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他莫昔芬与β-乳球蛋白的结合机制研究

Study on the mechanism of binding of tamoxifen and β-lactoglobulin

    摘要
  • 摘要:
    目的 探讨β-乳球蛋白（BLG）作为他莫昔芬载体的可能性。
    方法 采用光谱技术，研究β-乳球蛋白与他莫昔芬的结合机理。
    结果 他莫昔芬可以导致BLG发生荧光猝灭，其Kq值远高于动态猝灭常数的最大Kq值（2.0×1010 mol/（L·s），在不同pH值条件下猝灭常数值是不同的，热力学参数△H和△S值均大于0。BLG可与他莫昔芬结合形成BLG-他莫昔芬复合物，其吸热过程以疏水力为主要作用力。他莫昔芬与BLG在酸性和碱性条件下具有不同的结合模式，这主要取决于BLG的EF环的开闭状态。
    结论 BLG具有结合他莫昔芬的能力，显示了BLG作为难溶性药物载体的潜在价值。

     

    Abstract:
    Objective To explore the possibility of β-lactoglobulin (BLG) as carrier of tamoxifen.
    Methods The binding mechanism of BLG and tamoxifen was studied by spectroscopic technique.
    Results Tamoxifen would lead to the fluorescence quenching of BLG, and its Kq value was much higher than the maximal Kq value of the dynamic quenching constant (2.0×1010 mol/(L·s). The quenching constant values were different under different pH values, and the values of thermodynamic parameters △H and △S were greater than 0. BLG can be combined with tamoxifen to form BLG-tamoxifen complex, and the endothermic process took hydrophobic force as the main force. Tamoxifen and BLG had different binding patterns under acidic and alkaline conditions, which mainly depended on the opening and closing state of the EF ring of BLG.
    Conclusion BLG has the ability to bind tamoxifen, which shows the potential value of BLG as a carrier of insoluble drugs.

     

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