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Citation: MA Guo-Zheng, TAN Fei, JIANG Yong-Jun, ZHENG Ke-Wen, GUO Ming, YU Qing-Sen. The Binding Mode of Pefloxacin Mesylate with Human Serum Albumin[J]. Acta Physico-Chimica Sinica, ;2005, 21(02): 123-127. doi: 10.3866/PKU.WHXB20050203 shu

The Binding Mode of Pefloxacin Mesylate with Human Serum Albumin

1.
Department of Chemistry, Zhejiang University, Hangzhou　310027;　Key Laboratory for Molecular Design and Nutrition Engineering of Ningbo City, Ningbo Institute of Technology, Zhejiang University, Ningbo　315100

Received Date: 8 June 2004
Available Online: 15 February 2005

This study was designed to explore the binding mode of pefloxacin mesylate(PFLX) with human serum albumin (HSA).Fluorescence spectroscopic results showed pefloxacin-HSA complex with binding constants of 1.7×10⁵ L•mol^－1.The enthalpy change (Δ_rH_m) and entropy change (Δ_rS_m) were measured by microcalorimetry to be 1.03 kJ•mol_－1 and 101.28 J•K_－1•mol_－1,which indicated that hydrophobic interaction played a major role in the binding of PFLX with HSA. The possible binding domains of HSA for PFLX were studied by molecular modeling, which predicted that the hydrophobic interaction played a dominating role in this drug-protein interaction and PFLX could bind to Sudlow’s sites I and II of HSA. The binding energies obtained from the molecular modeling were in accordance with the experiment results.
- Pefloxacin mesylate; Human serum albumin; Molecular modeling;　Binding mode
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