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Application of cholest-3,6-dione to treatment of neuronal damage

A neuron injury, neuron technology, applied in the direction of nervous system diseases, neuromuscular system diseases, medical preparations containing active ingredients, etc.

Inactive Publication Date: 2018-12-07
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on the authorized patent of this compound

Method used

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  • Application of cholest-3,6-dione to treatment of neuronal damage
  • Application of cholest-3,6-dione to treatment of neuronal damage
  • Application of cholest-3,6-dione to treatment of neuronal damage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1. The protective effect of cholesta-3,6-dione in glutamate-induced HT-22 oxidative stress injury model

[0047] Take HT-22 cells that have been subcultured 3 times in the middle dish after resuscitation with liquid nitrogen, and observe the cell status before use. If the cell body is round and full, the synapse is intact, and there are almost no dead cells, digest with 0.5ml of 0.25% trypsin for half a minute, blow it into a single cell suspension, collect it in a 15ml centrifuge tube, add complete medium to 3ml, Centrifuge at 1000 rpm for 3 minutes, remove the supernatant, and evenly disperse the pellet in 4ml complete DMEM medium (DMEM+10% FBS+1% P / S), take 0.8ml cell suspension for passage, and then add an appropriate amount of suspension to the complete In DMEM medium, dilute to 4*10 4 cells / ml, planted in a 48-well plate (200μl / well), used for experiments 24 hours later.

[0048] First, cholesteryl-3,6-dione was dissolved in DMSO to a final concentration of ...

Embodiment 2

[0051] Example 2. Cholesterol-3,6-dione in the cerebellar granule neuron apoptosis injury model caused by potassium deprivation Protective effect

[0052] Take out the 7-day-old rat, use a major operation to cut off the head, use small ophthalmic scissors to cut the upper edge of the left and right ears from the vertebral foramen, and then use tweezers to open the upper brain layer to expose the brain tissue, and remove the cerebellum tissue into the device. With or without phenol red DMEM (used as dissecting fluid) in a medium dish on an ice bag.

[0053] After removing the meninges and blood vessels on the cerebellum with ophthalmic forceps, cut the cerebellum tissue with tissue scissors. Transfer the tissue to 0.25% trypsin, digest it at 37°C for 15 minutes, add complete BME medium to 15ml, and then add 100μl Dnase I (8mg / ml), use a dropper to blow away the tissue mass, then Centrifuge at 1000 rpm for three seconds, transfer the upper suspension to another centrifuge tube, ce...

Embodiment 3

[0059] Example 3. Cholesterol-3,6-dione in a model of cerebral cortical neuron excitotoxicity caused by glutamate Protective effects

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PUM

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Abstract

The invention discloses application of cholest-3,6-dione, deuterated substances thereof or pharmaceutically acceptable salts thereof to preparation of drugs used for treating the neuronal damage of patients. According to the invention, it is proved that cholest-3,6-dione can alleviate the oxidative stress damage of hippocampal neurons induced by glutamate, mitigate the apoptosis of cerebellar granule neurons caused by potassium deprivation, and abate the neuroexcitotoxic injury of cortical neurons induced by glutamate, so cholest-3,6-dione can be applied to treatment of neuronal damage.

Description

Technical field [0001] The invention relates to a new medical use of cholesterol-3,6-dione, in particular to the application of cholesterol-3,6-dione in the treatment of neuronal injury. Background technique [0002] Cholesterol-3,6-dione is a cholesterol derivative. The known synthesis method uses cholesterol as a raw material and can be obtained by a variety of synthetic methods (Zhang Wei et al , 2014; R Martinez-Pascual et al , 2017; JGSCBuchanan et al , 1969). The price of raw materials is low, the synthesis is simple and convenient, and the pharmaceutical properties are good. [0003] At present, the activity studies of this compound mainly include: (1) AKR1B10 enzyme inhibitor; (2) antibacterial activity; (3) heart rate reduction activity; (4) antitumor activity (Zhang Wei et al , 2014; Zakaria et al , 2011; ZhangZhaohui et al , 1999; Shi Dayong et al , 2011). So far there is no report about the compound in the field of neuroprotection. There is no report on the authorized...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61P25/00A61P25/16A61P25/28A61P21/00
CPCA61K31/575A61P21/00A61P25/00A61P25/16A61P25/28
Inventor 陈文礼颜光美银巍张静夏邱鹏新
Owner SUN YAT SEN UNIV
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