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亚甲蓝类似物的合成及其与牛血清白蛋白相互作用的研究

景姣姣 刘彬 刘阳 高博 李倩玉 许明玲 何玲玲 王新

药学研究2017,Vol.36Issue(3):125-131,7.
药学研究2017,Vol.36Issue(3):125-131,7.DOI:10.13506/j.cnki.jpr.2017.03.001

亚甲蓝类似物的合成及其与牛血清白蛋白相互作用的研究

Synthesis of methylene blue derivants and their interaction with bovine serum albumin

景姣姣 1刘彬 1刘阳 2高博 3李倩玉 1许明玲 1何玲玲 1王新1

作者信息

  • 1. 辽宁大学药学院,辽宁 沈阳110036
  • 2. 辽宁省天然产物制药工程技术研究中心,辽宁 沈阳110036
  • 3. 辽宁省新药研发重点实验室,辽宁 沈阳110036
  • 折叠

摘要

Abstract

Objective To synthesize a series of methylene blue derivants,N3,N3,N7,N7-Tetra-n-propyl-3,7-diaminophenothiazin-5-ium iodide,N3,N3,N7,N7-Tetra-n-butyl-3,7-diaminophenothiazin-5-ium iodide and N3,N3,N7,N7-Tetra-n-pentyl-3,7-diaminophenothiazin-5-ium iodide,and study the interactions between these methylene blue derivants and bovine serum albumin(BSA) under physiological condition.Methods These compounds were characterized by means of MS and 1H-NMR,and the interactions between these methylene blue derivants and bovine serum albumin(BSA) under physiological condition were studied using fluorescence spectroscopy.Results The fluorescence of BSA was quenched remarkably by these methylene blue derivants due to the formation of complexes,Gibbs free energy change(ΔG0) was negative.The binding distance between the tryptophan residue of BSA and these methylene blue derivants was less than 7 nm.Conclusion The fluorescence quenching mechanisms of BSA by these methylene blue derivants were considered as static quenching,the binding process was a spontaneous process and the energy transfer from the tryptophan residue of BSA to these methylene blue derivants can occur according to the Frster non-radioactive resonance energy transfer theory.In addition,the results of synchronous fluorescence spectra and three-dimensional fluorescence spectra showed that interaction between the methylene blue derivants and BSA can induce conformational changes in BSA.

关键词

亚甲蓝类似物/牛血清白蛋白/荧光光谱

Key words

Methylene blue derivants/Bovine serum albumin/Fluorescence spectrum

分类

医药卫生

引用本文复制引用

景姣姣,刘彬,刘阳,高博,李倩玉,许明玲,何玲玲,王新..亚甲蓝类似物的合成及其与牛血清白蛋白相互作用的研究[J].药学研究,2017,36(3):125-131,7.

基金项目

国家自然科学基金(No.21402125) (No.21402125)

辽宁省教育厅科学研究项目(No.L2016008) (No.L2016008)

药学研究

2095-5375

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