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Use of diphenyl ether compounds in the preparation of beta-amyloid aggregation inhibitors

A technology for amyloid and compounds, which is applied in the field of biphenyl ether compounds and the preparation of β-amyloid aggregation inhibitors, which can solve the problems of high toxicity of aggregates

Active Publication Date: 2016-02-10
珠海暨安特博生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although Aβ 42 Not much in the human body, only Aβ 40 1 / 99 of Aβ 42 Due to spontaneous aggregation, its aggregates are more toxic

Method used

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  • Use of diphenyl ether compounds in the preparation of beta-amyloid aggregation inhibitors
  • Use of diphenyl ether compounds in the preparation of beta-amyloid aggregation inhibitors
  • Use of diphenyl ether compounds in the preparation of beta-amyloid aggregation inhibitors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Aspergiullssp. 16-20-8-1 was isolated from the budless variety of lichen flat disc soft ground roll collected from Changbai Mountain, Jilin Province, China, and was identified as Aspergiullssp. by taxonomic research.

[0027] The Aspergillus fungus (Aspergiullssp.) 16-20-8-1 was preserved on January 26, 2014 in the General Microbiology Center of China Committee for the Collection of Microbial Cultures (No. CGMCCNo.8619, location: Beichen West, Chaoyang District, Beijing Institute of Microbiology, Chinese Academy of Sciences, No. 1 Courtyard No. 1 Road, 100101).

Embodiment 2

[0028] Embodiment 2: Aspergillus (Aspergiullssp.) 16-20-8-1 fermentation and sample pretreatment method thereof

[0029] Aspergillus (Aspergiullssp.) 16-20-8-1 was activated on a slope, inoculated in PDB medium, 25°C, 200r min -1 Shake culture for 5 days, inoculate into 2100g (70g×30) rice culture medium according to the inoculum size of 10.0mL, and culture at 25°C for 40 days statically to obtain a fermented product. Add 2 times the volume of ethyl acetate to continuously soak and extract the fermented product, filter the extract (repeat 3 times), and concentrate the extract to dryness to obtain a crude extract. The PDB medium consists of the following components by weight to volume ratio: potatoes 200g / L, glucose 20g / L, and purified water 1L.

Embodiment 3

[0030] Embodiment 3: compound is separated

[0031]The total extract of the fermentation product of this bacterial strain is suspended with 10 times the amount (M / V) of 90% methanol / water, then extracted with an equal volume of cyclohexane to obtain the cyclohexane extraction site (C) and 90% methanol / water layer site (W). The 90% methanol / water layer was further separated, using ODS medium and low pressure column chromatography, sequentially eluted with water-methanol at a volume ratio of 70:30, 50:50, 30:70 and 0:100 to obtain the fraction 16- 20-8-1W1, 16-20-8-1W2, 16-20-8-1W3 and 16-20-8-1W4; fraction 16-20-8- 1W3 was subjected to ODS medium and low pressure column chromatography, and eluted with water-methanol at volume ratios of 65:35, 55:45, 35:65, 25:75 and 0:100 in sequence, and 5 column volumes were eluted at each ratio to obtain Subfractions 16-20-8-1W3-1 (elution site with volume ratio 65:35 water-methanol), 16-20-8-1W3-2 (volume ratio 55:45 water-methanol site e...

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Abstract

The invention belongs to the field of natural medicine, and discloses application of a diphenyl ester compound in preparing a beta-amyloid protein aggregation inhibitor. The diphenyl ester compound has the function of inhibiting beta-amyloid protein aggregation activity, and the beta-amyloid protein aggregation inhibitor is applied to preparation of Alzheimer disease treatment medicine.

Description

technical field [0001] The invention belongs to the field of natural medicines, and in particular relates to the use of a diphenyl ether compound with the activity of inhibiting the aggregation of β-amyloid protein (Amyloid-β, Aβ) in the preparation of an inhibitor of β-amyloid protein aggregation. Background technique [0002] Alzheimer's disease is a kind of central nervous system degenerative disease syndrome caused by brain diseases, characterized by progressive cognitive dysfunction and memory impairment, which manifests as intelligence (including memory, learning ability, direction recognition ability, language ability, etc.) ability, comprehension, and judgment). Alzheimer's disease (AD), Vascular dementia (VA), Lewy body dementia (Dementia with Lewybodies, DLB) and frontotemporal dementia (Frontotemporaldementia, FTD). Types of. Among all dementia patients, Alzheimer's disease patients account for 50-70%, which is the most common type of senile dementia. [0003] ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/085A61P25/28C12P7/22C12R1/66
Inventor 高昊姚新生郑易之陈国栋郭良栋孙翔赵欢李小霞孔明珠
Owner 珠海暨安特博生物科技有限公司
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