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Application of farnesyltransferase inhibitors in preparation of medicine for facilitated cholinergic nerve system

A farnesyltransferase and nervous system technology, applied in the field of anti-dementia drugs, can solve the problems of high curative effect and less side effects, and achieve the effects of enhancing activity and expression, improving cognitive function decline, and improving dementia behavior

Inactive Publication Date: 2017-05-17
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is still a lack of anti-dementia drugs with high efficacy, few side effects, and no drug resistance after long-term use

Method used

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  • Application of farnesyltransferase inhibitors in preparation of medicine for facilitated cholinergic nerve system
  • Application of farnesyltransferase inhibitors in preparation of medicine for facilitated cholinergic nerve system
  • Application of farnesyltransferase inhibitors in preparation of medicine for facilitated cholinergic nerve system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1: Farnesyltransferase inhibitors can enhance the activity and expression of α7nACh receptors

[0034] Experimental main materials:

[0035] 30-35-day-old ICR mice were purchased from the Experimental Animal Center of Nanjing Medical University. The animals were kept in the Experimental Animal Center of Nanjing Medical University, and maintained in an environment with a temperature of 23±2°C, a humidity of 55±5%, and a 12:12h light / dark cycle. They have free access to food and water.

[0036] Drugs and Reagents

[0037] Farnesyltransferase inhibitors (farnesyltransferase inhibitors, FTI): ①Farnesyltransferase inhibitor (FTI, FTI-277) purchased from Calbiochem, USA (Cat#344555), produced emulsion in 5% Tween 80 or dissolved in dimethyl sulfoxide (DMSO), Perform intraperitoneal injection (50mg / kg) or brain slice incubation (1μM). ② Lonafarnib (SCH66336) was purchased from Medchemexpress (Cat#HY-15136) in the United States, dissolved in dimethyl sulfoxide (DMSO),...

Embodiment 2

[0050] Example 2: Inhibitors of farnesyltransferase improve the cognitive function of aged mice—anti-senile dementia.

[0051] Experimental main materials

[0052]4-month-old and 14-month-old male ICR mice (weight 27-30g, SPF grade) were provided by Shanghai Slack Experimental Animal Co., Ltd., license number: SCXK (Shanghai) 2007-0005, certificate number: 2007000517888. Animals were raised in a clean-grade animal room at a temperature of 22-25°C, using SPF-grade special pellet feed for rats and mice and SPF-grade sterilized litter (provided by Nanjing Anlimo Technology Co., Ltd.). 12-hour (6:00-18:00) light-dark cycle, free access to food and water (Nanjing Medical University Animal Center). All operating instruments and materials that come into contact with animals are sterilized by ultraviolet light. Experimental animal operators have been specially trained and have a certificate of qualification for using experimental animals. The preparation of experimental liquids is ca...

Embodiment 3

[0070] Example 3: Farnesyltransferase Inhibitor Improves Cognitive Function in Alzheimer's Disease Mice——Anti-Alzheimer's Disease Dementia (1)

[0071] Experimental main materials:

[0072] The animals were kept in the Experimental Animal Center of Nanjing Medical University, and maintained in an environment with a temperature of 23±2°C, a humidity of 55±5%, and a 12:12h light / dark cycle. They have free access to food and water.

[0073] Drugs and Reagents

[0074] With embodiment 1 and embodiment 2.

[0075] α7nACh receptor agonist 3-(2,4-dimethoxybenzylidene)-anabaseine (DMXB, provided by Dazhao Pharmaceutical Co., Ltd., Japan, code name GTS-21, Taisho Pharmaceuticals, Tokushima, Japan) was dissolved in normal saline for intraperitoneal injection (0.2mg / kg). The acetylcholinesterase inhibitor Galantamine hydrobromide (GAL, galantamine hydrobromide, 99%, Melonepharma, MD1560, Dalian, P.R. China) was dissolved in normal saline for intraperitoneal injection (2 mg / kg).

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Abstract

The invention relates to an application of farnesyltransferase inhibitors (FTI) in preparation of a medicine for a facilitated cholinergic nerve system. The farnesyltransferase inhibitors have an obvious improvement effect on senile dementia, Alzheimer's disease cognitive disorder, vascular dementia and Parkinson's disease cognitive function decline. Specifically speaking, in aging mice, Alzheimer's disease model mice, dementia model mice suffering cerebral ischemia and Parkinson's disease cognitive function decline model mice, the FTI, after subjected to treatment in the ways such as oral cavity injection, intraperitoneal injection, intracerebroventricular injection or cell incubation, can all dose-dependently (1) increase the activity and expression of a nerve cell acetylcholine receptor alpha7nACh, (2) improve dementia behavior, and (3) recover the synaptic transmission effect and long-term potentiation induction of the hippocampal brain.

Description

technical field [0001] The invention belongs to the field of anti-dementia drugs, and in particular relates to the application of a farnesyl transferase inhibitor in the preparation of drugs that facilitate the cholinergic nervous system. Background technique [0002] Alzheimer's disease (AD) is a neurodegenerative disease with progressive cognitive impairment as the main clinical manifestation. As the world's population is aging, the incidence of AD is rising rapidly, with one person suffering from the disease almost every 7 seconds, and it is predicted that it will increase to 90 million people by 2050. Due to the lack of effective prevention and treatment measures, AD has been listed as the fourth cause of death. Vascular dementia (VD) refers to a syndrome of severe cognitive impairment caused by ischemic stroke, hemorrhagic stroke, and cerebrovascular diseases that cause hypoperfusion in brain areas such as memory, cognition, and behavior. The prevalence of vascular de...

Claims

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Application Information

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IPC IPC(8): A61K31/198A61K31/223A61K31/4545A61K31/4709A61P25/28A61P25/16
CPCA61K31/198A61K31/223A61K31/4545A61K31/4709
Inventor 陈玲陈婷婷王亚张宝峰
Owner NANJING MEDICAL UNIV
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