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Application of cholestane-3 beta, 5 alpha, 6 beta-triol in preparation of neuronal protection medicine

A neuron protection, cholestane technology, applied in the field of endogenous steroid compounds, can solve the problems of no research reports

Active Publication Date: 2010-03-31
GUANGZHOU CELLPROTEK PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

So far, no studies have reported that cholestane-3β,5a,6β-triol (YC-5) has activity in nervous tissue or as a neuroactive steroid

Method used

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  • Application of cholestane-3 beta, 5 alpha, 6 beta-triol in preparation of neuronal protection medicine
  • Application of cholestane-3 beta, 5 alpha, 6 beta-triol in preparation of neuronal protection medicine
  • Application of cholestane-3 beta, 5 alpha, 6 beta-triol in preparation of neuronal protection medicine

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0037] 1. Synthesis of YC-5 from cholesterol

[0038]

[0039] YC-5's 13 C-NMR (DMSO)

[0040] 11.578(18-CH3), 18.107(21-CH3), 20.535(26-CH3), 21.988(27-CH3),

[0041] 23.581(24-CH3), 66.374(3-CH), 74.782(6-CH), 75.005(5-C)

[0042] 2. Culture of neurons

[0043] 1. Culture of Rat Cerebellar Granule Neurons

[0044] Take out the cerebellum of 7-8 days old rats weighing about 15-20g without meninges and blood vessels, digest with 0.25g / L trypsin, blow the cells into a single-cell suspension with 0.05g / L DNase I blowing solution solution, centrifuged, and the precipitate was taken, diluted with BME medium containing 10% (v / v) FBS and 25mM KCl, and inoculated on a petri dish pre-coated with polylysine. 10 μM Ara-C was added 24 hours after inoculation to inhibit the growth and proliferation of non-neuronal cells, so that the purity of cerebellar granule neurons was above 95%. Glucose was added during culture to supplement the energy required for cell metabolism. Experime...

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PUM

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Abstract

The invention reveals that endogenous cholesterol metabolic product cholestane-3 beta, 5 alpha, 6 beta-triol (YC-5) has protection function for neuronal damage caused by cerebral ischemia, ischemia ofspinal cord, epileptic seizure and convulsion and relates to an application of YC-5 in preparation of neuronal protection medicine. The YC-5 can be prepared from cholesterol through two steps. The primitive cell culture in vitro and spinal cord ischemia animal model proves that YC-5 has protection function for neuronal damage caused by cerebral ischemia, ischemia of spinal cord, epileptic seizureand convulsion. YC-5 in effective dose has no toxic and side reactions. YC-5 is an effective neural protectant which aims to multiple molecular mechanism and cures cerebral ischemia damage, spinal cord ischemia damage, epileptic seizure and convulsion.

Description

technical field [0001] The present invention relates to the protective effect of endogenous steroid compound cholestane-3β, 5a, 6β-triol on neuron damage in cerebral ischemia, spinal cord ischemia, epilepsy and convulsions. Background technique [0002] The vast majority of fast excitatory transmission in the central nervous system (CNS) is associated with release of glutamate receptors and the associated neurotransmitter glutamate. Glutamate receptors are involved in the early development of the human CNS and play a decisive role in synaptic plasticity such as learning and memory. Although glutamate is an important mediator for maintaining normal nerve cell activity, a large amount of excitatory neurotransmitters (such as glutamate, Glu) are released, and excessive stimulation of glutamate receptors can trigger nerve cell death (known as excitatory neurotransmitters). Toxic effect (excitotoxicity)). Nerve damage caused by this excitotoxicity is usually accompanied by exce...

Claims

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Application Information

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IPC IPC(8): A61K31/575A61P9/10A61P25/08A61P25/00
Inventor 颜光美胡海燕孙环环桑韩飞冷田东刘爱伶银巍黄奕俊张静夏邱鹏新
Owner GUANGZHOU CELLPROTEK PHARMA
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