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Application of compound in preparation of antithrombotic drugs

An anti-thrombotic drug and anti-platelet drug technology, applied in the field of medicine, can solve problems such as bleeding, and achieve the effects of inhibiting thrombosis, safe use, and reducing ischemic brain damage

Active Publication Date: 2022-04-29
THE FIRST AFFILIATED HOSPITAL OF GUANGXI MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aspirin and clopidogrel, which are recommended by many guidelines, also have "aspirin resistance" and "clopidogrel resistance". In addition, the existing antiplatelet drugs also have side effects such as bleeding

Method used

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  • Application of compound in preparation of antithrombotic drugs
  • Application of compound in preparation of antithrombotic drugs
  • Application of compound in preparation of antithrombotic drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0031] Experimental Materials:

[0032] The Col003 we used was purchased from MCE (MedChemExpress) company, the article number is HY-124817. Use 20% sulfobutyl-β-cyclodextrin (SBE-β-CD) co-solvent, product number HY-17031.

[0033] Rat MCAO model was used: healthy adult male Sprague-Dawley (SD) rats, clean grade (body weight 280 to 320 g), provided by the Experimental Animal Center of Guangxi Medical University.

[0034] Experiment 1 Confirmed the expression of HSP47 on the peripheral blood platelet membrane of rats

[0035] The rats were anesthetized by intraperitoneal injection of 10% chloral hydrate (0.3ml / 100g), and a midline incision was made in the neck, the thyroid gland was bluntly dissected, and the right common carotid artery, external carotid artery and internal carotid artery were separated. The thread embolus enters the internal carotid artery through the bifurcation of the common carotid artery, enters the cranium to the origin of the middle cerebral artery, an...

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Abstract

The invention relates to the technical field of medicines, in particular to application of a compound in preparation of antithrombotic drugs. At present, in the preclinical research of new anti-platelet drugs, hemostasis is more and more emphasized while thrombus formation is inhibited. In tMCAO, a receptor GPIb or GPVI which plays a role in the early stage of platelet activation can relieve ischemic brain injury of a mouse, and bleeding complications cannot be increased, so that intervention in the early stage of platelet activation is effective and safer. The compound Col003 is obtained by degrading a natural compound molecule AK778 in a culture medium or a buffer solution, can play an anti-platelet role in the early stage of platelet activation, can inhibit the formation of thrombus, does not affect the blood coagulation function, is relatively weak in cytotoxicity, and is expected to become an effective and safe therapeutic drug for cerebral arterial thrombosis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the application of a compound in the preparation of antithrombotic drugs. Background technique [0002] "Stroke" (cerebral stroke) is also known as "stroke" and "cerebrovascular accident" (cerebralvascularaccident, CVA). It is an acute cerebrovascular disease, which is a group of diseases that cause brain tissue damage due to sudden rupture of blood vessels in the brain or obstruction of blood circulation in the brain, including ischemic and hemorrhagic stroke. The incidence of ischemic stroke is higher than that of hemorrhagic stroke, accounting for 60% to 70% of the total number of strokes. The age of onset is more than 40 years old, and there are more men than women. Severe cases can cause death. [0003] Drugs commonly used in clinical treatment of ischemic stroke include ultra-early thrombolytic drugs, drugs that inhibit platelet aggregation, anticoagulant drugs, neuroprot...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61P7/02A61P9/10
CPCA61K31/11A61P7/02A61P9/10
Inventor 刘竞丽吴双梁程伟李劲频谢晓云黄海萍傅金凤王辞岚邓梦雨
Owner THE FIRST AFFILIATED HOSPITAL OF GUANGXI MEDICAL UNIV
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