Uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs

A compound, phenylpropanoid technology, applied in the field of aryl-substituted phenylpropanoid compounds to prepare anti-complement drugs, which can solve problems such as excessive activation of the autoimmune system

Active Publication Date: 2017-04-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Studies have shown that the above-mentioned diseases and pharmacological activities related to the treatment of Gangmegen are mostly related to the complement system, and the complement system plays a very important role in maintaining the balance of the body and eliminating foreign organisms. Many pathogenic microorganisms can cause disease in the human body. Excessive activation of the autoimmune system of the human body can lead to serious consequences, such as SARS, influenza, rheumatoid arthritis, etc. Therefore, it is particularly necessary to find low-toxicity and high-efficiency complement inhibitors from traditional Chinese medicines for the treatment of related diseases

Method used

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  • Uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs
  • Uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs
  • Uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs

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Experimental program
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Effect test

Embodiment 1

[0032] Embodiment 1. Preparation of phenylpropanoid compounds

[0033]Take 19 kg of root plum, heat and reflux with 95% ethanol to extract 3 times, suspend the extract with water after concentration, and extract with petroleum ether, ethyl acetate, and n-butanol respectively to obtain 135 g of ethyl acetate in the active part, and take 120 g of the extract to dry The method was applied to silica gel column chromatography, eluted with dichloromethane-methanol gradient (100:1→1:1), and the Fr.3 fraction eluted with dichloromethane-methanol (25:1) was reversed by ODS Column methanol / water (20% → 100%) for gradient elution, ultraviolet 210nm as the detection wavelength, a total of Fr.3 (1-8) fractions, Fr.3.4 and dichloromethane-methanol (20:1) Silica gel column chromatography and Sephadex LH-20 were carried out isocratically to separate, and finally HPLC was used to prepare the liquid phase for purification, and acetonitrile / water (32%) was used as the preparation condition to ob...

Embodiment 2

[0036] Example 2. Anti-complement classical pathway test in vitro

[0037] Take 0.1ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to prepare a 1:10 solution, and double-dilute with BBS to 1:20, 1:40, 1:80, 1:160, 1:10 320, 1:640 and 1:1280 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, put in 37℃ water bath for 30min Centrifuge at 5000rpm and 4°C for 10min in a low-temperature high-speed centrifuge; take 0.2ml of the supernatant from each tube and put it in a 96-well plate, and measure its absorbance at 405nm; set up a full hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml Triple-distilled water), using the absorbance of triple-distilled water lysed blood vessels as the standard of total hemolysis, calculate the hemolysis rate, take the dilution of complement as the X-axis, and the percentage of hemolysis as the Y-axis to draw a graph, and select the ...

Embodiment 3

[0038] Example 3. Anti-complement alternative pathway test in vitro

[0039] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mMMg 2+ , 8mM EGTA) to prepare a 1:1 solution, and double-dilute it into a 1:2, 1:4, 1:8, 1:16, 1:32, 1:64 and 1:128 solution; take 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 at 37°C for 30 minutes, and centrifuge at 5000rpm and 4°C for 10 minutes; take the supernatant of each tube separately 0.2ml was placed in a 96-well plate, and the absorbance was measured at 405nm. At the same time, a complete hemolysis group (0.20ml 0.5% RE dissolved in 0.3ml triple-distilled water) was set up in the experiment. The complement dilution is plotted on the X-axis, and the percentage of hemolysis is plotted on the Y-axis. The lowest complement concentration that achieves a similarly high hemolysis rate...

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Abstract

The present invention relates to the field of traditional Chinese medicine pharmacy, particularly to uses of aryl-substituted phenylpropanoid-based compounds in preparation of anti-complement drugs. According to the present invention, the aryl-substituted phenylpropanoid-based compounds 1-3 are extracted from the root of an Aquifoliaceae plant Ilexasprella by using an activity guide separation method, and the results of the classical pathway anti-complement activity evaluation test and the alternative pathway anti-complement activity evaluation test show that the compounds provide strong inhibition effects for the classical pathway and the alternative pathway of the complement system, wherein the inhibition effect on the classical pathway (CH50) is 0.032-0.059 mg/ml, and the inhibition effect on the alternative pathway (AP50) is 0.061-0.275 mg/ml; and the compounds can be used for preparing anti-complement drugs and further preparing drugs for treatment of complement-related diseases.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the use of aryl-substituted phenylpropanoid compounds isolated and identified from the traditional Chinese medicine Gangmei in the preparation of anti-complement drugs. Background technique [0002] Gangmeigen is the dried root of Ilexasprella (Hook. et Arn.) Champ.ex Benth., a plant of the Ilex family. It has the effects of clearing away heat and detoxification, relieving sore throat and reducing swelling, dissipating blood stasis and relieving pain. Gangmeigen is mainly used clinically for respiratory diseases, and played a more active role in the fight against SARS. According to data, some Chinese patent medicines use Gangmeigen as the main drug, such as Qingkailing, Gangmeigenqing Throat Granules, etc. This Chinese patent medicine can be used for acute and chronic pharyngitis, tonsillitis, laryngitis, and throat swelling and pain caused by cold and fever, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/09A61P37/02A61P29/00A61P19/02A61P31/16A61P11/00C07C43/23C07C41/34
CPCA61K31/09C07C41/34C07C43/23
Inventor 陈道峰温泉卢燕
Owner FUDAN UNIV
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