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Application of toluylene compounds in preparation of anticomplement medicaments

A technology of stilbenes and compounds, applied in the direction of active ingredients of hydroxyl compounds, drug combinations, antipyretics, etc.

Inactive Publication Date: 2014-09-24
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 there is no report on the anti-complement activity of stilbenes

Method used

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  • Application of toluylene compounds in preparation of anticomplement medicaments
  • Application of toluylene compounds in preparation of anticomplement medicaments
  • Application of toluylene compounds in preparation of anticomplement medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Preparation of stilbene compounds

[0024] Polygonum cuspidatum root coarse powder 16kg, extracted 3 times with 5 times the amount of 95% ethanol at 50 o C, each time for 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-butyl Alcohol extraction to obtain 400 g of ethyl acetate extract; 200 g of ethyl acetate extract was subjected to silica gel column chromatography, and gradient elution was performed with dichloromethane, dichloromethane-methanol, and methanol, and the obtained fractions were repeatedly subjected to different eluents. Silica gel column chromatography, RP-18 preparative chromatography and SephadexLH-20 purification, isolate compound resveratrol ( 1 ), polydatin ( 2 );

[0025] Specific steps are as follows:

[0026] 1. The obtained fraction was eluted with dichloromethane-methanol (5:1), and after repeated c...

Embodiment 2

[0028] Example 2 Anti-complement classical pathway test in vitro

[0029] 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 0.1 ml each of 1:1000 hemolysin and 2% SRBC, and dissolve 0.2 ml of each concentration of complement in 0.2 ml BBS, mix well, put into a low-temperature high-speed centrifuge after 30 min in a 37 oC water bath, and spin at 5000 rpm centrifuge at 4 oC for 10 min; take 0.2 ml of supernatant from each tube and place in a 96-well plate, and measure the absorbance at 405 nm; set up a complete hemolysis group (0.1 ml of 2% SRBC dissolved in 0.5 ml of three-distilled water); The absorbance of distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated; the dilution of complement was taken as the X-axis, and the percentage of hemolysis caused by each dilution of complement was p...

Embodiment 3

[0031] Example 3 In vitro anti-complement alternative pathway assay

[0032] Take 0.2 ml 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 0.15 ml of each concentration of complement, 0.15 ml of AP diluent, and 0.20 ml of 0.5% RE, mix well, place in a low-temperature high-speed centrifuge after 30 min in a 37 oC water bath, and centrifuge at 5000 rpm and 4 oC for 10 min; take 0.2 ml of supernatant from each tube in a 96-well plate, and measure the absorbance at 405 nm. At the same time, a complete hemolysis group (0.20 ml 0.5% RE dissolved in 0.3 ml three-distilled water) was set up, and the absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis to calculate the hemolysis rate; the dilution degree of complement was taken as the X-axis, and the percentage of the hemolysis caused by each dilution concentration was calcul...

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Abstract

The invention belongs to the field of pharmacy, and relates to a new application of toluylene compounds in preparation of anticomplement medicaments. According to the invention, toluylene compounds are prepared from ethyl acetate extraction positions of roots of polygonum cuspidatum Sieb. et Zucc., and are confirmed to have strong inhibition effect on the classical pathway and the alternative pathway of the complement system by in-vitro anticomplement activity evaluation tests. The CH50 of the compounds for the inhibition effect on the classical pathway of the complement system is 110+ / - 12, 250+ / -20 [mu]g / ml, and the AP50 for the inhibition effect on the alternative pathway of the complement system is 800+ / -25, 440+ / -15 [mu]g / ml. The compounds can be used for preparation of anticomplement medicaments.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy and relates to a new application of stilbene compounds in the preparation of 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. It is low cost and safe to rese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61K31/7034A61P37/02A61P19/04A61P29/00A61P19/02A61P11/00
Inventor 陈道峰沈路路卢燕
Owner FUDAN UNIV
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