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

A compound and anti-complement technology, applied in the direction of drug combination, antipyretics, anti-inflammatory agents, etc.

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

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Problems solved by technology

The pharmacological research on violadin is currently focused on antiviral and antibacterial aspects, and some flavonoids, coumarins and cyclic peptide compounds have been found in t

Method used

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

Examples

Experimental program
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Effect test

Embodiment 1

[0025] Embodiment 1. Preparation of alkaloid compounds

[0026] Take 20kg of dried Viola chinensis, crush it, and soak it in 95% ethanol at room temperature (50L x 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 4 compounds were i...

Embodiment 2

[0031] Example 2. Anti-complement classical pathway test in vitro

[0032] 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 into a low-temperature high-speed centrifuge after 30 minutes in a water bath at 37°C, and put them in a low-temperature high-speed centrifuge at 5000rpm, 4°C 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 w...

Embodiment 3

[0033] Example 3. Anti-complement alternative pathway test in vitro

[0034] 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 red blood cells (RE), mix well, put in a low-temperature high-speed centrifuge at 5000rpm and 4°C for 10min after bathing in 37°C water for 30min. 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 as the X-axis, th...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation, and relates to an alkaloid compound represented by a formula I and a new use of the alkaloid compound in preparation of anti-complement drugs. According to the present invention, the alkaloid 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 alkaloid 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 0.16-0.31 mg/ml, and the inhibition effect on the alternative pathway (AP50) is 0.26-0.46 mg/ml; and the alkaloid 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 alkaloid compounds in Viola chinensis and their new application in preparing anti-complement drugs. Background technique [0002] The study of anti-complement drugs has been the focus and focus of pharmaceutical research in the world for many years. Studies have reported that overactivation of the complement system can cause many major diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. At present, there is still a lack of ideal therapeutic drugs for such diseases, so there is an urgent need for new types of complement inhibitors with high efficiency, low toxicity and specificity in clinical practice. 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 cos...

Claims

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Application Information

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IPC IPC(8): C07C235/34C07C231/24A61K31/165A61P37/02A61P19/04A61P29/00A61P11/00
Inventor 程志红陈道峰杜冬生
Owner FUDAN UNIV
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