title: Potential toxicity of amphenicol antibiotic: binding of chloramphenicol to human serum albumin.
abstract: Antibiotics are widely used in daily life but their abuse has posed a potential threat to human health. To evaluate the toxicity of chloramphenicol (CAP) at the protein level, the interaction between CAP and human serum albumin (HSA) was investigated by fluorescence, Ultraviolet-visible (UV-Vis) absorption, Fourier transform infrared (FT-IR) spectroscopy and molecular docking methods. Fluorescence data revealed that the fluorescence quenching of HSA by CAP was the result of the formation of CAP-HSA complex, and the binding constant was determined to be 3.196 × 10(4) L mol(-1) at 310 K. The thermodynamic determination indicated that the interaction was driven by enthalpy change and entropy change together, where the multiple hydrogen bonds (CAP and the residues Arg 222 and His 242 of HSA) and van der Waals forces were the dominant binding force. The site marker competition revealed that CAP bound into sub-domain IIA of HSA. The binding of CAP induced the drastic reduction in α-helix conformation and the significant enhancement in β-sheet conformation of HSA. Molecular docking study further confirmed the binding mode obtained by experimental study. This work provides a new quantitative evaluation method for antibiotics to cause the protein damage.
authors.affiliation: School of Civil & Environmental Engineering, and National International Cooperation Base on Environment and Energy, University of Science and Technology Beijing, 30 Xueyuan Road, 100083, Beijing, People's Republic of China, chenhuilun@gmail.com.
authors.forename: Huilun
authors.initials: H
authors.lastname: Chen
authors.forename: Honghao
authors.initials: H
authors.lastname: Rao
authors.forename: Pengzhen
authors.initials: P
authors.lastname: He
authors.forename: Yongxiang
authors.initials: Y
authors.lastname: Qiao
authors.forename: Fei
authors.initials: F
authors.lastname: Wang
authors.forename: Haijun
authors.initials: H
authors.lastname: Liu
authors.forename: Minmin
authors.initials: M
authors.lastname: Cai
authors.forename: Jun
authors.initials: J
authors.lastname: Yao
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry*; D002701:Chloramphenicol / Q000737:chemistry*; D006801:Humans; D062105:Molecular Docking Simulation; D011485:Protein Binding; D017433:Protein Structure, Secondary; D012709:Serum Albumin / Q000737:chemistry*; D013050:Spectrometry, Fluorescence; D017550:Spectroscopy, Fourier Transform Infrared; D013816:Thermodynamics
chemical_list: D000900:Anti-Bacterial Agents; D012709:Serum Albumin; D002701:Chloramphenicol