Use of lometaxel in the preparation of a medicament for the treatment of neurological injury caused by cerebral apoplexy

A technique for lomitapide and nerve injury, which is applied in the field of medicine and can solve problems such as little effect

Active Publication Date: 2022-07-05
XUANWU HOSPITAL OF CAPITAL UNIV OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the past two decades, many countries in the world have invested a lot of manpower and material resources in the basic research of cerebrovascular diseases, but with little effect, and the neuroprotection and prevention strategies need to be further strengthened

Method used

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  • Use of lometaxel in the preparation of a medicament for the treatment of neurological injury caused by cerebral apoplexy
  • Use of lometaxel in the preparation of a medicament for the treatment of neurological injury caused by cerebral apoplexy
  • Use of lometaxel in the preparation of a medicament for the treatment of neurological injury caused by cerebral apoplexy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1. Using the cellular OGD model to investigate the protective effect of lometta on neurons

[0039] Subjects: The SH-SY5Y neuroblastoma cell line used in the in vitro experiments was derived from ATCC and preserved by the Cerebrovascular Disease Laboratory, Xuanwu Hospital, Capital Medical University; primary cortical neurons were obtained from C57BL / 6J at 16-18 days of gestation Mice, the cleaning grade is SPF grade, and the pregnant mice used in this study were provided by Beijing Weitong Lihua Laboratory Animal Technology Co., Ltd.

[0040] Establishment of cellular glucose and oxygen deprivation (OGD) model: The cellular glucose and oxygen deprivation model is a commonly used cell model to verify the effect of drugs on ischemic stroke. The cells were cultured in a 96-well plate. After the cells adhered to the wall, the cells were washed twice with PBS to remove the residual sugar in the plate. After adding sugar-free medium, they were placed in a closed box,...

Embodiment 2

[0053] Example 2. Using the mouse MCAO model to investigate the neuroprotective effect of lometaxel

[0054] Subjects: The in vivo experiment part of this study took healthy adult C57BL / 6J male mice as the research objects. The mice were 12-14 weeks old, weighing 21-23 g, and the cleaning grade was Specific pathogen Free (SPF). class). All experimental animals were provided by Beijing Weitong Lihua Laboratory Animal Technology Co., Ltd.

[0055] Lometapide dosing regimen: 0.5 mg / kg for C57BL / 6J male mice, administered immediately after ischemia-reperfusion, once a day for 14 days, the drug was dissolved in DMSO solution to prepare a high-concentration stock solution for storage, mice For intragastric administration, normal saline is diluted to the desired concentration.

[0056] Mouse middle cerebral artery occlusion model (MCAO): The mouse middle cerebral artery occlusion model is a commonly used animal model to verify the effect of drugs on ischemic stroke. After the mice...

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Abstract

The present invention provides the pharmaceutical use of lometaxel. For: the application of lometaxel in the preparation of the following 1)-4) products: 1) a drug for preventing and / or treating ischemic cerebrovascular disease; 2) a drug for preventing and / or treating stroke; 3) using Neuroprotective medicine for ischemic cerebrovascular disease; 4) nerve repairing medicine for ischemic cerebrovascular disease; the present invention shows through experiments that lometaxel causes nerve damage caused by stroke, especially ischemic stroke Has excellent therapeutic effect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the use of lometapaide in the preparation of a medicament for treating nerve damage caused by cerebral apoplexy. Background technique [0002] Lometopide, approved by the U.S. Food and Drug Administration (FDA) in 2012 for the treatment of homozygous familial hypercholesterolemia, works by inhibiting the activity of microsomal triglyceride transfer protein inhibitors, thereby preventing apolipoprotein The assembly of B(apoB) in intestinal epithelial cells and hepatocytes inhibits the synthesis of chylomicrons and very low-density lipoprotein, thereby reducing plasma low-density lipoprotein cholesterol (LDL-C) levels. However, there are no reports or patents on its activity in the treatment of nerve damage caused by ischemic cerebrovascular disease. Therefore, on this basis, we continue to study the new uses of lomitapide and expand its application fields. [0003] Cerebrovasc...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4468A61P9/10A61P25/00
Inventor 郑仰民罗玉敏韩子萍赵海苹闫峰王荣亮陶真范俊芬张斯佳
Owner XUANWU HOSPITAL OF CAPITAL UNIV OF MEDICAL SCI
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