Application of anthraquinone compound in preparation of anticomplement medicine

A compound and anthraquinone technology are applied in the field of new use of anthraquinone compounds in the preparation of anti-complement drugs, and can solve the problems such as no reports of anti-complement active compounds.

Inactive Publication Date: 2014-09-17
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, a series of anthraquinones, naphthoquinones, stilbenes and flavonoids have been isolated from Polygonum cuspidatum, but no anti-complement active compounds have been reported

Method used

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  • Application of anthraquinone compound in preparation of anticomplement medicine
  • Application of anthraquinone compound in preparation of anticomplement medicine
  • Application of anthraquinone compound in preparation of anticomplement medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation of embodiment 1 anthraquinone compound

[0029] Polygonum cuspidatum root coarse powder 16kg, extract 3 times with 5 times of amount 95% ethanol 50 ℃, each 2 hours. The solvent was recovered under reduced pressure to obtain 950 g of extract, which was suspended in distilled water and extracted with petroleum ether, ethyl acetate and n-butanol to obtain 400 g of ethyl acetate extract. Take 200g of ethyl acetate extract and go through silica gel column chromatography, eluting with dichloromethane, dichloromethane-methanol, methanol gradient, and the obtained fraction is subjected to repeated silica gel column chromatography through recrystallization or different eluents, polyamide, RP- 18 Preparative chromatography and SephadexLH-20 purification, isolated compounds emodin (1), emodin-8-methyl ether (2), Emodin-8-O-β-D-glucoside (3), Fallacinol (4), Citreorosein (5), and Xanthorin (6).

[0030] Specific steps are as follows:

[0031] 1. The obtained frac...

Embodiment 2

[0037] Example 2 Anti-complement classical pathway test in vitro

[0038] Take 0.1ml of complement (guinea pig serum), add BBS buffer to make a 1:5 solution, and double-dilute with BBS to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solution. Take 0.1ml each of 1:1000 hemolysin and 2% SRBC, and dissolve 0.2ml of each concentration of complement in 0.2ml BBS, mix well, put it in a low-temperature high-speed centrifuge after 30 minutes in a 37°C water bath, and centrifuge at 5000rpm and 4°C 10min. 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 (0.1ml 2% SRBC dissolved in 0.5ml triple distilled water) was set up. 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 comple...

Embodiment 3

[0040] Example 3 Anti-complement alternative pathway test in vitro

[0041] 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. 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 a...

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Abstract

The invention belongs to the field of pharmacy and relates to a new application of an anthraquinone compound in the preparation of an anticomplement medicine. According to the invention, the anthraquinone compound is prepared from an ethyl acetate extracted part of roots of Polygonum cuspidatum Sieb.et Zucc., and it proves through an evaluation test of in vitro anticomplement activity that the anthraquinone compound has a strong effect of inhibiting classical pathway and alternative pathway of a complement system. Under the inhibitory effect of the compound to the classical pathway and the alternative pathway of complement system, concentration of complement tested by CH50 is 6+ / -2-500+ / -25 microgram / ml and concentration of complement tested by AP50 50+ / -5-350+ / -20 microgram / ml. The compound can be used in preparation of an anticomplement medicine.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a new application of anthraquinone compounds in preparing anti-complement drugs. Background technique [0002] The complement system is an important immune defense system in the body and participates in most pathophysiological processes in the body. The complement system is a double-edged sword. Its normal activation plays an important role in resisting the invasion of foreign microorganisms and maintaining the balance of the body. However, excessive activation of the complement system can cause systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. symptoms and many other diseases. 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 develo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61K31/704A61P37/02A61P19/04A61P29/00A61P19/02A61P11/00
Inventor 陈道峰沈路路卢燕
Owner FUDAN UNIV
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