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Preparation method and application of 3'8''-bis-apigenin type bis-flavonoid

A technology of biflavonoids and compounds, which is applied in the application field of bisflavonoids, can solve problems such as the research and the effect of 3'8"-bispigenin-type bisflavonoids, and achieve the purpose of inhibiting the formation of senile plaques and preventing Or reduce senile plaques, the effect of simple and easy preparation process

Inactive Publication Date: 2010-05-26
广州市爱菩新医药科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there is no research on the effect of 3’8”-bipigenin-type biflavonoids in inhibiting β-amyloid

Method used

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  • Preparation method and application of 3'8''-bis-apigenin type bis-flavonoid
  • Preparation method and application of 3'8''-bis-apigenin type bis-flavonoid
  • Preparation method and application of 3'8''-bis-apigenin type bis-flavonoid

Examples

Experimental program
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Effect test

Embodiment 1

[0035] The method for preparing Jinsong biflavone from artificially cultivated Yunnan yew:

[0036] The branches and leaves of Taxus yunnanensis were artificially cultivated, air-dried, crushed into 80 meshes, heated and refluxed with 8 times the volume of 95% ethanol to extract 3 times, each time for 1 hour, filtered, combined filtrates, concentrated under reduced pressure, and recovered ethanol to obtain extract or concentrate. The extract is dissolved in acetone, mixed with silica gel (80-100 mesh) at a mass ratio of 1:1, and dried in the air. Weigh 8 times the sample mass of silica gel (200-300 mesh), use petroleum ether as the eluent, and wet-pack the column, first elute with 3 column volumes of petroleum ether to remove fat-soluble substances such as pigments, and then use 5 column volumes Volume petroleum ether: acetone (volume ratio 55:45) for elution. The eluate was collected and concentrated under reduced pressure to obtain crude extract A (Part A). Part A continue...

Embodiment 2

[0041] 1. The effect of Aquinone on the aggregation of β-amyloid protein and the aggregation state of Aβ.

[0042]1.1 Experimental method: Establish an in vitro aging model of β-amyloid protein, use Thioflavin T fluorescence analysis, and observe the effect of candidate drugs on β-amyloid protein aggregation and fiber formation and depolymerization of aging fibers through in vitro incubation.

[0043] (1) Solution preparation:

[0044] Thioflavin T solution: Take 3 mg powder and dissolve it in glycine-NaOH buffer solution (50 mM, pH 8.5), and the concentration of the stock solution is 1 mM. The working concentration was diluted to 5 μM;

[0045] β-amyloid protein solution: β-amyloid protein powder is prepared into a 25 μM solution with phosphate buffer PBS (0.1M, pH 7.4), and stored in -80°C in aliquots, melted and diluted when used;

[0046] Drug solution: dissolved in dimethyl sulfoxide (DMSO, dimethylsulfoxide), prepared to a concentration of 1mg / ml, stored in a low-tempe...

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Abstract

The invention discloses a preparation method and application of 3'8''-bis-apigenin type bis-flavonoid. The preparation method of the compound comprises the following steps of: hot refluxing and extracting coarse powders of Taxus cuspidatea twigs and leaves by using ethanol to obtain total extract; and performing reversed phase and normal phase column chromatography, gel and recrystallization and separation on the total extract to obtain the 3'8''-bis-apigenin type bis-flavonoid. The 3'8''-bis-apigenin type bis-flavonoid is used for preparing medicaments for inhibiting formation of senile plaques or treating an Alzheimer disease, can effectively reduce the generation of Beta amyloid, also depolymerizes the aggregated Beta amyloid, has no toxic effect on cells, and also can stimulate growth of cells at a high concentration; and the preparation method has simple process and high yield.

Description

technical field [0001] The invention relates to the application field of biflavonoids, in particular to a preparation method and application of a 3'8"-bipigenin type biflavonoids. Background technique [0002] Alzheimer's disease (Alzheimer's disease), is a primary degenerative brain disease, is a frequently-occurring and common disease of the elderly, clinically characterized by progressive memory and cognitive dysfunction. Senile dementia is a neurodegenerative disease caused by a variety of reasons, involving various pathological mechanisms and various pathological manifestations. The main pathological manifestation is the accumulation of β-amyloid protein in the cerebral cortex and hippocampus. Senile plaques (senile plaque, SP), as well as neurofibrillary tangles (neurofibrillary tangle, NFT) and loss of nerve cells. Studies generally believe that the abnormal increase and deposition of β-amyloid in the brain of Alzheimer's patients is the core event that initiates neu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30C07D311/40A61K31/352A61P25/28
Inventor 顾琼李艳萍古练权黄志纾欧田苗
Owner 广州市爱菩新医药科技有限公司
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