Effects of N-1 substituent on the phototoxicity of fluoroquinolone antibiotics: comparison of pefloxacin and difloxacin
文献类型：期刊论文
| 作者 | Zhao, JF; Liu, YC; Xu, YL; Wang, WF |
| 刊名 | NUCLEAR SCIENCE AND TECHNIQUES
 |
| 出版日期 | 2020 |
| 卷号 | 31期号:7页码:- |
| ISSN号 | 1001-8042 |
| 关键词 | PHOTOCHEMICAL PROPERTIES PHOTOSENSITIZED OXIDATION AQUEOUS-SOLUTION GRAPHENE OXIDE EXCITED-STATES STEADY-STATE LOMEFLOXACIN OXYGEN LYSOZYME KINETICS |
| DOI | 10.1007/s41365-020-00776-9 |
| 文献子类 | 期刊论文 |
| 英文摘要 | 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 bulky 1-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 >= 0.1) being shifted from 319 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 the 1-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. |
| 语种 | 英语 |
| 源URL | [http://ir.sinap.ac.cn/handle/331007/32833]  |
| 专题 | 上海应用物理研究所_中科院上海应用物理研究所2011-2017年 |
| 作者单位 | 1.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Appl Phys, Shanghai 201800, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhao, JF,Liu, YC,Xu, YL,et al. Effects of N-1 substituent on the phototoxicity of fluoroquinolone antibiotics: comparison of pefloxacin and difloxacin[J]. NUCLEAR SCIENCE AND TECHNIQUES,2020,31(7):-. |
| APA | Zhao, JF,Liu, YC,Xu, YL,&Wang, WF.(2020).Effects of N-1 substituent on the phototoxicity of fluoroquinolone antibiotics: comparison of pefloxacin and difloxacin.NUCLEAR SCIENCE AND TECHNIQUES,31(7),-. |
| MLA | Zhao, JF,et al."Effects of N-1 substituent on the phototoxicity of fluoroquinolone antibiotics: comparison of pefloxacin and difloxacin".NUCLEAR SCIENCE AND TECHNIQUES 31.7(2020):-. |
入库方式： OAI收割
来源：上海应用物理研究所
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