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(E)-2-[2-(4-甲氧苄基)肼基]-4-苯基噻唑与人血清蛋白的相互作用
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国家自然科学基金项目(21266024)


Interaction Between(E)-2-[2-(4-methoxybenzylidene) hydrazinyl]-4-phenylthiazole and Albumin Human
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    摘要:

    目的: 研究(E)-2-[2-(4-甲氧苄基)肼基]-4-苯基噻唑(MHP)与人血清蛋白(HSA)之间的相互作用,为揭示噻唑类衍生物与DNA作用的机制提供实验依据. 方法: 根据MHP与HSA相互作用的荧光敏化作用,利用Stern-Volmer方程,及非辐射能量转移理论处理实验数据,采用同步荧光光谱探讨了MHP对HSA构象的影响. 结果: 实验发现MHP可以使HSA的荧光增强,表明两者之间发生了能量转移,能量转移的机理是MHP与HSA结合形成了复合物.荧光增强(敏化)效应主要源于给体-受体间的偶极-偶极作用的能量转移. 结论: 能量转移的结果为内原发色基团的荧光被猝灭和外源发色基团荧光被敏化,计算得到其敏化常数为-2.620 8×104.同步荧光光谱表明,相互作用引起HSA构象变化,提示结合位点更接近于色氨酸.

    Abstract:

    Objective: The aim of this study was to investigate the interaction of (E)-2-[2-(4-methoxybenzylidene)hydrazinyl]-4-phenylthiazole(MHP) and human Albumin(HSA),in order to provide experimental basis for revealing the mechanism of interaction between MHP and HSA. Method: The impactof MHP on HSA conformation was investigated by using synchronous fluorescence spectroscopy, based on Stern-Volmer equation and the theory of non-radiative energy transferring. Result: The experiment result showed that MHP can lead to the enhancement of HSA fluorescence, indicating energy transferring between them. And the mechanism of energy transferring is that MHP and HSA formed complexes. Fluorescence enhancement (sensitization effect) mainly resulted from the-energy transferring of dipole-dipole effect between donor and receptor. Conclusion: The results of the energy transferring were the fluorescence quenching of endogenous chromophoric group, and the fluorescence sensitization of exogenous chromophoric group, and the sensitization constant was calculated as -2.620 8×104.Synchronous fluorescence spectra showed that the interaction between HSA and HA could cause the HSA conformation change, implying the binding sites closer to tryptophan.

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林枫,杨水兰,李明.(E)-2-[2-(4-甲氧苄基)肼基]-4-苯基噻唑与人血清蛋白的相互作用[J].中国实验方剂学杂志,2014,20(24):110~113

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  • 收稿日期:2014-04-24
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  • 在线发布日期: 2014-12-16
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