| 常鹏飞,谢宪,喻凯荔,吴啸宇,林翠梧.化学通报,2015,78(7):613-620. |
| 染料木素磺化衍生物的合成及其与人血清白蛋白作用的研究 |
| Study on the Synthesis of Genistein Sulfonated Derivatives and their Interaction with Human Serum Albumin |
| 投稿时间：2014-11-27 修订日期：2014-12-23 |
| DOI： |
| 中文关键词: 染料木素 磺化衍生物 人血清白蛋白(HSA) 紫外-可见吸收光谱 荧光光谱 |
| 英文关键词:genistein, sulfonated derivatives, human serum albumin(HSA), UV-Vis spectrum, fluorescent spectrum |
| 基金项目:国家自然科学基金项目; 广西自然科学基金重点项目; 广西大学“大学生创新创业训练计划”项目 |
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| 中文摘要: |
| 本文以染料木素为原料,利用Mannich反应,设计合成了其与胺(正丁胺、异丙胺、二乙胺)的Mannich碱衍生物,再进一步磺化,从而制得三个未见文献报道的磺化衍生物(GSD),对其结构进行ESI-MS、1H-NMR、13C-NMR表征。应用荧光光谱、紫外-可见吸收光谱方法对三个磺化衍生物(GSD)与人血清白蛋白(HSA)的相互作用机制进行了研究。荧光光谱检测结果表明,GSD与HSA结合并引起其内源荧光的猝灭,该猝灭过程以静态猝灭为主。根据热力学参数确定了该结合主要是通过氢键和范德华力,是一个自发的放热过程。同时,根据紫外-可见吸收光谱及同步荧光光谱探讨二者结合后HSA的构象改变。本研究为GSD作为药物先导在血液中的运输及传递提供理论支持。 |
| 英文摘要: |
| Three novel genistein sulfonated derivatives (GSD) which derived from genistein, amines (n-butylamine, isopropylamine and diethylamine) and sulfuric acid were synthesized and characterized by ESI-MS、1H-NMR and 13C-NMR. The interaction between GSD and human serum albumin (HSA) was studied using UV-Vis absorption spectroscopy and fluorescence spectroscopy. The experimental results indicated that GSD effectively quenched the intrinsic fluorescence of HSA via a static quenching process. The thermodynamic parameters showed that hydrogen bonding and van der Waal’s forces were the predominant intermolecular forces between GSD and HSA. And it is a spontaneous exothermic process. In addition, the effect of GSD on the conformation of HSA was investigated via UV-Vis and synchronous fluorescence spectroscopy. A theoretical support was given by this study for the GSD which as drug leads were transported and transferred in the blood. |
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