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Application of compound EPZ5676 and related inhibitor thereof in preparation of medicines for resisting cerebral ischemia diseases

EPZ5676, anti-cerebral ischemia technology, applied in the field of preparation of drugs for preventing or treating cerebral ischemic diseases, compounds and related inhibitors, can solve the problems that have not yet been seen in EPZ5676

Pending Publication Date: 2021-04-09
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But so far, there is no report on the role of EPZ5676 in cerebral ischemia

Method used

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  • Application of compound EPZ5676 and related inhibitor thereof in preparation of medicines for resisting cerebral ischemia diseases
  • Application of compound EPZ5676 and related inhibitor thereof in preparation of medicines for resisting cerebral ischemia diseases
  • Application of compound EPZ5676 and related inhibitor thereof in preparation of medicines for resisting cerebral ischemia diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 EPZ5676 Protective Effect Test on Primary Neuronal Cells Injured by OGD / R in Vitro

[0021] Grouping: The primary cultured cortical neuron cells were randomly divided into 5 groups, namely: 1) Sham group; 2) I / R group; 3) inhibitor 10 μM group; 4) inhibitor 20 μM group; 5) inhibitor 40 μM group . Inhibitors were administered for 4 hours in advance, followed by hypoxia and glucose deficiency for 2 hours, and reoxygenation for 4 hours to prepare an in vitro cerebral ischemia model. Collect proteins, detect p53, PARP1, caspase3, caspase9, Bax, Bcl-2, iNOS, COX-2, VCAM-1, ZO-1, Claudin-1 protein expression by Western blot method; climb slices, stain tunnel, Caspase3, iNOS, VCAM-1 indicators. The results showed that EPZ5676 could significantly reduce the expression of apoptosis indicators and inflammatory indicators; at the same time, it decreased the expression of inflammatory proteins and apoptotic proteins, and increased the expression of linker proteins.

[...

Embodiment 2

[0028] Example 2 Therapeutic effect of EPZ5676 on mouse cerebral ischemia model in vivo

[0029] Grouping: Male C57 mice weighing 21-24 g were anesthetized by intraperitoneal injection of 1% pentobarbital sodium and fixed in a supine position. The skin was opened in the middle of the neck and the incision was about 2 cm long. Bluntly dissect the subcutaneous tissue to expose the left common carotid artery (CCA), then dissect and expose the external carotid artery (ECA) and internal carotid artery (ICA) upwards sequentially, hang the thread at the distal end of the common carotid artery and external carotid artery, and slipknot The common carotid artery was ligated, the external carotid artery was ligated with a dead knot, and then the thread was hung on the distal end of the internal carotid artery and pulled with a retractor. Then hang the thread at the proximal end of the external carotid artery and tie a slipknot. Then, at the "Y-shaped" bifurcation of the external carotid...

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Abstract

The invention belongs to the field of pharmacy, relates to a new application of a compound EPZ5676 in pharmacy, and particularly relates to an application of a compound (C30H42N8O3) and a related inhibitor thereof in preparation of medicines for preventing or treating cerebral ischemia diseases. The result of the established mouse cerebral ischemia model and OGD / R-induced primary neuron cell in-vitro model experiment indicates that the EPZ5676 has a protective action on cerebral ischemia diseases by improving the behavioral symptoms of cerebral ischemia mice, reducing the cerebral infarction volume, inhibiting the expression of inflammatory proteins and apoptotic proteins and promoting the expression of linker proteins. The compound EPZ5676 can be used for preparing medicines for resisting cerebral ischemia, and provides a new direction for researching cerebral ischemia diseases.

Description

technical field [0001] The invention belongs to the field of pharmacy, relates to the new application of compound EPZ5676 in pharmacy, specifically relates to compound (C 30 h 42 N 8 o 3 ) and related inhibitors thereof in the preparation of drugs for the prevention or treatment of cerebral ischemic diseases. Background technique [0002] The prior art discloses that cerebral ischemia (also known as cerebral apoplexy) is one of the three major diseases that threaten human health, and has the characteristics of high prevalence, high recurrence rate, high disability rate, and high mortality rate. Surveys show that ischemic stroke accounts for 60% to 80% of cerebral apoplexy. However, there is still a lack of effective drugs for the treatment of ischemic stroke in clinical interventions; clinical practice shows that after cerebral ischemia, the ischemic area will swell and secrete a large amount of Inflammatory factors; because neurons are the most sensitive cells, a large ...

Claims

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Application Information

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IPC IPC(8): A61K31/7076A61P9/10
CPCA61K31/7076A61P9/10
Inventor 朱依谆刘新华王静欢
Owner FUDAN UNIV
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