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Application of flavan compound in preparing anti-complement medicines

A kind of compound and flavan technology, which is applied in the new application field of flavan compounds in the preparation of anti-complement drugs

Inactive Publication Date: 2013-05-08
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 flavonoids, tannins and flavans, etc., but there is no report that they have an inhibitory effect on the complement system

Method used

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  • Application of flavan compound in preparing anti-complement medicines
  • Application of flavan compound in preparing anti-complement medicines
  • Application of flavan compound in preparing anti-complement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 prepares flavan compound

[0029] (1) Take 14kg of Commelina chinensis, 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 use petroleum ether, ethyl acetate, n-butyl Alcohol extraction (each 2 L x 3 times), the combined n-butanol extracts were concentrated to dryness to obtain 19.2 g of n-butanol extracts. The n-butanol part was subjected to silica gel column chromatography, eluted with petroleum ether (60-90°C), petroleum ether-acetone, and acetone gradient, and the fraction was purified by repeated column chromatography and SephadexLH-20 to obtain flavan compounds (1). Specific steps are as follows:

[0030] The obtained fraction was eluted with petroleum ether-acetone (2:1), and purified by Sephadex LH-20 to obtain compound 1 (4 mg). Using spectral analysis, its structure was determined to be p-catechin-3-O-β-D-(2-cinnamoyl)-glucopy...

Embodiment 2

[0035] Example 2 Anti-complement classical pathway test in vitro

[0036] Take 0.1ml of complement (guinea pig serum), add BBS to prepare a 1:5 solution, and dilute it to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:320 with BBS 640 solution. Dissolve 1:1000 hemolysin, 0.1ml of each concentration of complement and 2% SRBC in 0.3ml BBS, mix well, put in a low-temperature high-speed centrifuge after 30min in a 37°C water bath, and centrifuge at 5000rpm and 4°C for 10min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure the absorbance at 405nm. A full hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml triple distilled water) was also set up in the experiment. The absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of complement is plotted as the Y-axis. ...

Embodiment 3

[0037] Example 3 Anti-complement alternative pathway test in vitro

[0038] Take 0.2ml of complement (human serum), add AP diluent to prepare a 1:5 dilution solution, and double-dilute to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solution. Take 0.15ml of complement of each concentration, 0.15ml of AP diluent and 0.20ml of 0.5% RE, mix well, place in a low-temperature high-speed centrifuge after 30 minutes in a 37°C water bath, and centrifuge at 5000rpm and 4°C for 10 minutes. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure the absorbance at 405nm. At the same time, a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple distilled water) was set up in the experiment. The absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of compl...

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Abstract

The invention belongs to the field of pharmacy, and relates to a novel application of a flavan compound in preparing anti-complement medicines. According to the invention, a modern pharmacological screening method is applied, and researches are carried out upon anti-complement active substances in plant medicines. According to the invention, the flavan compound is obtained by separation from an n-butanol extract of a commelinaceae plant commelina and an n-butanol extract of a polygonum plant fagopyrum. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the inhibition effect of the compound upon the classical pathway of the complement system is 0.13 (plus or minus 0.03)-0.78 (plus or minus 0.06) mM, and the AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.12 (plus or minus 0.01)-1.00 (plus or minus 0.15) mM. The compound can be used for preparing anti-complement medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy and relates to a new application of flavan compounds in the preparation of anti-complement drugs. Background technique [0002] The prior art discloses that excessive activation of the complement system can cause various diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. 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 therapeutic drug for this kind of disease in clinical practice. Therefore, there is an urgent need for a new type of complement inhibitor with high efficiency, low toxicity and specificity. Studies have shown that 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 the body as part of natura...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/353A61P37/02A61P19/04A61P29/00A61P11/00
Inventor 陈道峰金家宏
Owner FUDAN UNIV
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