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Butyl phthalide derivative and application thereof in preparation of medicine for protecting nerve cells

A derivative, butylphthalide technology, applied in the field of biomedicine and chemistry, can solve problems such as elevated transaminases

Active Publication Date: 2021-08-24
INST OF LAB ANIMAL SCI CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, all drugs have to be metabolized by liver and kidney function, and some patients may experience elevated transaminases

Method used

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  • Butyl phthalide derivative and application thereof in preparation of medicine for protecting nerve cells
  • Butyl phthalide derivative and application thereof in preparation of medicine for protecting nerve cells
  • Butyl phthalide derivative and application thereof in preparation of medicine for protecting nerve cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Embodiment 1, the synthesis of derivative

[0058] ①3-Butyl-7-nitroisobenzofuran

[0059] The chemical formula is as follows:

[0060]

[0061] The synthetic route is as follows:

[0062]

[0063] The picture of the quality inspection result is as follows figure 1 shown.

[0064] ②3-Butyl-7-(trifluoromethyl)isobenzofuran

[0065] The chemical formula is as follows:

[0066]

[0067] The synthetic route is as follows:

[0068]

[0069] The picture of the quality inspection result is as follows figure 2 shown.

[0070] ③3-Butyl-5-bromoisobenzofuranone

[0071] The chemical formula is as follows:

[0072]

[0073] The synthetic route is as follows:

[0074]

[0075] The picture of the quality inspection result is as follows image 3 shown.

[0076] ④3-Butyl-5-(trifluoromethyl)isobenzofuranone

[0077] The chemical formula is as follows:

[0078]

[0079] The synthetic route is as follows:

[0080]

[0081] The picture of the qualit...

Embodiment 2

[0083] Example 2. Detection test of butylphthalide derivatives on Aβ-induced anti-apoptotic MTT activity of SY5Y nerve cells

[0084] Experimental steps:

[0085] 1. SHY5Y cells were treated with 1*10 5 piece / cm 2 Density inoculated in 96-well plate and cultivated for 24h.

[0086] 2. When the confluence of the cells reaches 80%~90%, discard the medium, wash with PBS 3 times, add drugs (0.5mM, diluted in normal medium DMEM), and incubate at 37°C for 4h.

[0087] 3. Discard the drug, wash twice with PBS, and add 20 μM Aβ 25-35 (Add PBS in advance to dissolve, incubate at 37°C for 2 days) and incubate with the drug mixture at 37°C for 48h, in which Aβ 25-35 group as a model control. In addition, a PBS group (edge ​​holes were filled with sterile PBS to eliminate edge effects) and a blank control group (normal cells were cultured in normal medium without any treatment) were set up.

[0088] 4. Add 10 μL of MTT solution (5 mg / mL) prepared in PBS to each well, and incubate ...

Embodiment 3

[0093] Example 3, butylphthalide derivatives release test for active oxygen in Aβ-induced SY5Y nerve cell damage

[0094] According to the results of the MTT experiment, the nerve cell injury reactive oxygen species release experiment was further tested. In this experiment, all compounds were detected at the same time, but the cells in group ③ were not involved in the analysis due to more cell death.

[0095] Experimental steps:

[0096] 1. SHY5Y cells were treated with 1*10 5 piece / cm 2 Density inoculated in 96-well plate and cultivated for 24h.

[0097] 2. When the confluence of the cells reaches 80%~90%, discard the medium, wash with PBS 3 times, add drugs (0.5mM, diluted in normal medium DMEM) and incubate at 37°C for 4h.

[0098] 3. Discard the drug, wash twice with PBS, and add 20 μM Aβ 25-35 (Add PBS in advance to dissolve, incubate at 37°C for 2 days) and incubate with the drug mixture at 37°C for 48h, in which Aβ 25-35 group as a model control. In addition, a ...

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PUM

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Abstract

The invention relates to the fields of biological medicine and chemistry, provides a butyl phthalide derivative and application thereof in preparation of a medicine for protecting nerve cells. More specifically, the invention provides application of the butyl phthalide derivative or a pharmaceutical composition composed of the butyl phthalide derivative to preparation of drugs for preventing and / or treating cell injury related diseases and neurodegenerative diseases. The nerve cell injury diseases include but are not limited to stroke, spinal injury and nervous system diseases accompanied with blood-brain barrier injury; and the neurodegenerative disease includes, but is not limited to, Parkinson's disease, Alzheimer's disease, Huntington's disease, amyotrophic lateral sclerosis, spinal muscular atrophy, primary lateral sclerosis, or spinal cerebellar ataxia.

Description

technical field [0001] The invention relates to the fields of biomedicine and chemistry, in particular to butylphthalide derivatives and their application in preparing medicines for protecting nerve cells. Background technique [0002] Butylphthalide is a small molecular protein extracted from celery or celery seeds. The protein is small and easily passes through the blood-brain barrier to affect brain cells. In 1978, the Institute of Materia Medica, Chinese Academy of Medical Sciences isolated L-butylphthalide from cress seed. Butylphthalide was chemically synthesized for the first time in 1980. The initial research direction of butylphthalide was anti-epileptic, but because the therapeutic dose of butylphthalide for anti-epileptic treatment was close to the toxic dose, there was a big safety hazard, so the research was stranded. [0003] Butylphthalide is mainly used in the treatment of mild and moderate acute ischemic stroke. It can reduce the concentration of intracell...

Claims

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Application Information

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IPC IPC(8): C07D307/88A61P25/00A61P25/14A61P25/16A61P25/28A61K31/343
CPCA61P25/00A61P25/14A61P25/16A61P25/28C07D307/88
Inventor 秦川李彦红梁唯
Owner INST OF LAB ANIMAL SCI CHINESE ACAD OF MEDICAL SCI
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