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Application of phenol compounds in preparation of anti-complement medicines

A phenolic compound and compound technology are applied in the field of phenolic compounds and their new uses in the preparation of anti-complement drugs, and can solve the problems such as the anti-complement effect of phenolic compounds that have not been seen yet.

Inactive Publication Date: 2011-11-23
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemical composition research shows that the main components are tannins, and there are no reports on phenolic compounds and their anti-complement effects

Method used

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  • Application of phenol compounds in preparation of anti-complement medicines
  • Application of phenol compounds in preparation of anti-complement medicines
  • Application of phenol compounds in preparation of anti-complement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1 Preparation of phenolic compounds

[0040]Take 14kg of Commelina chinensis, soak in ethanol at room temperature (50L×5 times), combine the extracts and concentrate until there is no alcohol smell, dilute the extracts with water to 2L, and extract with petroleum ether, ethyl acetate, and n-butanol in sequence ( Each 2L x 3 times), the combined n-butanol extracts were concentrated to dryness to obtain 19.2g of n-butanol extracts; , acetone gradient elution, and the fractions were subjected to repeated column chromatography, SephadexLH-20 purification and preparative chromatography to obtain phenolic compounds ( 1 )and( 2 ),Specific steps are as follows:

[0041] ① The obtained fractions were eluted with petroleum ether-acetone (5:1). After repeated column chromatography, using chloroform-methanol as eluent, gradient elution, the fractions were purified by SephadexLH-20 and eluted with methanol to obtain the compound ( 1 ) (7 mg). Using spectroscopic anal...

Embodiment 2

[0043] The preparation of embodiment 2 phenolic compounds

[0044] Take 20kg of dried roots of Comfrey, and the coarse powder is cold soaked and percolated several times with 95% ethanol at room temperature, and then the solvent is recovered under reduced pressure to obtain 820g of extract, which is suspended in distilled water and mixed with petroleum ether and ethyl acetate. Ethyl acetate and n-butanol were extracted to obtain 420 g of ethyl acetate extract; 180 g of ethyl acetate extract was subjected to silica gel column chromatography, and petroleum ether (60-90°C), petroleum ether (60-90°C)-acetone, acetone gradient Elution, the resulting fraction was subjected to repeated silica gel column chromatography with different eluents, purified by SephadexLH-20 and separated by preparative chromatography to obtain the compound ( 3 ), ( 4 ), ( 5 )and( 6 ),Specific steps are as follows:

[0045] ① The fractions eluted with petroleum ether-acetone (3:1) were subjected to sili...

Embodiment 3

[0048] Example 3 Preparation of phenolic compounds

[0049] Take 15kg of golden buckwheat rhizome powder, cold-soak with ethanol at room temperature (50L×5 times), combine the extracts and concentrate until there is no alcohol smell, add water to dilute the extracts to 2L, and extract with petroleum ether, ethyl acetate, and n-butanol in sequence ( 2L × 4 times each), the combined n-butanol extracts were concentrated to dryness to obtain 790 g of n-butanol extracts; 220 g of n-butanol fractions were dry-loaded for silica gel column chromatography, and chloroform, chloroform-methanol , methanol gradient elution, the obtained fractions were subjected to repeated silica gel column chromatography with different eluents, SephadexLH-20 purification and preparative chromatography, and the compound ( 7 ), ( 8 )and( 9 ).

[0050] ① The obtained fractions were eluted with chloroform-methanol (10:1), subjected to silica gel column chromatography, petroleum ether-acetone (4:1) was used...

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to phenol compounds represented by a formula I and novel purposes of the compounds in the preparations of anti-complement medicines. According to the invention, phenol active substances are separated from n-butyl alcohol site of ethanol extract of commelinaceae commelina commelina communis Linn., ethyl acetate site of ethanol extract of boraginaceae arnebia arnebia euchroma (Royal) Johnst dried root, and n-butyl alcohol site of ethanol extract of polygonaceae fagopyrum fagopyrum dibotrys (D. Don) Hara dried rhizome. As a result of in vitro anti-complement activity selection experiments, the compounds have substantial inhibitive effects against classical pathways and alternative pathways of complement systems. CH50 of the inhibitive effects of the compounds against classical pathways of complement systems are 41+-8mug / ml to 278+-11mug / ml. AP 50 of the inhibitive effects of the compounds against alternative pathways of complement systems are 39+-5mug / ml to 761+-110mug / ml. The compounds can be applied in the preparation of anti-complement medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to phenolic compounds and their new application in the preparation of anti-complement drugs; the phenolic compounds are derived from Commelina chinensis, comfrey or golden buckwheat. Background technique [0002] Excessive activation of the complement system can lead to systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases. The study of anti-complement drugs has been the focus and focus of the world's pharmaceutical research for many years. At present, there is no ideal drug for the treatment of such diseases, so there is an urgent need for a new type of complement inhibitor with high efficiency, low toxicity and specificity in clinical practice. The cost of researching and developing complement inhibitors directly from natural products is low, and most active ingredients can be directly digested and absorbed by...

Claims

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Application Information

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IPC IPC(8): C07C39/07C07C39/04C07C37/70C07C43/23C07C41/34C07C69/84C07C67/48
Inventor 陈道峰金家宏
Owner FUDAN UNIV
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