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A kind of enrichment method and application of Sophora dihydroflavonoid G

A technology of dihydroflavonoids and Sophora genus, which is applied in the field of preparation of antitumor drugs, Sophora genus dihydroflavonoids G, can solve the problems of low content and low extraction yield, and achieve high purity and extraction yield of Sophora flavescens The effect of improving and enriching the method is simple and easy to implement

Active Publication Date: 2016-11-30
HEILONGJIANG UNIV OF CHINESE MEDICINE +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Although the anticancer activity of Sophora flavone G in Sophora flavescens has been reported in the prior art, because the content of Sophora flavanone G in Sophora flavescens is relatively low, the extraction yield is not high, and the extraction method disclosed in CN1676521A The yield of Sophora dihydroflavone G is less than 0.1%. Therefore, it is necessary to develop a more effective extraction and enrichment method for Sophora genus dihydroflavone G

Method used

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  • A kind of enrichment method and application of Sophora dihydroflavonoid G
  • A kind of enrichment method and application of Sophora dihydroflavonoid G
  • A kind of enrichment method and application of Sophora dihydroflavonoid G

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Embodiment 1

[0035] Example 1, the enrichment method of Sophora dihydroflavone G

[0036] 1) 500g of Sophora flavescens raw material, crushed and passed through No. 2 sieve, added 3000mL of ethyl acetate, ultrasonically extracted for 30min, filtered, added 3000mL of ethyl acetate to the residue, continued ultrasonically for 30min, filtered, combined filtrate, at a temperature lower than 50°C The organic solvent was recovered under reduced pressure to dryness to obtain 10.2 g of the total flavonoids sample of Sophora flavescens.

[0037] 2) Mix the total flavone solids of Sophora flavescens in step 1) with the newly prepared pyridine hydrochloride in a weight ratio of 1:1, N 2 Under protective conditions, the temperature was raised to 60°C for reaction. React for 4 hours, cool, add 100 mL of water, and freeze overnight at 4°C. Filtration, the solid is the crude product of Sophora flavone G.

[0038] 3) The converted crude product is subjected to silica gel H column chromatography, and th...

Embodiment 2

[0041] Embodiment 2, the enrichment method of Sophora dihydroflavone G

[0042] 1) 500g of Sophora flavescens raw material, crushed and passed through No. 1 sieve, add 3000mL of 60% ethanol, ultrasonically extract for 60min, filter, add 60% ethanol to the residue, continue ultrasonic for 30min, filter, combine the filtrates, under the condition of lower than 50°C The organic solvent was recovered under reduced pressure to dryness, and 25.3 g of the total flavonoids of Sophora flavescens was obtained.

[0043] 2) Add 25.3g of the total flavonoids of Sophora flavescens in step 1) into a 1000mL dry four-necked reaction flask, add 10g of pyridine and 100g of methanol, heat up to 40°C, slowly add 5g of anhydrous aluminum trichloride in batches, add Complete the reaction at 50°C. TLC detection, stop reaction. Cool down to room temperature, add a small amount of saturated ammonium chloride aqueous solution until there is no solid in the reaction mixture, add ethyl acetate for extra...

Embodiment 3

[0047] Embodiment 3, the enrichment method of Sophora dihydroflavone G

[0048] 1) Sophora flavescens raw material 500g, crushed and passed through No. 2 sieve, add methanol 3000mL, ultrasonically extract for 60min, filter, add methanol to the residue and continue ultrasonically for 30min, filter, combine filtrate, and recover organic The solvent was dried to obtain 20.2 g of the total flavonoids of Sophora flavescens.

[0049] 2) Mix the 20.2g total flavonoids sample of Sophora flavescens in step 1) with the newly prepared pyridine hydrochloride in a weight ratio of 1:1, N 2 Under protective conditions, the temperature was raised to 50°C for reaction. React for 4 hours, cool, add 200 mL of water, and freeze at 4°C overnight. Filtration, the solid is the crude product of Sophora flavone G.

[0050] 3) performing silica gel column chromatography on Sophora dihydroflavone G, and eluting with petroleum ether-ethyl acetate system as the mobile phase system;

[0051] 4) Differe...

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Abstract

The invention relates to an enrichment method of Sophoraflavanone G and application of the Sophoraflavanone G in preparing antineoplastic drugs. A catalytic conversion step is introduced into the Sophoraflavanone G extraction and enrichment process to obviously enhance the extraction yield of the Sophoraflavanone G. According to the detected physicochemical properties of the Sophoraflavanone G, the Sophoraflavanone G is prepared into tablets, capsules, liposome, nanoparticles, nano suspensoids, self-microemulsions, phospholipid composites, enteric coated tablets and the like, thereby being beneficial to better displaying the anticancer effect of the Sophoraflavanone G.

Description

technical field [0001] The invention relates to the field of medicines, in particular to a method for enriching dihydroflavone G of the genus Sophora and its application in the preparation of antitumor drugs. Background technique [0002] Cancer is a malignant tumor originating from epithelial tissue. It is a common type of malignant tumor and has always been one of the serious diseases that threaten human life. According to the WHO, the incidence of cancer in China is rising sharply. In 2014, there were about 220 people in China. Thousands of people die from cancer, so finding effective anticancer drugs has become a top priority for cancer treatment. my country is rich in resources of Chinese herbal medicines, and a variety of Chinese herbal medicines have been found to have anti-cancer effects, such as Sophora flavescens, Hedyotis diffusa, Cocklebur, dandelion, Mylabris, etc. However, due to the complex components in Chinese herbal medicine and the low content of active i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D311/32C07D311/40A61K31/352A61P35/00
CPCA61K31/352C07D311/32C07D311/40
Inventor 杨志欣单柏松李霞王祺茹
Owner HEILONGJIANG UNIV OF CHINESE MEDICINE
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