Application of FTS (Trans Farnesyl Thiosalicylic Acid/Salirasib)

A technology of farnesyl thiosalicylic acid and farnesyl thiosalicylic acid, which is applied in the directions of salicylic acid active ingredients, nervous system diseases, drug combinations, etc., can solve the problems of lack of significant and reliable curative effect and few side effects.

Inactive Publication Date: 2017-05-10
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 significant and re

Method used

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  • Application of FTS (Trans Farnesyl Thiosalicylic Acid/Salirasib)
  • Application of FTS (Trans Farnesyl Thiosalicylic Acid/Salirasib)
  • Application of FTS (Trans Farnesyl Thiosalicylic Acid/Salirasib)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1: FTS Improves Cognitive Function and Nervous System Function of APP / PS1 Transgenic Mice (Alzheimer's Disease Model)

[0030] Experimental main materials:

[0031] 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.

[0032] Alzheimer's disease model mice

[0033] APP / PS1 mice: 10-month-old male and female APPswe / PS1dE9 double transgenic mice (hereinafter referred to as APP / PS1 mice) were purchased from Jackson Laboratory (Bar Harbor, ME, USA), and were recommended by Jackson Laboratory. Genotype identification by PCR method.

[0034] Drugs and Reagents

[0035] Trans-farnesylthiosalicylic acid (Trans-farnesylthiosalicylic acid, FTS) was purchased from Calbiochem, USA (Cat# 344555). FTS produces an emulsion in 5% Tween 80 or dissolved in dimethylsulfoxide (DMSO). Dilu...

Embodiment 2

[0054] Example 2: FTS improves Aβ 25-35 Cognitive Impairment and Protected Nerve Cells in Mice (Alzheimer's Disease Model)

[0055] Experimental main materials:

[0056] 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.

[0057] Drugs and Reagents

[0058] With embodiment 1.

[0059] Alzheimer's disease model mice

[0060] Aβ 25-35 Dissolve in sterile double-distilled water to make a 1mg / mL solution, and incubate in a 37°C water bath for 4 days to make it aggregated. It can be diluted to the final concentration with normal saline before injection. Maurice et al. found that after the above method, two types of Aβ aggregates can be seen, which are birefringent fibrous and spherical structures. [1] . The mice were anesthetized intraperitoneally with 2% chloral hydrate (400 mg / kg)...

Embodiment 3

[0074] Example 3: FTS enhances the synaptic transmission effect and induction of long-term potentiation in the hippocampal brain region of mice.

[0075] Experimental main materials:

[0076] Three-month-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.

[0077] Drugs and Reagents

[0078] With embodiment 1. FTS produces an emulsion in 5% Tween 80 or dissolved in dimethyl sulfoxide (DMSO). Use normal saline or artificial cerebrospinal fluid (mM: 124.0NaCl, 4.5KCl, 2.0CaCl 2 , 1.0MgCl 2 , 26.0NaHCO 3 , 1.2NaH 2 PO 4 , 10.0D-glucose) was diluted to the use concentration (the final concentration of DMSO was lower than 0.1%), and then intraperitoneally injected (5mg / kg) or incubated in bra...

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Abstract

The invention relates to application of FTS (Trans Farnesyl Thiosalicylic Acid/Salirasib) in preparing an anti-dementia medicine. The application has the advantages that the cognitive disorder of an Alzheimer's Disease model mouse can be relieved by the FTS through oral or intraperitoneal injection, the toxicity of nerves and the withering of nerve cells of Abeta are reduced, and the synaptic transmission effect and long-time-course enhanced induction of a hippocampal brain area are restored; the synaptic transmission effect and long-time-course enhanced induction of the hippocampal brain area of the mouse are improved by the FTS through oral or intraperitoneal injection or cell incubation in a dose-dependent manner; the activity of a nerve cell glutamic acid NMDA receptor and the activity of an acetylcholine receptor alpha7 subtype can be enhanced by the FTS.

Description

technical field [0001] The invention belongs to the field of anti-dementia drugs, in particular to the application of trans-farnesyl Thiosalicylic Acid / Salirasib (FTS) in the preparation of anti-dementia drugs. Background technique [0002] Dementia has been called one of the world's current "epidemics" and is estimated to rank as the fourth most common cause of death in developed countries. So-called senile dementia, the most common is Alzheimer's disease (Alzheimer's disease, AD). Alzheimer's disease is a neurodegenerative disease that occurs in old age and early old age with progressive cognitive impairment as the main clinical manifestation. As the world's population ages, the incidence of Alzheimer's disease is rising rapidly, with one person suffering from the disease almost every 7 seconds, and it is predicted that it will increase to 115.4 million people by 2050. However, there is still a lack of anti-dementia drugs with significant and reliable curative effect, le...

Claims

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Application Information

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IPC IPC(8): A61K31/60A61P25/28
CPCA61K31/60
Inventor 陈玲陈婷婷王亚洪娟
Owner NANJING MEDICAL UNIV
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