Method for preparing 5,6,7,4'-tetrahydroxyflavone and application of 5,6,7,4'-tetrahydroxyflavone in medicaments

A tetrahydroxyflavone and reaction technology, applied in the field of medicine, can solve problems such as no literature and patent reports in research

Active Publication Date: 2009-12-02
KPC PHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] At present, the drug application of 5,6,7,4'-tetrahydroxyflavone in the treatment of senile dementia, memory loss, diabetes, arthritis, osteoporosis There are no literature and patent reports on the research

Method used

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  • Method for preparing 5,6,7,4'-tetrahydroxyflavone and application of 5,6,7,4'-tetrahydroxyflavone in medicaments
  • Method for preparing 5,6,7,4'-tetrahydroxyflavone and application of 5,6,7,4'-tetrahydroxyflavone in medicaments
  • Method for preparing 5,6,7,4'-tetrahydroxyflavone and application of 5,6,7,4'-tetrahydroxyflavone in medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] Example 1: Weigh 20.0g of breviscapine raw material, add 500ml of ethylene glycol, 1ml of 4% dilute hydrochloric acid, heat and reflux for 4 hours, filter the product, and dry it to constant weight to obtain 5,6,7,4' -Tetrahydroxyflavone 10.6g, the purity is 96.2% through high performance liquid phase detection. Recrystallize with 60% methanol, filter, and dry to constant weight to obtain 10.1 g of fine product, the purity of which is 98.9% by HPLC.

Embodiment 2

[0141] Example 2: Weigh 15.0g of breviscapine raw material, add 300ml of 1,2-propanediol, 1ml of 5% dilute sulfuric acid, heat and reflux for 3 hours, filter the product, and dry it to constant weight to obtain 5, 6, 7, 7.9g of 4'-tetrahydroxyflavone, the purity is 95.8% by HPLC. Recrystallize with ethanol, filter, and dry to constant weight to obtain 7.1 g of fine product, the purity of which is 99.5% by HPLC.

Embodiment 3

[0142] Example 3: Weigh 12.0 g of scutellarin raw material, add 400 ml of n-butanol, 1 ml of 5% dilute nitric acid, heat and reflux for 5 hours, filter the product, and dry it to constant weight to obtain 5, 6, 7, 4' - 6.5g of tetrahydroxyflavone, the purity of which is 95.7% as detected by high performance liquid phase. Recrystallize with acetone, filter, and dry to constant weight to obtain 5.8 g of fine product, the purity of which is 99.9% by HPLC.

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Abstract

The invention provides a method for preparing a 5,6,7,4'-tetrahydroxyflavone compound, which is characterized by comprising the following steps: taking breviscapinun as a raw material, and performing heating reflux reaction between the breviscapinun and alcohol under the catalysis of acid, namely adding 200 to 500 ml of alcohol substance and 1 to 3 ml of 4 to 5 percent acid into 12 to 20 g of the breviscapinun for the heating reflux reaction; and filtering a product, and drying to a constant weight to obtain 5,6,7,4'-tetrahydroxyflavone shown in a formula I. Experiments prove that the 5,6,7,4'-tetrahydroxyflavone shows obvious strengthening effect on acquisition, consolidation and representation of brain memory of a mice model of alzheimer disease, has obvious improving effect on learning memory of the mice model with memory loss caused by anisodine of an M-cholinergic inhibitor, and can obviously improve the recent memory and long-term memory capacities of mice. The experiments also prove that the 5,6,7,4'-tetrahydroxyflavone has the effect of treating arthritis, and also has good treating effects on diabetes mellitus and osteoporosis.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically a method for preparing 5,6,7,4'-tetrahydroxyflavone by using scutellarin as a raw material, and 5,6,7,4'-tetrahydroxyflavone in the treatment of elderly Drugs for dementia, memory loss, diabetes, arthritis, cancer, and osteoporosis. Background technique [0002] Erigeron breviscapus (Vant.) Hand-Mazz, also known as Erigeron breviscapus (Vant.) Hand-Mazz, belongs to the genus Asteraceae. It has the functions of promoting blood circulation and removing blood stasis, dispelling cold and relieving the exterior, relaxing meridian and activating collaterals, etc. It is often used clinically to treat cardiovascular and cerebrovascular diseases . Breviscapine is an active ingredient of flavonoids extracted from the whole plant of Breviscapus breviscapus. Its main ingredient is scutellarin, and it also contains breviscapine A and other ingredients. At present, scutellarin has been mass-pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/30A61K31/352A61P25/28A61P3/10A61P19/02A61P29/00A61P35/00A61P19/10
Inventor 周荣光
Owner KPC PHARM INC
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