related,representative fluoroquinolone drugs,different photoreaction processes and their rationalizations are reviewed.The results can help understand the correlation between structural characteristics and photochemical,phototoxic properties.This review focuses on： structural characteristics of representative fluoroquinolones;the UV and fluorescence spectra in different pH and solvents;quantum yields and quenching-rate constants of triplet states by oxygen,some inorganic salts and some biomolecules;photoionization process;defluorination at 6 and 8 position;decarboxylation and side-chain degradation;transient intermediates generated in the photoprocesses of fluoroquinolone drugs and their dynamic processes;photodamage of DNA and proteins by fluoroquinolones.General trends in the photoreactivity and phototoxicity of fluoroquinolone drugs are also presented.

关 键 词：氟喹诺酮 光化学 光敏毒性 激光光解 脉冲辐解 

分 类 号：Q632[生物学—生物物理学]