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Application of germacrane lactone sesquiterpenoid compounds to preparing anti-complement medicine

A technology of sesquiterpenoids and compounds, applied in the field of preparation of anti-complement drugs

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

In the prior art, the pharmacological research on Viola ditin only focuses on antiviral and antibacterial aspects, and some flavonoids, coumarins, alkaloids and cyclic peptides have been found in the chemical composition research, but no one has been found so far. Reports of Gemarane Lactone Sesquiterpenoids with Complement Inhibition

Method used

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  • Application of germacrane lactone sesquiterpenoid compounds to preparing anti-complement medicine
  • Application of germacrane lactone sesquiterpenoid compounds to preparing anti-complement medicine
  • Application of germacrane lactone sesquiterpenoid compounds to preparing anti-complement medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1. Preparation of Gemarane Lactone Sesquiterpenoids

[0029] 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, and n-butanol extraction (2.5 L x 3 times each), combined petroleum ether extracts and concentrated to dryness to obtain 323 g of petroleum ether extracts. Petroleum ether extraction fraction (200g) was separated by silica gel column chromatography, followed by petroleum ether-ethyl acetate (petroleum ether, 50:1, 30:1, 20:1, 10:1, 5:1, 1:1) gradient Eluted to obtain 7 fractions (Fr.A-G), wherein 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 (chloroform-methanol, 1:1) were repeatedly purified, and final...

Embodiment 2

[0030] Example 2. Anti-complement classical pathway test in vitro

[0031] 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, each concentration of complement and 2% sheep red blood cell (SRBC) each 0.1ml dissolved in 0.3ml BBS, mix well, 37 ℃ water bath for 30min, then put into low temperature Centrifuge in a high-speed centrifuge at 5000rpm and 4°C for 10min, take 0.2ml of the supernatant from each tube and put it in a 96-well plate, measure its absorbance at 405nm, and set up a full hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml three-distilled water), using the absorbance of three-distilled water lysed blood vessels as the standard of full hemolysis, calculate the hemolysis rate, take the dilution of complement as the X-axis, and the percentage of hemolysis caused by each dilution of complement as the ...

Embodiment 3

[0032] Example 3. Anti-complement alternative pathway test in vitro

[0033] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH7.4, containing 5mMMg 2+ ,8mMEGTA) 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, and each concentration of complement 0.15ml, 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 after 30min in 37℃ water bath, centrifuge at 5000rpm and 4℃ for 10min, and take the supernatant of each tube separately Put 0.2ml in a 96-well plate, measure the absorbance at 405nm, set up a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple distilled water) at the same time, use the absorbance of triple distilled water lysed blood vessels as the standard of complete hemolysis, calculate the hemolysis rate, Take the dilution of complement as the X-axis, and the percentage of hemolysis caused by...

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Abstract

The invention belongs to the field of Chinese pharmaceutical manufacturing, and relates to sesquiterpenoid compounds in a formula I and application of the sesquiterpenoid compounds to preparing anti-complement medicine. Five germacrane lactone sesquiterpenoid compounds are separated from petroleum ether extraction parts of dry whole-herb ethanol extracts of violaceae plants, namely, viola yedoensis makino, it is proved that suppression effects can be realized by the other compounds for classical pathways and alternative pathways of complement systems except for aristolactone (4) (which only is active for the classical pathways of the complement systems), and the germacrane lactone sesquiterpenoid compounds can be used for preparing the anti-complement medicine and further preparing medicine for treating complement-related diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a gemane lactone sesquiterpene compound in violadin and its new application in the preparation of 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. The study of anti-complement drugs has been the focus and focus of the world's pharmaceutical research for many years. However, there is still a lack of ideal therapeutic drugs for such diseases at present, so there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors 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 th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61P37/02A61P29/00A61P19/02A61P11/00C07D493/06C07D307/93
Inventor 陈道峰程志红杜冬生
Owner FUDAN UNIV
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