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Application of compound to repair of nerve damage

一种神经损伤、化合物的技术，应用在医药领域，能够解决影响功能恢复、难治疗、阻碍再生轴突延伸等问题

Active Publication Date: 2017-06-13
冯世庆 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Glial scar hinders the extension of regenerated axons to the distal end, and ultimately seriously affects the long-term functional recovery
The pathological environment change of this kind of injury determines the severity of the final injury to a large extent, and greatly affects the repair effect of intervention measures, but there is no systematic and complete mechanism theory
Because the exact injury mechanism in spinal cord injury is not clear, it is difficult to carry out targeted treatment, so the treatment effect is not ideal

Method used

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  • Application of compound to repair of nerve damage
  • Application of compound to repair of nerve damage
  • Application of compound to repair of nerve damage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035]Embodiment 1: Rat spinal cord injury animal model establishment

[0036] An experimental animal model of acute spinal cord injury was established using the IMPACTOR MODEL-Ⅱ spinal cord injury strike system. Female Wistar rats aged 8-10 weeks and weighing 230-250 g were selected, and 60 rats were divided into three groups, 20 rats in each group, which were respectively sham operation group, control group (spinal cord injury group) and experimental group. The rats in the experimental group were injected with the compound of formula (I) at a dose of 15 mg / kg body weight 15 minutes before hitting the injury. After the rats were anesthetized, the lamina of the 10th thoracic vertebra was surgically excised, and the corresponding segment of the spinal cord was exposed, and fixed under the percussion device. figure 1 shown). After the blow, the injured spinal cord was congested and edematically localized, and the rat's hind limbs convulsed and twitched briefly. After the tail...

Embodiment 2

[0037] Embodiment 2: the influence of formula (I) compound on the inflammation of spinal cord injury site

[0038] 6 hours, 24 hours, 48 ​​hours, 7 days, 14 days, and 28 days after the injury, the rat spinal cord tissue was collected for Western Blot detection to detect the inhibitory effect of the compound of formula (I) on pro-inflammatory factors at the spinal cord injury site.

[0039] 1. Expression of ICAM1

[0040] Western Blot analysis found that 48 hours after the injury, the expression of ICAM1 in the control group was higher than that in the sham operation group, but the expression of ICAM1 in the experimental group was significantly reduced when the compound of formula (I) was applied. Through grayscale analysis, it was found that the relative expression of ICAM1 in the experimental group was significantly lower than that in the control group (see figure 2 ).

[0041] Western Blot analysis found that at 2 weeks after injury, the expression of ICAM1 in the control...

Embodiment 3

[0049] Embodiment 3: Effect of formula (I) compound on apoptosis after spinal cord injury

[0050] Respectively after injury 6 hours, 24 hours, 48 ​​hours, 7 days, 14 days, 28 days, 56 days, the rat spinal cord tissue was taken for Western Blot detection and TUNEL staining, and the effect of the compound of formula (I) on apoptosis in the spinal cord injury site was detected. Inhibition of death.

[0051] 1. Expression of Caspase 3

[0052] By Western Blot analysis, it was found that 48 hours after injury, the expression of Caspase 3 in the control group was higher than that in the sham operation group, while the expression of Caspase 3 in the experimental group was significantly lower. By grayscale analysis, it was found that the relative expression level of Caspase 3 in the experimental group was also lower than that in the control group (see Figure 5 ).

[0053] By Western Blot analysis, it was found that at 2 weeks after injury, the expression of Caspase 3 in the contr...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to application of a compound shown in a formula (1) shown in the description to the preparation of a drug for preventing and / or treating nerve damage. The compound can reduce pro-inflammatory cytokines, lower the apoptosis level, promote the survival of neurons and inhibit the formation of glial scars after damage, and has a significant protecting effect on motion function recovery.

Description

technical field [0001] The invention belongs to the technical field of medicine. In particular, the present invention relates to the application of the compound represented by formula (I) in the preparation of medicaments for preventing and / or treating nerve damage. [0002] Background technique [0003] Spinal cord injury (SCI) is a severe traumatic disease with a high incidence and high disability rate, and its repair has always been a difficult problem in the world medical community. Due to the lack of effective repair options, less than 1% of spinal cord injury patients achieve complete neurological recovery. [0004] Spinal cord injury includes primary injury and secondary injury. The primary injury is caused by factors such as mechanical compression, bleeding, and electrolyte overflow. Primary spinal cord injury occurs at the moment of injury and is irreversible, but the scope is limited. The evolution of secondary damage lasts hours to days and is reversible. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61P25/00A23L33/10
CPCA61K31/505A23V2002/00A23V2200/30A23V2200/322A61P25/00
Inventor 冯世庆郝剑姚雪李波段会全赵晨曦张焱孙超孔晓红魏志坚刘畅
Owner 冯世庆
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