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Agonist of deacetylase and application thereof

A deacetylase and agonist technology, applied in the field of medicine, can solve the problems of not studying the protein targets of cinnamic aldehyde structural analogs and cinnamaldehyde derivatives, and the lack of in-depth research on the protein targets of cinnamaldehyde.

Inactive Publication Date: 2020-10-30
GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most studies have focused on drug efficacy evaluation, cell molecular phenotype changes, and classic pathways, and have not studied in depth the specific protein targets of cinnamic aldehyde in animals or humans, nor have they studied cinnamic aldehyde structural analogs and cinnamic aldehyde. Specific protein targets of derivatives in animals or humans;

Method used

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  • Agonist of deacetylase and application thereof
  • Agonist of deacetylase and application thereof
  • Agonist of deacetylase and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] This example uses the Target Hunter software to predict the binding of cinnamic aldehyde to the target protein in vivo

[0041] Prediction results: if figure 1 As shown, according to the 3D structure of the small molecule of cinnamon aldehyde, the Target Hunter software combines CVDPlatform to predict the protein target of cinnamic aldehyde binding in vivo, and selects the top 5 proteins according to the p-value, among which 3 prediction results show that cinnamon aldehyde and histone deacetylation There is a strong binding effect on deacetylase 6, 8 or histone deacetylase.

Embodiment 2

[0043] This example is a study of the effect of cinnamaldehyde on the HDAC activity of endothelial cells induced by high glucose

[0044] 1. Cell culture

[0045] Inoculate HUVEC in human umbilical vein endothelial cell culture medium containing 10% fetal bovine serum and 100 U / ml double antibody, and place at 37°C, 5% CO 2 Culture in an incubator, digest and subculture when the cells are cultured to 80%-90%.

[0046] 2. Drugs and main reagents

[0047] Cinnamaldehyde (Trans-cinnamaldehyde, TCA) was purchased from Sigma-Aldrich Company (China, Shanghai); Dimethylsulfoxide (DMSO) was purchased from Sigma-Aldrich Company (China, Shanghai); glucose (D(+)- Glucose), purchased from Sigma-Aldrich Company (China, Shanghai); human umbilical vein endothelial medium, purchased from Beijing Yuhengfeng Company (China, Beijing).

[0048] 3. Experimental method

[0049] 1. Cell grouping and high-glucose modeling: the cells were divided into 3 groups, normal control group (control), high...

Embodiment 3

[0059] This example is a study of the agonistic effect of cinnamic aldehyde on HDAC6 activity

[0060] One, cell culture: with embodiment 2.

[0061] Two, medicines and main reagents: with embodiment 2.

[0062] 3. Experimental method

[0063] HDAC6 activity kit detection (Enzo Life Sciences, BML-AK516): the kit uses the FluordeLys system (fluorescent histone deacetylase lysine substrate / developer), which can be used for specific histone deacetylase 6 detection . The assay process is divided into two steps, first, the SIRT1 substrate containing acetylated lysine side chain is incubated with HDAC6, the deacetylation of the substrate will make the substrate sensitive, in the second step, it is treated with the developer Fluorophores are produced. The operation steps are as follows:

[0064] 1) Make cinnamon aldehyde into different final concentrations according to the gradient: 10 μ TCA (diluted with DMSO, diluted with Buffer in the last step) is added to 140 μ mixed soluti...

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Abstract

The invention relates to an agonist of deacetylase and application thereof, and belongs to the technical field of medicines. The agonist of deacetylase comprises cinnamyl aldehyde, cinnamyl aldehyde structural analogues or cinnamyl aldehyde derivatives, wherein the cinnamyl aldehyde structural analogues comprises phenylpropionaldehyde, phenylacetaldehyde, benzaldehyde, propionaldehyde, acetaldehyde or formaldehyde; the cinnamyl aldehyde derivatives comprise alpha-bromo cinnamaldehyde, alpha-bromo p-chloro cinnamaldehyde, alpha-bromo p-methyl cinnamaldehyde, alpha-methyl cinnamaldehyde, alpha-hexylcinnamaldehyde, 4-chloro cinnamaldehyde, 4-methoxy cinnamaldehyde, 4-fluoro cinnamaldehyde, 2-nitro cinnamaldehyde and p-chloro cinnamaldehyde. The regulation effect of an ARG-NO pathway in a high-glucose induced endothelial cell injury model proves that the agonist of the deacetylase has a protective effect on vascular endothelial injury as an agonist of HDAC.

Description

technical field [0001] The invention relates to a sirtuin agonist and application thereof, belonging to the technical field of medicine. Background technique [0002] Histone deacetylase (HDAC) is a kind of protease related to epigenetic modification. In human body, it can make chromatin compact, inhibit mRNA synthesis, or play translation by regulating transcription factors, proto-oncogenes and signal mediators. Post-modification, regulation of cellular homeostasis. At present, the HDAC family is divided into four categories, including a total of 18 subtypes, and the biological functions of each specific subtype are different. HDAC currently mainly participates in physiological and pathological processes through two regulatory mechanisms. One is the regulation of histone acetylation level: in the nucleus, HDAC acts by converting the acetyl group of acetyl-CoA from a specific lysine at the amino terminal of histone Residues are removed to complete deacetylation of histones...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61K31/115A61P3/10A61P9/14
CPCA61K31/11A61K31/115A61P3/10A61P9/14
Inventor 姚琳陈永君卢甜古江勇夏宇岑陈心怡程红郑媛嘉
Owner GUANGZHOU UNIVERSITY OF CHINESE MEDICINE
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