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Application of three compounds in terminalia in preparation of anti-inflammatory drug and preparation method of compounds

A compound and drug technology, applied in the field of medicine, can solve the problems of application research and reporting of anti-inflammatory activity of uncompounded compounds

Active Publication Date: 2020-08-11
云南西草资源开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose; 4-O-(3”,4”-di-O-galloyl-α-L-rhamnopyranosyl) ellagic acid; Erythro- guaiacyl-glycerol-β-coniferylaldehyde ether, but the anti-inflammatory activity of this compound and its application in medicine have not been studied and reported, and there is no report on its related preparation method

Method used

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  • Application of three compounds in terminalia in preparation of anti-inflammatory drug and preparation method of compounds
  • Application of three compounds in terminalia in preparation of anti-inflammatory drug and preparation method of compounds
  • Application of three compounds in terminalia in preparation of anti-inflammatory drug and preparation method of compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose and its anti-inflammatory pharmaceutical composition, and its application in medicine.

[0026]

[0027] 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose

[0028] Step 1: Preparation of 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose:

[0029] 50kg Yongde produce the fresh fruit of Myrobalan chebula, and use 3 times the volume of 70% acetone aqueous solution to extract by cold soaking at room temperature for 3 times, each time for 5 days, filter, and the filtrate is concentrated under reduced pressure at 50°C to remove the organic solvent. The remaining aqueous solution was subjected to DiaionHP-20 column chromatography, and gradient elution was carried out with a methanol / water volume ratio of 35% and 60% solution to obtain Fr. 35 , Fr. 60 . Fr. 35 On Sephadex LH-20 chromatography column, use MeOH / H 2 O volume ratio 80% and 90% elution, wherein methanol / water volume ratio 90% elution part carries out MCI-gel CHP...

Embodiment 2

[0033] Preparation of 4-O-(3", 4"-di-O-galloyl-α-L-rhamnopyranosyl) ellagic acid, its anti-inflammatory pharmaceutical composition, and its application in medicine.

[0034]

[0035] 4-O-(3”,4”-di-O-galloyl-α-L-rhamnopyranosyl) ellagic acid

[0036] Step 1: Preparation of 4-O-(3”,4”-di-O-galloyl-α-L-rhamnopyranosyl) ellagic acid

[0037] 50kg Yongde produce the fresh fruit of Myrobalan chebula, and use 3 times the volume of 70% acetone aqueous solution to extract by cold soaking at room temperature for 3 times, each time for 5 days, filter, and the filtrate is concentrated under reduced pressure at 50°C to remove the organic solvent. The remaining aqueous solution was subjected to DiaionHP-20 column chromatography, and gradient elution was carried out with a methanol / water volume ratio of 35% and 60% solution to obtain Fr. 35 , Fr. 60 . Fr. 35 On Sephadex LH-20 chromatography column, use MeOH / H 2 O volume ratio 80% and 90% elution, wherein methanol / water volume ratio...

Embodiment 3

[0041] Preparation of Erythro-guaiacyl-glycerol-β-coniferyl aldehyde ether, its anti-inflammatory pharmaceutical composition, and its application in medicine.

[0042]

[0043] Erythro-guaiacyl-glycerol-β-coniferyl aldehyde ether

[0044] Step 1: Preparation of Erythro-guaiacyl-glycerol-β-coniferyl aldehyde ether

[0045] 50kg Yongde produce the fresh fruit of Myrobalan chebula, and use 3 times the volume of 70% acetone aqueous solution to extract by cold soaking at room temperature for 3 times, each time for 5 days, filter, and the filtrate is concentrated under reduced pressure at 50°C to remove the organic solvent. Under the detection guidance of thin-layer chromatography, the remaining aqueous solution was subjected to Diaion HP-20 column chromatography, and gradient elution was carried out with a methanol / water volume ratio of 35% and 60% solution to obtain Fr. 35 , Fr. 60 . Fr. 60 The MCI-gel CHP20P chromatography column was eluted with a solution with a volume ra...

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Abstract

The invention provides application of compounds with anti-inflammatory activity in terminalia chebula in preparation of an anti-inflammatory drug and a preparation method of the compounds. The preparation method comprises the following steps of obtaining 1, 2, 3, 4, 6-penta-O-galloyl-beta-D-glucopyranose, 4-O-(3", 4"-di-O-galloyl-alpha-L-rhamnopyranosyl) ellagic acid and Erythro-guaiacryl-glycerol-beta-coniferol aldehyde ether from fresh fruits of terminalia chebula; a thin-layer chromatography method is mainly adopted for guiding and other plant chemistry research means and a conventional anti-inflammatory activity evaluation model are combined, the solid, liquid or paste dosage form can be prepared according to the conventional method. The three chemical components are simple and convenient in preparation method, high in yield and excellent in purity, and the obtained compound is a natural secondary metabolite with remarkable anti-inflammatory activity.

Description

Technical field: [0001] The invention belongs to the field of medicine, in particular, it relates to compound 1,2,3,4,6-penta-O-galloyl-β-D-glucopyranose; 4-O-(3",4"-di-O-galloyl- Preparation of α-L-rhamnopyranosyl) ellagic acid; Erythro-guaiacyl-glycerol-β-coniferyl aldehyde ether and its application in anti-inflammatory pharmaceutical composition and its application in medicine. Background technique: [0002] Inflammatory reactions can occur in tissues and organs in various parts of the body. It is an important immune and anti-epidemic mechanism produced by the body after the action of inflammatory factors, which helps to reduce the infection of pathogenic microorganisms. However, when the inflammatory response is out of balance, it will cause damage to tissue cells, causing degeneration and necrosis, resulting in damage to tissues and organs, and promoting the occurrence of diseases. The invasion of pathogenic factors such as avian influenza, SARS, and 2019-nCoV may indu...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61K31/7048A61K31/11A61P29/00C07H1/08C07H13/08C07H17/04C07C45/79C07C47/277
CPCA61K31/7024A61K31/7048A61K31/11A61P29/00C07H1/08C07H13/08C07H17/04C07C45/79C07C47/277A61K2300/00Y02A50/30
Inventor 张颖君朱宏涛张晓芮王东杨崇仁
Owner 云南西草资源开发有限公司
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