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Histone deacetylase fluorescence probe, and preparation method and applications thereof

A deacetylase and fluorescent probe technology, applied in the field of biochemistry, to achieve the effects of fast response rate, good clinical application value and high sensitivity

Active Publication Date: 2018-06-29
湖南融健生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, it is still a challenge to develop a simple and effective fluorescent probe to detect the activity of HDACs.

Method used

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  • Histone deacetylase fluorescence probe, and preparation method and applications thereof
  • Histone deacetylase fluorescence probe, and preparation method and applications thereof
  • Histone deacetylase fluorescence probe, and preparation method and applications thereof

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Embodiment 1

[0041] (1) A method for preparing a fluorescent probe for histone deacetylase comprises the following steps:

[0042] (1) Synthesis of Compound 1

[0043]

[0044] Measure 6.4mL of 40% dimethylamine aqueous solution into a 100mL rear wall pressure-resistant sealed tube, then add 3.5g of sodium metabisulfite and 1.93g of 6-bromo-2-naphthol, and add 30mL of water, stir well, and put the thick-walled resistant Place the pressure tube at 150°C under heating conditions and stir for 72 hours. After the reaction is completed, cool to room temperature, collect the filter cake by filtration, wash the filter cake with deionized water until neutral, and purify the crude product by column chromatography [V (petroleum ether) : V(dichloromethane)=3:1] to obtain compound 1 (2.18g, yield 87.3%). 1 HNMR (400MHz, CDCl 3 )δ (ppm): 7.81 (1H, s, Ar-H), 7.59 (1H, d, J = 8.8Hz, Ar-H), 7.52 (1H, d, J = 8.0Hz, Ar-H), 7.41 (1H,d,J=8.0Hz,Ar-H),7.15(1H,dd,J 1 =2.0Hz,J 2 =8.8Hz, Ar-H), 6.85(1H, d, J...

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Abstract

The invention provides a histone deacetylase fluorescence probe, and a preparation method and applications thereof. The structure formula of the histone deacetylase fluorescence probe is disclosed inthe invention. In synthesis, 6-(dimethylamino)-2-naphthaldehyde with two-photon effect is selected as a dye, so that further nucleophilic reaction is realized after deacetylation reaction, and fluorescence signals are generated; aldehyde group carbon is modified into cyanogroup alcohol structures, hydroxyl is connected with HDACs responsive groups, and the histone deacetylase fluorescence probe isused for detecting and imaging of the activity of histone deacetylase in tissue. According to the histone deacetylase fluorescence probe, cyanogroup with excellent electron-withdrawing capability isintroduced, so that after response of HDACs with the histone deacetylase fluorescence probe, intramolecular cyclization reaction is carried out rapidly, activation of fluorescence signals is realized,detecting and imaging on histone deacetylase in living cells and tissue are realized, and excellent clinical application value is achieved.

Description

technical field [0001] The invention belongs to the field of biochemistry, and in particular relates to a histone deacetylase fluorescent probe and a preparation method and application thereof. Background technique [0002] Post-transcriptional modifications of nuclear histone acetylation, methylation, and phosphorylation play key regulatory roles in chromatin structure and gene expression. Acetylation of histones is reversible and is controlled by histone acetyltransferases (HATs) and histone deacetylases (HDACs). HDACs can hydrolyze the acetyl group on acetylated lysine to obtain positively charged lysine. At the same time, HDACs are closely related to gene expression. Studies have shown that the deacetylation of HDACs changes the electrical state of histone ends and enhances the interaction with DNA, thus making the chromatin structure more stable. In addition, HDACs have been found to be associated with certain diseases such as cancer and mental disorders, and even lea...

Claims

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Application Information

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IPC IPC(8): C07C253/30C07C255/43C09K11/06G01N21/64
CPCC07C209/18C07C221/00C07C253/00C07C253/30C07C255/43C09K11/06C09K2211/1011G01N21/6428G01N21/6486C07C223/06C07C211/59
Inventor 蒋健晖汪凤林刘贤军罗凤焱唐丽娟
Owner 湖南融健生物科技有限公司
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