Application of (22trans)-3β-hydroxy-cholesta-5,22-dien-24-one in neuroprotective drugs

A neuroprotective and cholesteric technology, applied in drug combinations, steroids, nervous system diseases, etc., can solve unseen problems and achieve the effect of preventing Alzheimer's disease

Active Publication Date: 2017-01-25
南通药享科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And, so far, there is no research report on the biological activity of the compound (22trans)-3β-hydroxyl-cholesta-5,22-dien-24-one

Method used

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  • Application of (22trans)-3β-hydroxy-cholesta-5,22-dien-24-one in neuroprotective drugs
  • Application of (22trans)-3β-hydroxy-cholesta-5,22-dien-24-one in neuroprotective drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Example 1 (22 trans)-3β - Preparation of Hydroxy-cholesta-5,22-dien-24-one

[0022] (1) Frozen Pteris racemosa ( C. racemosa ) (collected from the coast of Zhanjiang, Guangdong) 5 kg (dry weight) was thawed at room temperature, extracted three times by percolation with 30 L 95% ethanol, each percolation for 24 hours, and combined the extracts;

[0023](2) Concentrate the above extract under reduced pressure at a temperature of ≤45°C to recover ethanol to obtain 350 g of crude extract; disperse the crude extract in water to form a suspension, and use petroleum ether (1.5 L), Ethyl acetate (1.5L) and n-butanol (1L) were extracted three times respectively, and the obtained extracts were concentrated under reduced pressure to obtain petroleum ether extract (38g), ethyl acetate extract (160g) and n-butanol extract ( 120g);

[0024] (3) carry out silica gel column chromatography with ethyl acetate extract, with sherwood oil / acetone gradient elution, the separation compon...

Embodiment 2

[0025] Example 2 (22 trans)-3β-hydroxyl-cholesta-5,22-dien-24-one on Aβ 25-35 Induced protective effect of SH-SY5Y cell injury

[0026] 1. Experimental samples and experimental methods

[0027] Preparation of test sample solution: The test sample is the pure compound (22trans)-3β-hydroxy-cholesta-5,22-dien-24-one prepared in Example 1 above. Accurately weigh an appropriate amount of sample and prepare a solution with the desired concentration with DMSO for pharmacological activity testing.

[0028] Cell line and cell subculture: The activity test uses the SH-SY5Y cell line (purchased from ATCC (American type culture collection) in the United States). Subculture in DMEM medium containing 10% FBS in an incubator with 5% carbon dioxide at 37°C.

[0029] Cell activity test method (MTT method): the present invention uses the MTT method to test and evaluate the tested sample for Aβ 25-35 Protective effect leading to decreased viability of SH-SY5Y cells. Dehydrogenase in the mit...

Embodiment 3

[0037] Get the compound obtained in Example 1, add commonly used pharmaceutical excipients, and make dosage forms such as tablets, capsules, and oral preparations.

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Abstract

The invention relates to a compound (22-trans)-3beta-hydroxyl-cholester-5,22-diene-24-ketone, a preparation method and an application thereof. The compound is obtained through extraction from Caulerpa racemosa, pressure reduction and concentration, extraction, silica gel column chromatography and gel column chromatography purification; which has the structure which is measured via a rationalize constant and defined via a spectrum data analysis. Multiple in-vitro SH-SY5Y cell injury neuroprotection experiments prove that the compound has obvious protection effect to beta-amyloid protein 25-35(Abeta-25-35)injury-SY5Y cell, and can be used for preparing the neuroprotectants and medicines to prevent and treat Alzheimer's disease.

Description

technical field [0001] The present invention relates to a kind of extracting (22trans)-3β-hydroxyl-cholesta-5,22-dien-24-one from Racemosa and its preparation method and application; Aβ 25-35 The damaged SH-SY5Y cells have protective active ingredients, so they can be used to prepare neuroprotective drugs and drugs for preventing Alzheimer's disease. Background technique [0002] Alzheimer's disease (AD) is a primary degenerative disease of the central nervous system, which affects more than 35 million people worldwide. Its clinical manifestations are progressive memory impairment, motor impairment, cognitive impairment, etc. (Prince, M. er al, World Alzheimer Report 2013 ; Alzheimer’s Disease International: London, UK, 2013; pp 1−92). There are about 8 million AD patients in my country. Because advanced AD patients cannot take care of themselves and are often accompanied by severe mental and neurological symptoms, it not only seriously reduces the quality of life of the...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61P25/00A61P25/28C07J9/00
CPCA61K31/575C07J9/00
Inventor 毛水春章海燕郭跃伟刘定权
Owner 南通药享科技有限公司
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