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Insights into the interaction mechanism between tiagabine hydrochloride and two serum albumins

机译：盐酸三滨与两种血清白化素之间的相互作用机制见解

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摘要

Tiagabine hydrochloride (TGB) is a widely used anticonvulsive drug for the treatment of epilepsy. To better understand the interactions of TGB with plasma proteins, human serum albumin (HSA) and bovine serum albumin (BSA) were selected as model proteins. TGB slightly increased thermal stability of the proteins as confirmed by VP-capillary differential scanning calorimetric (DSC) measurements. Isothermal titration calorimeter (ITC) results showed that TGB could be combined with HSA and BSA moderately, which was also corroborated by fluorescence analysis. Besides, the thermodynamic parameters (H 0, S 0) indicated that hydrophobic forces played a major role in the formulation of TGB-HSA and TGB-BSA complexes. Moreover, the main binding sites of TGB to HSA and BSA were also examined by classical fluorescent probe (dansylsarcosine and dansylamide) experiments, showing that TGB and dansylsarcosine competitively interacted with HSA and BSA at the same binding sites. Additionally, TGB had no obvious effect on the conformation change of HSA and BSA as indicated by spectroscopic analyses. This study provides useful information about the interaction mechanism of TGB and serum albumins, which could help to better utilize TGB in biomedical field.
机译：盐酸噻吩（TGB）是一种广泛使用的抗菌药，用于治疗癫痫。为了更好地理解TGB与血浆蛋白的相互作用，选择人血清白蛋白（HSA）和牛血清白蛋白（BSA）作为模型蛋白质。 TGB通过VP-毛细管差示扫描量热（DSC）测量确认的蛋白质的热稳定性略微增加。等温滴定量热计（ITC）结果表明，TGB可适度地与HSA和BSA组合，这也通过荧光分析证实。此外，热力学参数（H＆GT; 0，S> 0）表明疏水力在TGB-HSA和TGB-BSA配合物的配方中发挥了重要作用。此外，还通过经典的荧光探针（丹曲霉素和丹酰胺）实验检查了TGB至HSA和BSA的主要结合位点，表明TGB和丹曲霉在相同的结合位点处与HSA和BSA竞争地相传性地相互作用。此外，TGB对SPSA和BSA的构象变化没有明显的影响，如光谱分析所示。本研究提供了有关TGB和血清白化素的相互作用机制的有用信息，这可能有助于更好地利用生物医学领域的TGB。

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  • 来源
    《RSC Advances》 |2018年第44期|共8页
  • 作者

    Zhuo Weiling; Peng Xilin; Lin Xiang;

  • 作者单位

    Sichuan Univ Sch Chem Engn Chengdu 610065 Sichuan Peoples R China;

    Sinopharm Chuankang Pharmaceut Co Ltd Chengdu 611731 Sichuan Peoples R China;

    Sichuan Univ Sch Chem Engn Chengdu 610065 Sichuan Peoples R China;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
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