Application of axitinib and analogue in preparing anti-ischemic cerebral stroke medicine

A technology of axitinib and analogs, which is applied in the application field of axitinib and analogs in the preparation of anti-ischemic stroke drugs, can solve the problems of slow onset, limited therapeutic value, etc., and achieves safety High efficacy, convenient administration, and high application value

Inactive Publication Date: 2021-08-06
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, rhVEGF165 can only exert its curative effect after 48 hours of ischemia, and the onset of effec

Method used

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  • Application of axitinib and analogue in preparing anti-ischemic cerebral stroke medicine
  • Application of axitinib and analogue in preparing anti-ischemic cerebral stroke medicine
  • Application of axitinib and analogue in preparing anti-ischemic cerebral stroke medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 Axitinib Reverses the Apoptosis of Cerebral Microvascular Endothelial Cells under Oxygen and Glucose Deprivation Conditions

[0032] 1.1 Oxygen-glucose deprivation-induced vascular endothelial cell injury and drug regulation Taking mouse brain microvascular endothelial cells bEnd3 as the research object, using oxygen glucose deprivation (Oxygen Glucose Deprivation, OGD) to induce vascular endothelial cell injury as an in vitro model, simulating ischemic cerebral microvascular injury, and investigating the relevant indicators of vascular endothelial cells before and after ischemic injury expression changes. The specific method is as follows: when the cells were completely confluent, they were washed 3 times with sugar-free medium HBSS (Hank’s balance salt solution, HBSS) preheated to 37°C, and replaced with an appropriate volume of sugar-free medium for culture. That is, the cells were placed in a hypoxic airtight box, and anaerobic mixed gas (95% N 2 and 5%...

Embodiment 2

[0043] Example 2 Axitinib inhibits down-regulation of tight junction proteins in brain microvascular endothelial cells under oxygen-glucose deprivation conditions

[0044] The oxygen-glucose deprivation injury constructed by the method described in 1.1 of Example 1 was used as a model. The barrier function of the blood-brain barrier is mainly controlled by tight junction proteins Claudin-5 and Occludin on brain microvascular cells. Therefore, this patent mainly investigates the protective effect of axitinib administration on the tight junction protein damage of bEnd.3 cells induced by OGD.

[0045] 2.1 Western blot method to detect the expression of tight junction protein Claudin-5 in each treatment group

[0046] bEnd.3 cells at 2×10 5 The density per well was seeded on a 6-well plate. After 7 days of culture, axitinib was added at a dose of 400 ng / mL (dissolved in 2 μL of DMSO). Both the OGD group and the treatment group were treated with OGD for 8 hours, and the contro...

Embodiment 3

[0051] Example 3 Administration of axitinib restores blood-brain barrier function in rats with acute ischemic stroke

[0052] 3.1 Construction of animal model of middle cerebral artery occlusion and reperfusion in rats

[0053] Referring to the rat middle cerebral artery occlusion model and reperfusion (MCAO / R) model established based on the literature, the rat unilateral middle cerebral artery embolism model was prepared by suture method, resulting in focal ischemic cerebral infarction. stroke. Specifically, male adult Wistar rats with a body weight of 270-290 g were selected. 10% chloral hydrate 0.33ml / 100g intraperitoneal injection of anesthetized rats, the rats were fixed in the supine position, the skin was incised in the middle of the neck, each layer of tissue was bluntly separated, the right common carotid artery was exposed, and the external carotid artery and Internal carotid artery. Tie a slipknot at the proximal end of the common carotid artery. The common ca...

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Abstract

The invention discloses application of axitinib and analogues in preparing an anti-ischemic cerebral stroke medicine. According to the invention, the treatment effect of axitinib on ischemic cerebral stroke is evaluated, and it is found that axitinib can reduce the cerebral ischemia infarction volume of middle cerebral artery occlusion and reperfusion model rats, relieve cerebral edema and improve dyskinesia; and axitinib can also slow down the apoptosis state of bEnd.3 cerebrovascular cells under the oxygen-glucose deprivation condition. Therefore, the axitinib and the analogue thereof can be used for preparing the anti-ischemic cerebral stroke medicine.

Description

technical field [0001] The invention belongs to the field of biotechnology, and specifically relates to the application of axitinib and analogues in the preparation of anti-ischemic stroke drugs. Background technique [0002] According to the 2016 Global Burden of Disease Research data released by the journal "Lancet Neurology", stroke is the second leading cause of death (5.5 million) in the world, and the number of stroke patients worldwide is 80.1 million. Of the two major categories of stroke (ischemic and hemorrhagic), ischemic stroke accounts for 87% of all stroke-related events. Ischemic stroke is necrosis that occurs when part of the brain tissue is deprived of oxygen and glucose supply due to a blood vessel being blocked by a thrombus or embolism. [0003] A series of pathophysiological pathways occur in the early stage (0-48h) of ischemic stroke, including angioedema, leakage of the blood-brain barrier, potential hemorrhagic transformation, astrocyte damage and ne...

Claims

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Application Information

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IPC IPC(8): A61K31/454A61P9/10
CPCA61K31/454A61P9/10
Inventor 胡富强王凯袁弘孟廷廷金翔宇周文韬
Owner ZHEJIANG UNIV
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