Application of guanidino compound

A compound, guanidine-based technology, applied in the application field of guanidine-based compounds, can solve problems such as toxic side effects, difficult synthesis, high cost, etc., and achieve remarkable effects and potential clinical application value

Active Publication Date: 2017-02-01
SHANGHAI INST OF PHARMA IND CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a guanidinium compound in order to overcome the certain toxic and side effects and use limitations of Alzheimer's disease drugs or inhibitors in the prior art, such as defects such as difficult synthesis and high cost. Applications

Method used

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  • Application of guanidino compound
  • Application of guanidino compound
  • Application of guanidino compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030]

[0031] The effect of guanidine on the protective effect of 100 μM hydrogen peroxide-induced hippocampal nerve cell damage in neonatal rats was tested. The specific operation is: separate and culture the neurons in the hippocampal region of the rat brain born within 24 hours, and use 1x10 6 / ml cell density cultured for 7 days to the best state of growth. Then the well-grown hippocampal neurons were divided into blank group, model group and test drug group (n=4, ie 4 duplicate wells). The blank group and model group were given blank DMEM medium, and the treatment group was given medium containing different final concentrations of the drug to be tested. After 2h, add H 2 o 2 After 24 hours of injury in DMEM medium (final concentration: 100 μM), the cell viability was measured by MTT method. The results are shown in Table 1.

[0032] Table 1. Protective effect of guanidine on hippocampal nerve cell injury in neonatal rats induced by 100 μM hydrogen peroxide

[0...

Embodiment 2

[0039] Guanidine was tested for its inhibitory effect on Aβ aggregation in vitro. Since Aβ protein has the phenomenon of spontaneous aggregation in 10MPBS, the specific operation of this experiment is to set up different Aβ protein aggregation systems according to the experimental needs. Blank group: put in 10M PBS; Aβ 1-42Control group: Aβ dissolved in 10M PBS 1-42 , (Aβ 1-42 Final concentration 100μg / ml); Different drug groups to be tested: Aβ dissolved in 10M PBS 1-42 , and contain different concentrations of the drug to be tested (Aβ 1-42 The final concentration is 100 μg / ml), and the above Aβ protein aggregation system is put into a 96-well plate and cultured in a 37° C. incubator. Select the corresponding measurement time point. When measuring, take 2 μL of the solution of each aggregation system, add 198 μL of 3 μM Th-T (thioflavin T) to a black transparent bottom 96-well plate, set the microplate reader Ex=442nm, Em=480nm for detection, at this time Aβ 1-42 The f...

Embodiment 3

[0046]

[0047] According to the method of Example 2, the inhibitory effect of guanidine formic acid on Aβ aggregation in vitro was tested, and the results are shown in Table 3.

[0048] Table 3. Inhibitory effect of guanidine formic acid on Aβ aggregation in vitro (n=3, )

[0049]

[0050] Among them, * indicates that in the one-way analysis of variance, P<0.05, that is, the difference is significant compared with the model group; ** indicates that in the one-way analysis of variance, P<0.01, that is, the difference is extremely significant compared with the model group.

[0051] The level of effect in this example suggests that the compound may prevent and treat neurodegenerative diseases by inhibiting Aβ aggregation in the brain in future clinical applications.

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Abstract

The invention discloses an application of a guanidino compound represented by formula I or a pharmaceutically acceptable salt of the guanidino compound in the preparation of medicines for treating nervous system degenerative diseases. R in the formula I is hydrogen, a carboxyl group or a -C1~C5 alkyl-carboxyl group. The guanidino compound has a substantial protection effect on hydrogen peroxide induced neonatal rat hippocampal nerve cell injures, has a substantial inhibition effect on in vitro beta-amyloid protein aggregation, and has potential clinic application values.

Description

technical field [0001] The present invention relates to the application of a guanidinium compound. Background technique [0002] Alzheimer's disease (AD) is the most common neurodegenerative disease and the most common cause of dementia, accounting for about 70% of the total incidence of dementia. Clinically, it is commonly characterized by generalized dementia such as memory impairment, aphasia, apraxia, agnosia, impairment of visuospatial skills, executive dysfunction, and personality and behavior changes. Epidemiological data show that at least 35 million people around the world suffer from AD, with an incidence rate as high as 5% among the elderly over 65 years old. The fourth leading cause of death after cancer, cancer and heart disease. Alzheimer's disease not only endangers the physical and mental health and quality of life of the elderly, but also brings a heavy burden to the family and society. Because senile dementia is closely related to aging, the incidence of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/155A61K31/325A61K31/195A61P25/28
Inventor 董文心顾丰华陈嘉刘翔吴彤张美璇李默影
Owner SHANGHAI INST OF PHARMA IND CO LTD
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