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Application of 2-APB in the preparation of anti-cerebrovascular drugs

A cerebrovascular disease, 1.2-APB technology, applied in the field of biomedicine, can solve the problem of lack of safe and effective treatment methods, and achieve the effect of reducing apoptosis

Inactive Publication Date: 2019-01-11
WUXI CHILDRENS HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is currently no safe and effective treatment

Method used

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  • Application of 2-APB in the preparation of anti-cerebrovascular drugs
  • Application of 2-APB in the preparation of anti-cerebrovascular drugs
  • Application of 2-APB in the preparation of anti-cerebrovascular drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Effects of 2-APB on Primary Rat Cortical Neurons

[0060] After the primary rat cortical neuron cells were cultured for 7 days, different concentrations of 2-APB were added (final concentrations were 1, 12.5, and 25 μM), and 0.1% DMSO was used as the normal control group (Control), and the cells were cultured under the same conditions. 2-24h. MTT assay showed that 2-APB had no toxic effect on primary rat cortical neurons in the concentration range of 1, 12.5, and 25 μM (see Figure 1).

Embodiment 2

[0061] Example 2: Effect of 2-APB on activity of primary rat cortical neurons after OGD / R injury

[0062] The rat cortical neuron cells cultured to the 7th-10th day were incubated with sugar-free Earle’s solution, and placed in a three-gas anoxic incubator at 37°C (1% O 2 , 5% CO 2 , 94%N 2 ) and cultivated for 30min, after taking it out, replace the whole medium with normal culture medium, and place it at 37°C, 5% CO 2 Continue culturing for 24 h in the incubator. 2-APB (final concentration of 1, 12.5, 25 μM), NBP (final concentration of 25 μM) and Eda (final concentration of 25 μM) were added 2 hours before OGD and maintained during the whole process of OGD / R. The solvent (0.1% DMSO) was used as the control, the normal control group (Control) was not treated with OGD / R, and the model control group (OGD / R) was also treated with OGD / R. Measure the corresponding indicators after the experiment.

[0063] Such as figure 2 As shown, compared with the Control group, after OG...

Embodiment 3

[0064] Example 3: 2-APB on NOX2, Rac1, p40 on the cell membrane of primary rat cortical neurons after OGD / R injury phox , p47 phox and p67 phox Effect on protein expression

[0065] The rat cortical neuron cells cultured to the 7th-10th day were incubated with sugar-free Earle's solution, and placed in a three-gas anoxic incubator (1% O2, 5% CO2, 94% N2) at 37 ° C for 30 min After taking it out, replace the whole medium with normal culture medium, and place it in a 37°C, 5% CO2 incubator to continue culturing for 24 hours. 2-APB (final concentration 25 μM) was added 2 hours before OGD and maintained throughout the OGD / R process. The solvent (0.1% DMSO) was used as the control, the normal control group (Control) was not treated with OGD / R, and the model control group (OGD / R) was also treated with OGD / R. Measure the corresponding indicators after the experiment. The result is as image 3 and Figure 4 As shown, OGD / R injury can induce NOX2, Rac1 and p40 in primary rat cor...

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Abstract

The invention provides an application of 2-APB in the preparation of anti-cerebrovascular drugs, which belongs to the field of biomedical technology. The present invention firstly studies the protective effect of 2-APB on ischemic stroke in a nerve cell oxygen-glucose deprivation model. The mechanism of 2-APB in decreasing neuronal death is related to the inhibition of oxidative stress and Wnt / Ca2 + signaling pathway. 2-APB has protective effect on ischemic neurons and can reduce brain damage in ischemic stroke patients. These results further supplement and enrich the relevant research of neuronal protection mechanism, and provide more scientific basis for the research and development of new drugs for the treatment of cerebral ischemia.

Description

technical field [0001] The present invention relates to the application of 2-aminoethoxydiphenyl borate (2-APB) in the preparation of anti-cerebrovascular disease drugs, in particular to the application of 2-APB in the preparation of anti-ischemic stroke drugs , belonging to the field of biomedical technology. Background technique [0002] Ischemic stroke is a common disease that seriously endangers human health and life safety worldwide, with high morbidity, disability and mortality. Patients who have suffered from cerebral apoplexy are prone to relapse, and every time there is a relapse, it gets worse. Clinically, there has been a lack of effective treatment measures, so it is very urgent and necessary to find new drugs and discover new treatment mechanisms. [0003] After cerebral ischemia, many mechanisms are involved in the process of brain tissue injury, such as oxidative stress injury, excitatory amino acid toxicity, mitochondrial dysfunction, and inflammatory respo...

Claims

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Application Information

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IPC IPC(8): A61K31/69A61P9/10A23L33/00
CPCA23L33/00A23V2002/00A61K31/69A61P9/10A23V2200/326
Inventor 凌菁菁平锋锋朱立红叶建林王燕洪远陈艳华朱扣柱姜辰周丹丽刘功莲
Owner WUXI CHILDRENS HOSPITAL
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