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.

Development of a quantitative fluorescence-based lateral flow immunoassay for determination of chloramphenicol, thiamphenicol and florfenicol in milk

“…With the health side-effects to humans and the emergence of drug-resistant bacteria (Chen et al, 2014), the use of these antibiotics was strictly limited in many countries including China, European Community, the United States, Canada and Japan. In China, CAP was prohibited for use in any food-producing animals and the maximum residue limit for TAP was set at 50 μg L −1 in milk.…”

Investigation on the interaction of antibacterial drug moxifloxacin hydrochloride with human serum albumin using multi-spectroscopic approaches, molecular docking and dynamical simulation

“…40 To investigate the possible binding sites of MOXH, site marker displacement studies were conducted using phenylbutazone and ibuprofen as sites I and II probes, respectively. 41 The percentage of displacement (I) by a site marker can be calculated as follows: 15…”

A simple and sensitive flow injection chemiluminescence immunoassay for chloramphenicol based on gold nanoparticle‐loaded enzyme

“…Chloramphenicol (CAP) was discovered in 1947, it is a highly efficient broad‐spectrum antibiotic, especially against Gram‐positive and Gram‐negative bacteria 1, 2 . However, many studies have shown that CAP administration produces many side effects in the human body, such as aplastic anaemia, leukaemia, grey infant syndrome, and so on 3, 4 . These results suggest that CAP residues in the food chain would cause food safety problems that could seriously harm human health 5–7 .…”