Application of marine steroids compound in preparing medicine for treating neuronal damage

A technology for steroids and neuron damage, which is applied in the application field of marine steroids in the preparation of drugs for the treatment of neuron damage, and can solve problems such as inconsistent dosage, neuron damage, and membrane structure damage

Inactive Publication Date: 2008-04-23
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, some scholars have put forward the opposite view, thinking that anticoagulant treatment immediately after the onset of the disease, including the use of heparin, low molecular weight heparin, heparin factor or special thrombin inhibitors, did not show long-term or short-term improvement; The risk of thrombosis and pulmonary embolism is offset by the risk of intracranial and intracranial hemorrhage
[0007] 3. Anti-platelet aggregation Aspirin has anti-platelet aggregation effect and has been widely used in the treatment of ischemic brain injury, but its dosage has not been unified in recent years
[0012] 2. Free radical scavenger During acute cerebral ischemia, a large number of free radicals in the brain are produced, which destroys the membrane structure and causes neuron damage
NASs have the classic mode of action of general steroid hormones, that is, by binding to specific nuclear receptors in neurons such as progesterone and androgen receptors, they regulate the gene expression of various receptors and proteins in neurons and glial cells , known as genome effect, the process involves DNA transcription, translation and protein modification, so the onset is slow; NASs can also rapidly modulate the activity of GABA receptors, Glu receptors, acetylcholine receptors and intracellular Sigmal receptors to non- The genomic approach directly affects central activities such as emotion, neuronal plasticity and excitability, synaptic transmission, and learning and memory

Method used

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  • Application of marine steroids compound in preparing medicine for treating neuronal damage
  • Application of marine steroids compound in preparing medicine for treating neuronal damage
  • Application of marine steroids compound in preparing medicine for treating neuronal damage

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Experimental program
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Embodiment Construction

[0040] 1. Synthesis of marine steroid YC-1 (24-methylene-cholesta-3β, 5α, 6β, 19-tetrol) using cheap hyodeoxycholic acid as raw material, and obtained the target through 14 steps of organic reaction synthesis Compound YC-1 and its related analogues, and the intermediates and target compounds were characterized by spectral techniques.

[0041] 1. For the synthetic route of YC-1 (24-methylene-cholesta-3 5 6 19-tetrol), see figure 1 .

[0042] 2. Optimization of YC-1 synthesis process conditions

[0043] (1) Synthesis of 3-acetoxy-cholesta-5-bromo-6-hydroxyl-24-one

[0044] This step reaction 3-acetoxy-cholest-5-ene-24-ketone and N-bromosuccinimide react to obtain, there are multiple isomers in the product, and productive rate is lower, by selecting solvent Optimizing the reaction process of the reaction conditions such as temperature and reaction temperature; researching the separation method through purification methods such as recrystallization, solvent precipitation, and c...

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Abstract

The present invention relates to an application of marine steroid YC-1 (24-methylene-cholesterol-3 beta, 5 alpha, 6 beta, 19-tetraol) in preparation of medicine for curing neuronal injury. It is characterized by that the oxysterol compound marine steroid YC-1 extracted from lip-softened coral of the Nansha Islands has protection action for several kinds of neuronal injuries, under the condition of effective protection dosage it does not produce toxic reaction. Said invention adopts a chemical synthesis method to make large-scale production.

Description

[technical field] [0001] The present invention relates to the application of neural steroid compounds, in particular to marine steroid YC-1 (24-methylene-cholesta-3β, 5α, 6β, 19-tetrol) in the preparation of drugs for treating neuron damage Applications. [Background technique] [0002] Cerebrovascular disease is a common and frequently-occurring disease, and it is one of the three major diseases that seriously endanger human health. In the spectrum of diseases, the number of deaths due to cerebrovascular disease every year ranks second in Japan and third in the United States , and has occupied the first place in our country for several years! Cerebrovascular disease can basically be regarded as a kind of senile disease, and its incidence rate increases with age. Over 55 years old, the incidence rate doubles for every 10 years of age increase. With the improvement of human living standards and the extension of human life span , the aging degree of the social population is i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61P9/10
CPCA61K31/56A61P9/00A61P9/10A61P25/00A61P25/16A61P25/28A61P43/00
Inventor 颜光美邱鹏新黄奕俊银巍苏兴文刘爱伶桑韩飞蔡翔
Owner SUN YAT SEN UNIV
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