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Uses of macrocyclic germacrane sesquiterpenoids in preparation of anticomplementary drugs

A technology of macrocyclic gemmane and sesquiterpenoids, which is applied in the field of traditional Chinese medicine and pharmaceuticals, and can solve the problems that macrocyclic gemmane-type sesquiterpenoids have not yet been discovered.

Inactive Publication Date: 2015-11-25
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous pharmacological studies on Viola dicin only focused on antiviral and antibacterial aspects. The chemical composition research found some flavonoids, coumarins, alkaloids and cyclic peptide compounds, but so far no inhibitory effect on complement has been found. A report on macrocyclic gemmane-type sesquiterpenoids

Method used

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  • Uses of macrocyclic germacrane sesquiterpenoids in preparation of anticomplementary drugs
  • Uses of macrocyclic germacrane sesquiterpenoids in preparation of anticomplementary drugs
  • Uses of macrocyclic germacrane sesquiterpenoids in preparation of anticomplementary drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1. Preparation of macrocyclic guimarane-type sesquiterpenoids

[0026] Take 20kg of dried Viola sibiricum whole plant, crush it, and extract with 95% ethanol at room temperature cold soaking (50L×5 times), combine the extracts and concentrate until there is no alcohol smell, dilute the extract with water to 2.5L, and then use equal volume of petroleum Extract with ether (60-90°C), ethyl acetate, and n-butanol (2.5L×3 times each), combine the petroleum ether extracts and concentrate to dryness to obtain 323 g of petroleum ether extract. The extraction fraction of petroleum ether (200g) was separated by silica gel column chromatography, followed by a gradient of petroleum ether-ethyl acetate (petroleum ether, 50:1, 30:1, 20:1, 10:1, 5:1, 1:1) After elution, 7 fractions (Fr.AG) were obtained, of which fraction Fr.E (22.2g) was subjected to silica gel column chromatography (petroleum ether-ethyl acetate as eluent, 30:1, 20:1, 15 :1,10:1,5:1) and SephadexLH-20 (chlorof...

Embodiment 2

[0027] Example 2. In vitro anti-complement classic pathway test

[0028] Take 0.1ml of complement (guinea pig serum), add barbital buffer (BBS) to make a 1:5 solution, and use BBS to dilute to 1:10, 1:20, 1:40, 1:80, 1: 160, 1:320 and 1:640 solutions. Dissolve 0.1ml each of 1:1000 hemolysin, each concentration of complement and 2% sheep red blood cells (SRBC) in 0.3ml 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 to a 96-well plate, and measure the absorbance at 405nm. The experiment also set up a complete hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml tri-distilled water). The absorbance of the three-distilled water-soluble blood vessel was used as the standard for total hemolysis to calculate the hemolysis rate. Taking complement dilution as the X axis, the percentage of hemolysis caused by each dilution of complement is plotted ...

Embodiment 3

[0029] Example 3. In vitro anti-complement alternative pathway test

[0030] Take 0.2ml of complement (human serum), add AP to dilute (barbital buffer, pH=7.4, containing 5mMMg 2+ , 8mMEGTA) 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, place in a low-temperature high-speed centrifuge after 30min in 37℃ water bath, and centrifuge at 5000rpm and 4℃ for 10min. Take 0.2ml of the supernatant from each tube to a 96-well plate, and measure the absorbance at 405nm. The experiment also set up a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple distilled water). The absorbance of the three-distilled water-soluble blood vessel was used as the standard for total hemolysis to calculate the hemolysis rate. Taking complement dilution as the X axis, the percentage of hemol...

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Abstract

The invention belongs to the field of Chinese pharmaceutical manufacturing and relates to macrocyclic germacrane sesquiterpenoids as shown in the formula I and their novel uses in the preparation of anticomplementary drugs. Three macrocyclic germacrane sesquiterpenoids are separated from a petroleum ether extraction fraction of dried all-grass ethanol extract of Viola yedoensis Makino and are proved to have inhibitory effects of different degrees upon classical and alternative pathways of a complement system. The sesquiterpenoids can be prepared into anticomplementary drugs and further be prepared into drugs for treating complement-related diseases.

Description

Technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a macrocyclic gimarane-type sesquiterpenoid compound in Viola fragrans and its new use in preparing anti-complement drugs. Background technique [0002] Excessive activation of the complement system can cause systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other major diseases. Anti-complement drug research is the hotspot and focus of pharmaceutical research in the world. However, there is still a lack of ideal therapeutic drugs for such diseases. In clinical practice, there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors. In recent years, the research and development of complement inhibitors from natural products has attracted more and more attention in this research field. The natural products have the characteristics of low cost and low toxicity. Scholars at home and abroad hav...

Claims

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Application Information

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IPC IPC(8): A61K31/11A61P37/02A61P19/04A61P19/02A61P29/00A61P11/00C07C45/78C07C47/46
Inventor 程志红陈道峰杜冬生
Owner FUDAN UNIV
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