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Binding of esketamine to human serum albumin for clinical implications

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Abstract

The interaction of the newly approved pharmacon esketamine with HSA (human serum albumin) has been investigated by various spectrographic methods. The fluorescence quenching results of HSA by esketamine revealed that the 1:1 ground state complex has formed. The results of binding parameters lead to the conclusion that the reaction was exothermic. In the presence of esketamine, HSA was found to undergo partial unfolding, and thermodynamic parameters (ΔG° = − 2.08 × 104 J·mol−1, ΔS° = 35.7 J·mol−1·K−1, and ΔH° = − 1.20 × 104 J·mol−1 at 298 K) revealed that electrostatic forces dominated the stabilization of the complex. The qualitative and quantitative analyses of conformational changes of HSA were conducted using circular dichroism, three-dimensional, and synchronous fluorescence spectroscopy, revealing the loosening of skeleton structure and adaptive modifications of secondary structures. Fe3+ and Mg2+ may help prolong the storage time and improve the drug efficacy.

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Author notes

  1. Yan Li and Fengqiang Sun have contributed equally to this work.

Authors and Affiliations

  1. Department of Anesthesiology, Yantaishan Hospital, Yantai, 264000, China

    Yan Li, Wei Shao & Yulin Zhu

  2. Department of Anesthesiology, Haiyang People’s Hospital, Yantai, 265100, China

    Fengqiang Sun

  3. Department of Anesthesiology, Cheeloo College of Medicine, Shandong University, Jinan, 250100, China

    Jingui Yu

  4. Department of Pain, Central Hospital of Jinan Affiliated to the First Medical University of Shandong, Jinan, 250000, China

    Lingzhi Yu

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  1. Yan Li
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  2. Fengqiang Sun
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  3. Jingui Yu
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  4. Lingzhi Yu
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  5. Wei Shao
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  6. Yulin Zhu
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Correspondence to Yulin Zhu.

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Li, Y., Sun, F., Yu, J. et al. Binding of esketamine to human serum albumin for clinical implications. J Incl Phenom Macrocycl Chem 101, 101–109 (2021). https://doi.org/10.1007/s10847-021-01090-6

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  • DOI: https://doi.org/10.1007/s10847-021-01090-6

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