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Use of aryl-substituted acryloyl triterpenoids in the preparation of anti-complement drugs

A technology of acryloyl triterpenoids and compounds, which is applied in the field of preparation of anti-complement drugs and aryl-substituted acryloyl triterpenoids, and can solve problems that have not yet been seen

Active Publication Date: 2019-02-26
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In recent years, there have been many studies on the chemical constituents and biological activities of the ethanol extract of Prunus mellifera, but so far there has been no research on the ethanol extract of Plum mellifera, especially the aryl-substituted acryloyl triterpenoids as complement inhibitory compounds. to report

Method used

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  • Use of aryl-substituted acryloyl triterpenoids in the preparation of anti-complement drugs
  • Use of aryl-substituted acryloyl triterpenoids in the preparation of anti-complement drugs
  • Use of aryl-substituted acryloyl triterpenoids in the preparation of anti-complement drugs

Examples

Experimental program
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Effect test

Embodiment 1

[0030] Embodiment 1. Preparation of aryl-substituted acryloyl triterpenoids

[0031]Take 19kg of Plum root, heat and reflux with 95% ethanol to extract 3 times, suspend the extract with water after concentration, extract with petroleum ether, ethyl acetate, and n-butanol respectively to obtain 135g of ethyl acetate in the active part, take 120g of the extract for extraction Silica gel column chromatography, eluting with dichloromethane-methanol gradient (100:1→1:1). The fraction of Fr.4 eluted with dichloromethane-methanol (10:1) was then passed through an ODS reverse column, followed by gradient elution with methanol / water (20% → 100%), with ultraviolet 210nm as the detection wavelength, and a total of Fr .4 (1-6) 6 fractions, Fr.3 also carried out gradient elution through ODS column methanol / water (30% → 100%) to obtain Fr.3 (1-8) fractions, Fr.4.5 again Using a silica gel column dichloromethane-acetone-methanol (20:2:1) for isocratic elution and separation, the compound As...

Embodiment 2

[0032] Example 2. Anti-complement classical pathway test in vitro

[0033] 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, 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 after 30 minutes in a water bath at 37°C, and put them in a low-temperature high-speed centrifuge at 5000rpm and 4°C. Centrifuge for 10 min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure its absorbance at 405nm. At the same time, a complete hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml triple distilled water) was 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...

Embodiment 3

[0034] Example 3. Anti-complement alternative pathway test in vitro

[0035] Take 0.2ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5mM Mg 2+ ,8mMEGTA) was prepared as a 1:1 solution, and double-diluted into 1:2, 1:4, 1:8, 1:16, 1:32, 1:64 and 1:128 solutions. Take 0.15ml of complement of each concentration, 0.15ml of AP diluent and 0.20ml of 0.5% rabbit erythrocytes (RE), mix them evenly, put them in a low-temperature high-speed centrifuge at 37°C for 30min, and centrifuge at 5000rpm and 4°C for 10min. Take 0.2ml of the supernatant from each tube and place it in a 96-well plate, and measure the absorbance 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 absorbance of three-distilled water lysed blood vessels was used as the standard of total hemolysis, and the hemolysis rate was calculated. Plot the dilution of complement on the X-axis and...

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Abstract

The invention belongs to the field of traditional Chinese medicine preparation and relates to a new application of aryl substitute acryl triterpenoids in roots of radix ilex asprella to preparation of anticomplement drugs. Five aryl substitute acryl triterpenoids are extracted from roots of Aquifoliaceae plant ilex asprella with a bioassay guided isolation method, and the result of evaluation of anticomplement activity of the compounds for a classic pathway and an alternative pathway indicates that the inhibition effect (CH50) of the compounds for the classic pathway of a complement system is 0.058-0.130 mg / ml and the inhibition effect (AP50) of the compounds for the alternative pathway is 0.080-0.390 mg / ml. The compounds can be used for preparing the anticomplement drugs.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to the use of aryl-substituted acryloyl triterpenoids isolated and identified from the traditional Chinese medicine Gangmei in the preparation of anti-complement drugs. Background technique [0002] The prior art discloses that Gangmegen is the dry root of Ilex asprella (Hook.et Arn.) Champ.ex Benth., a plant of the family Ilex (Aquifoliaceae), which is a commonly used heat-clearing and detoxifying drug in Lingnan, and can relieve throat and detumescence , The effect of dissipating blood stasis and relieving pain. Gangmegen is widely used clinically. Many Chinese patent medicines use Gangmegen as the main drug, such as Qingkailing, Gangmegen Qinghou Granules, etc. It can be used for acute and chronic pharyngitis, tonsillitis, laryngitis and It is more effective for diseases such as sore throat and sore throat caused by cold and fever. The prior art also discloses...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J63/00A61K31/56A61P37/02
Inventor 陈道峰温泉卢燕
Owner FUDAN UNIV
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