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Preparation method and use of cerebroside compounds

A technology of cerebrosides and compounds, which is applied in the field of medicine, can solve the problems of being unable to pass through the blood-brain barrier and having a large molecular weight, and achieve the effect of significantly mimicking nerve growth factor activity, high purity, and improving immunity

Inactive Publication Date: 2012-07-25
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, at present, NGF still has the problem of large molecular weight and cannot pass through the blood brain barrier (BBB). The treatment can only be completed by intraventricular injection, and there are many technical problems in long-term treatment.

Method used

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  • Preparation method and use of cerebroside compounds
  • Preparation method and use of cerebroside compounds
  • Preparation method and use of cerebroside compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 compound 1 and compound 2

[0021] (1) Crushing and extraction:

[0022] After crushing 3.4 kg of Termitomyces albuminosus (Berk.) Heim, leaching with ethanol by shaking at room temperature. After suction filtration and concentration, a crude ethanol extract (593.3 g) was obtained. Subsequently, the n-butanol layer crude sample (74.9g) was obtained through solvent distribution; this part was completed with reference to the literature (Tetrahedron, 2000, 56, 5835-5841);

[0023] (2) Separation and purification:

[0024] The crude n-butanol layer was first separated by reversed-phase silica gel ODS chromatography (solvent system by volume: methanol: water=90: 10, 95: 5, 100: 0), to obtain an active component (9.9g, The elution system is methanol: water=95:5); then the component is separated by silica gel column chromatography (the solvent system is methanol by volume ratio: chloroform=5:95, 10:90, 100:0), and finally obtains The active ...

Embodiment 1

[0026] Qualitative identification of the physical and chemical characteristics and chemical structure of compound 1 and compound 2 obtained in embodiment 1:

[0027] The chemical structures of compound 1 and compound 2 were analyzed by HR MS, MS / MS, 1 H NMR, 13 C NMR, COZY, HSQC, HMBC tests determined.

[0028] Physical and chemical properties of compound 2: amorphous powder, molecular formula is C 43 h 83 NO 10 ;

[0029] HRESI-TOF-MS m / z(M+H) + Calcd.for C 43 h 84 NO 10 : 774.6090, Found: 774.6118; FAB-MS / MS m / z 796.7 (M+Na, precursor) + , 514.7 (M+Na-fatty acyl) + , 348.6; see Table 1 for hydrogen spectrum and carbon spectrum data.

[0030] Using MS / MS technique, the length of the two carbon links of compound 2 was determined. In the MS / MS mass spectrum, the parent ion peak of compound 2 is m / z 797 (M+Na) + , the product ion peak is m / z 514 (M+Na-fatty acyl group) + , it is speculated that the aliphatic carbon chain of compound 2 contains 18 carbons (molecul...

Embodiment 3

[0045] Neurogrowth-mimicking activity of cerebrosides.

[0046] PC 12 cells are cell lines cloned from rat adrenal pheochromocytoma. Under the action of NGF, PC12 cells will stop dividing, grow protrusions, and transform into neuron-like cells. Therefore, using PC 12 cells as an effective activity identification system to screen active small molecular compounds will become an effective drug for the treatment of Alzheimer's disease.

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Abstract

The invention provides a preparation method of cerebroside compounds with a high purify. The preparation method comprises the following steps: smashing Termitomyces albuminosus, performing lixiviation in ethanol, suction filtration and concentration to obtain a crude sample of an ethanol extractum educt, distributing by a solvent, finally obtaining two pure compounds through performing positive and reverse phase silica gel chromatographic column separation and repeated high performance liquid chromatography purification on a normal butanol layer crude sample, and identifying the compounds as cerebroside compounds through spectral analysis. The compounds have new chemical structures, are respectively named as termitomycesphin G (n=16) and termitomycesphin H (n=18), and both have obvious quasi nerve growth factor activities confirmed by experiments. The preparation method is applied to preparation of medicaments for preventing neurodegenerative diseases, such as senile dementia and the like, and is in particular applied to the preparation of the medicaments for treating the neurodegenerative diseases, such as Alzheimer's disease and the like. The chemical structure is as follows.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of cerebroside compound and its application in the preparation of drugs for preventing and treating neurodegenerative diseases such as senile dementia. Background technique [0002] With the growth of the global elderly population, the prevalence and incidence of Alzheimer's disease are gradually increasing. In 2011, according to data from the International Alzheimer's Association, the number of patients worldwide has increased to more than 30 million. In my country, senile dementia has gradually become a persistent disease that seriously threatens the health of the elderly. The current drugs for the treatment of Alzheimer's disease mainly increase the level of acetylcholine in the patient's body by inhibiting acetylcholinesterase, that is, acetylcholinesterase inhibitors, which are the earliest and most mature drugs used in clinical treatment o...

Claims

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Application Information

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IPC IPC(8): C07H15/10C07H1/08A61K31/7032A61P25/28
Inventor 戚建华曲媛
Owner ZHEJIANG UNIV
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