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A kind of agonist of adenylate-activated protein kinase and its application

A technology of gingerol and blood vessels, applied in the field of agonists of adenylate-activated protein kinase, to achieve the effects of inhibiting vascular stenosis, inhibiting proliferation, and enhancing activity

Active Publication Date: 2021-08-24
THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dried ginger extract has the effects of lowering blood sugar, lowering blood fat, and anti-atherosclerosis, but there is no report that 10-gingerol prevents and treats vascular restenosis, and there is no report that 10-gingerol is an AMPK agonist or can activate AMPK.

Method used

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  • A kind of agonist of adenylate-activated protein kinase and its application
  • A kind of agonist of adenylate-activated protein kinase and its application
  • A kind of agonist of adenylate-activated protein kinase and its application

Examples

Experimental program
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Effect test

Embodiment 11

[0029] Example 1 10-gingerol can inhibit vascular stenosis induced by ligation of common carotid artery

[0030] The inventors adopted a mouse model of ligation of the left common carotid artery. The mice were anesthetized by intraperitoneal injection, the mouse was fixed, the skin was cut along the middle of the mouse neck, the subcutaneous tissue and fat were bluntly separated with microscopic curved forceps, and the thyroid gland and muscle were separated under a microscope to expose the left common carotid artery. The bifurcation of the external carotid artery and the internal carotid artery was ligated with No. 6 sterile braided suture. 4 weeks after carotid artery ligation, neointimal hyperplasia in mice was observed, and blood vessel tissues were isolated from the sham operation group, model group, low dose (25 mg / kg) and high dose (50 mg / kg) groups and made into eosin-stained images. Artery slices.

[0031] Morphological analysis showed that after 4 weeks of ligation...

experiment example 210

[0032] Experimental example 2 10-gingerol can inhibit the proliferation of vascular smooth muscle cells

[0033] Two kinds of vascular smooth muscle cells were selected, namely rat thoracic artery smooth muscle cells A7r5 and human aortic smooth muscle cells HASMC. Two kinds of VSMCs (A7r5 and HASMC cells) were treated with drug 10-gingerol concentration gradient (1 μM, 3 μM, 10 μM) respectively, incubated for 24 hours, and a normal control group (0.1% DMSO) was set up at the same time, and the MTS method (cell viability assay) was used The proliferation of VSMCs was detected (Number of cases=6).

[0034] The result is as figure 2 A-B shows that in VSMCs (A7r5 and HASMC), compared with the control group, the cell activity of the drug treatment group is lower, and has a certain concentration dependence, that is, the difference between the middle and high dose groups of A7r5 cells is statistically significant (P figure 2 The results indicated that 10-gingerol could inhibit the...

experiment example 310

[0035] Experimental example 3 10-gingerol can activate AMPKα

[0036] VSMCs (A7r5 and HASMC cells) were treated with different concentrations of 10-gingerol (1 μM, 3 μM, 10 μM), and after incubation for 24 h, p-AMPKα was detected by Western blot (rabbit anti-p-AMPKα antibody was purchased from CST Company, 1:1000 ), AMPKα (rabbit anti-p-AMPKα antibody was purchased from CST Company, 1:1000) and GAPDH (rabbit anti-GAPDH antibody was purchased from Abcam Company, 1:5000) (case number = 3).

[0037] The result is as image 3 As shown, 10-gingerol can dose-dependently increase the phosphorylation level of AMPKα, and the difference is statistically significant (P<0.05); the above results suggest that 10-gingerol can activate AMPKα in a concentration-dependent manner.

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Abstract

The invention discloses an agonist of adenylate-activated protein kinase, and the agonist is 10-gingerol; the invention also discloses the application of 10-gingerol in the preparation of drugs for preventing and treating vascular restenosis. The inventors of the present application found that 10-gingerol can enhance the activity of AMPK, effectively inhibit the proliferation of vascular smooth muscle cells, and inhibit the vascular stenosis induced by ligation of the carotid artery. In addition, the inventors of the present application also found that 10-gingerol can be sterically combined with AMPK, and is a natural AMPK agonist.

Description

technical field [0001] The invention relates to a kinase agonist, in particular to an adenylate-activated protein kinase agonist and application thereof. Background technique [0002] Coronary atherosclerotic heart disease is mainly due to coronary atherosclerosis, lipid deposition on the blood vessel wall causes coronary artery stenosis or blockage, resulting in myocardial ischemia and insufficient oxygen supply. Percutaneous transluminal angioplasty (PTA) uses bulbar fillings to expand occluded or narrow blood vessels, which can improve myocardial blood perfusion, and can quickly and effectively relieve the condition. effective treatment for cardiovascular disease. Among them, transluminal coronary angioplasty (PTCA) has been widely used in the treatment of coronary heart disease. After more than 20 years of development, PTA technology has achieved remarkable results in improving the success rate and reducing acute complications. [0003] However, the long-term outcome ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/12A61P9/10A61L31/08A61L31/16
CPCA61K31/12A61L31/08A61L31/16A61L2300/216A61L2300/416A61P9/10
Inventor 刘彬刘世明张竞之刘宁宁邓波江小梨
Owner THE SECOND AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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