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Dipeptide compound and use of the same in preparation of anti-complement drugs

A compound and anti-complement technology, applied in drug combination, antipyretics, anti-inflammatory agents, etc., can solve problems such as compounds that have not yet seen complement inhibition

Inactive Publication Date: 2014-01-15
FUDAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, the pharmacological research on violadin only focuses on antiviral and antibacterial aspects, and some flavonoids, coumarins and cyclic peptide compounds have been found in the research on its chemical constituents, but so far no traditional Chinese medicine violadin has been found. Reports disclosing compounds with complement inhibitory effects in

Method used

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  • Dipeptide compound and use of the same in preparation of anti-complement drugs
  • Dipeptide compound and use of the same in preparation of anti-complement drugs
  • Dipeptide compound and use of the same in preparation of anti-complement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1. Preparation of dipeptide compounds

[0021] Take 20kg of dried Viola chinensis, crush it, soak it in 95% ethanol at room temperature (50L×5 times), combine the extracts and concentrate until there is no alcohol smell, add water to dilute the extract to 2.5L, and then add an equal volume of petroleum ether (60-90°C), ethyl acetate, n-butanol extraction (each 2.5 L x 3 times), combined ethyl acetate extracts and concentrated to dryness to obtain 180 g of ethyl acetate extract. The ethyl acetate extraction part was separated by silica gel (200-300 mesh) column chromatography, followed by petroleum ether-acetone (petroleum ether, 50:1, 30:1, 20:1, 10:1, 5:1, 1:1 ) gradient elution to obtain 7 fractions (Fr1-7), of which fraction Fr.4 (21.5g) was subjected to silica gel column chromatography (petroleum ether-ethyl acetate as eluent, 30:1, 20:1 , 15:1, 10:1, 5:1) and Sephadex LH-20 (chloroform-methanol, 1:1) were repeatedly purified, and two compounds were isol...

Embodiment 2

[0024] Example 2. Anti-complement classical pathway test in vitro

[0025] Take 0.1ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare 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 solutions. Take 1:1000 hemolysin, 0.1ml of each concentration of complement and 2% sheep red blood cells (SRBC) and dissolve them in 0.3ml of BBS, mix well, put them in a low-temperature high-speed centrifuge at 5000rpm, 4°C after 30min in 37°C water bath Centrifuge for 10 min under conditions. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure its 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 ...

Embodiment 3

[0026] Example 3. Anti-complement alternative pathway test in vitro

[0027] Take 0.2ml of complement (human serum), add AP to dilute (barbital buffer, pH=7.4, containing 5mM Mg 2+ , 8mM EGTA) solution was prepared into a 1:5 solution, and double-diluted into 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solutions. Take 0.15ml of complement of each concentration, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit erythrocytes (RE), mix well, put 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. A full hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml 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...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation, and relates to a dipeptide compound represented by a formula I and a new use of the dipeptide compound in preparation of anti-complement drugs. According to the present invention, the dipeptide compound is separated from the ethyl acetate extraction position of the ethanol extract of the dry whole herb Viola yedoensis Makino, and results confirm that the dipeptide compound provides inhibition effects for the classical pathway and the alternative pathway of the complement system, wherein the inhibition effect on the classical pathway (CH50) is 0.21-0.23 mg / ml, and the inhibition effect on the alternative pathway (AP50) is 0.33-0.41 mg / ml; and the dipeptide compound can be adopted as the drug active component to be adopted to prepare the anti-complement drug so as to be further adopted to treat systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases initiated by excessive activation of the complement system.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a dipeptide compound in violadin and its new application in preparing anti-complement drugs. Background technique [0002] The prior art discloses that excessive activation of the complement system can lead to various serious diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. Over the years, the research on anti-complement drugs has been the focus and focus of the world's pharmaceutical research. However, so far, there is still a lack of ideal therapeutic drugs for systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases in clinical treatment. agent. The research and development of complement inhibitors from natural products is an important research field that has received more and more attention in recent years, and it has the characteristics of low co...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C237/22C07C231/24A61K31/222A61K31/166A61P37/02A61P29/00A61P19/02A61P11/00
Inventor 陈道峰程志红杜冬生
Owner FUDAN UNIV
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