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1Effects of N-1 substituent on the phototoxicity of fluoroquinolone antibiotics: comparison of pefloxacin and difloxacin显示文摘The photophysics and photochemistry of pefloxacin(PEF),a 1-ethyl-substituted fluoroquinolone(FQ)antibiotic,were studied using transient,steady-state experimental methods and computational methods.The fundamental photoproperties of PEF and its phototoxicity toward lysozyme,a single-chain protein,were compared with those of a 1-fluorophenyl-substituted FQ antibiotic,difloxacin(DIF).The results showed that the phototoxicity was significantly decreased by the insertion of the bulky1-fluorophenyl substituent(the phototoxicity of DIF was approximately one-quarter of that observed for PEF).This trend was attributed to the lowest lying singlet state with sizeable oscillator strength(f C 0.1)being shifted from319 nm in PEF to 266 nm in DIF upon the insertion of the bulky substituent at the 1-position,as investigated by using computational methods.In addition,95%of the solar UV irradiation that reaches the earth’s surface has wavelength[315 nm.Therefore,reducing the most effective excitation wavelength by optimizing the substituent at the1-position may be a promising strategy to alleviate the phototoxicity of FQ antibiotics.These findings may be applied to other FQ antibiotics because a large number of phototoxicity studies on FQ antibiotics with different substituents at the 1-position can prove these finding’s effectiveness.Delafloxacin,an FQ antibiotic bearing a chlorine and bulky substituent at the 8-and 1-positions,respectively,exhibits no phototoxicity is the most recent example reported to date.To the best of our knowledge,this is the first transient and steady-state study of the effect of the N-1 substituent on the photochemistry and phototoxicity of FQ antibiotics.These findings will be beneficial to the development of novel FQ antibiotics without phototoxicity.Jian-Feng Zhao Yan-Cheng Liu Yu-Lie Xu Wen-Feng Wang 2020Nuclear Science and Techniques2020,31,7:1
2pH值和DO对UVA-LED光降解氧氟沙星的影响:动力学、机理及路径显示文摘在UVA-LED光照射下,考察了氧氟沙星在不同的pH值(3、7、11)和溶解氧浓度(DO=9、0 mg/L)条件下超纯水中的光降解过程。结果表明:其光降解过程符合一级反应动力学,主要为直接光降解,DO存在时,自敏化光降解有显著促进作用。在不同DO条件下,其光降解效率及速率均在pH值为7时最快,pH值为11时次之,pH值为3时最慢,氧氟沙星的光量子产率随pH值变化而变化是导致差异产生的主要原因。对降解产物及其生成过程进行分析表明,氧氟沙星的降解路径为脱甲基、哌嗪环的裂解和氧化、羟基化和脱羧基反应,不同pH值和DO条件下的降解路径及其产物差别细微,但其对产物在降解过程中的生成和进一步降解随时间的变化有显著影响。研究成果阐明了pH值和DO对氧氟沙星光降解的影响。姚娟娟 甘敬业 夏彬 2020土木与环境工程学报(中英文)2020,42,3:1
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