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Application of phenolic glycoside compounds in anticomplement medicine preparation

A technology of compounds and phenolic glycosides, which is applied in the field of traditional Chinese medicine and pharmaceuticals, and can solve problems such as anti-complement activity that has not yet been seen

Inactive Publication Date: 2017-12-12
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Modern pharmacological studies have shown that paeonol has anticoagulant, antihypertensive, anti-inflammatory, and inhibitory effects on the central nervous system, but there is no report on its anti-complement activity

Method used

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  • Application of phenolic glycoside compounds in anticomplement medicine preparation
  • Application of phenolic glycoside compounds in anticomplement medicine preparation
  • Application of phenolic glycoside compounds in anticomplement medicine preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1. Preparation of phenolic glycosides

[0029] Take 20 kg of Cortex paeonol, crush it, soak it with 95% ethanol at room temperature (40 L × 3 times), combine the extracts and concentrate to obtain 2.6 kg of extract, take 1.0 kg of extract, add water to suspend, and successively dilute with equal volume Extract with ethyl acetate and n-butanol (each 2.0 L x 5 times), combine the extracts and concentrate to dryness to obtain 390 g of ethyl acetate extract and 260 g of n-butanol extract. Take the n-butanol extract and add water to suspend it, load the sample on Diaion HP-20 resin, and elute with water, 25%, 50%, 75%, and 100% methanol aqueous solution in sequence to obtain 5 fractions (PS-BU-1 ~5). The fractions (PS-BU-2~4) were repeatedly purified by ODS column chromatography (methanol:water, 25:75-80:20) and Sephadex LH-20 (methanol), and separated by preparative HPLC to obtain the compound paeonol glycoside A (paeonolide A, 1), paeonolide B (paeonolide B, 2...

Embodiment 2

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

[0037] Take 0.1 ml of complement (guinea pig serum), add barbiturate buffer solution (BBS) to make a 1:10 solution, and dilute it to 1:20, 1:40, 1:80, 1:160, 1:10 with BBS 320, 1:640 and 1:1280 solutions. Take 1:1000 hemolysin, 0.1 ml of each concentration of complement and 2% sheep red blood cells (SRBC) and dissolve them in 0.3 ml BBS, mix well, put them in a low-temperature high-speed centrifuge at 5000 rpm, 4 ºC after 30 min in a water bath at 37 ºC Centrifuge for 10 min under conditions. Take 0.2 ml of the supernatant from each tube in a 96-well plate, and measure the absorbance at 405 nm. A full hemolysis group (0.1 ml 2% SRBC dissolved in 0.5 ml 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. Plot the dilution of complement on the X-axis and the p...

Embodiment 3

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

[0039] Take 0.2 ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5 mM Mg 2+ , 8mM EGTA) was prepared as a 1:5 solution and double diluted to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solutions. Take 0.15 ml of complement of each concentration, 0.15 ml of AP diluent and 0.20 ml of 0.5% rabbit red blood cells (RE), mix well, place in a low-temperature high-speed centrifuge at 5000 rpm and 4 ºC for 10 min in a 37 ºC water bath . Take 0.2 ml of the supernatant from each tube in a 96-well plate, and measure the absorbance at 405 nm. A complete hemolysis group (0.20 ml 0.5% RE dissolved in 0.3 ml 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 the percentage of hemolysis on ...

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Abstract

The invention belongs to the field of manufacturing of traditional Chinese medicines, and relates to phenolic glycoside compounds in Paeonia suffruticosa Andr. velamen and novel application of the compounds in anticomplement medicine preparation. According to the invention, a modern pharmacological research method is adopted, dried velamen anticomplement active materials of Paeonia suffruticosa Andr. belonging to Paeonia L. are researched, six phenolic glycoside compounds are separated at an n-butyl alcohol extraction position of a 95% ethanol extract, and the phenolic glycoside compounds are verified to have inhibiting effects on a complement system classical pathway and an alternative pathway. The inhibiting effect CH<50> of the compounds on the complement system classical pathway is 0.062-0.364 mg / mL, and the inhibiting effect AP<50> on the alternative pathway is 0.102-0.566 mg / mL. The compounds can be used to prepare complement inhibitors.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to phenolic glycoside compounds in paeony cortex and their new application in preparing anti-complement drugs. Background technique [0002] Studies have shown that excessive activation of the complement system can lead to many major 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 the above-mentioned diseases caused by the overactivation of the complement system. Therefore, 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 mo...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/08A61K31/7034A61P37/02
CPCC07H1/08C07H15/203
Inventor 陈道峰宋伟华
Owner FUDAN UNIV
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