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Phenolic glycoside compounds and application thereof in preparation of anticomplement drugs

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: 2014-12-24
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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  • Phenolic glycoside compounds and application thereof in preparation of anticomplement drugs
  • Phenolic glycoside compounds and application thereof in preparation of anticomplement drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1. Preparation of phenolic glycosides

[0036]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 × 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

[0046] Example 2. Anti-complement classical pathway test in vitro

[0047] 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 and 4 oC for 30 minutes 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 its absorbance at 405 nm; set up a complete hemolysis group (0.1 ml 2% SRBC dissolved in 0.5 ml triple-distilled water) at the same time; Hemolysis standard, calculate the hemolysis rate. Take the complement dilution as the X-axis and the hemolysis percentage as the Y-axis to draw a graph, select the lowest complement concentration that...

Embodiment 3

[0048] Example 3. Anti-complement alternative pathway test in vitro

[0049] Take 0.2 ml of complement (human serum), add AP diluent (barbital buffer, pH=7.4, containing 5 mM Mg 2+ , 8 mM 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 erythrocytes (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 full 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 the Y-...

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Abstract

Belonging to the field of Chinese medicine preparation, the invention relates to phenolic glycoside compounds in cortex moutan and application thereof in preparation of anticomplement drugs. The invention employs a modern pharmacological research method to study the anticomplement active substances in dry root barks of Paeonia plant Paeonia suffruticosa Andr., separate 8 phenolic glycoside compounds from an n-butanol extraction position of a 95% ethanol extract, and prove the strong inhibiting effect of the compounds on a complement system classical pathway and an alternative pathway. The inhibiting effect (CH50) of the compounds on the complement system classical pathway is 0.062-0.185mg / ml, and the inhibiting effect (AP50) on the alternative pathway is 0.102-0.393mg / ml. The compounds can be used for preparing 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. A novel complement inhibitor. 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 the characteristics of low cost and low toxicity. Scholars ...

Claims

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Application Information

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IPC IPC(8): C07H15/203C07H1/08A61K31/7034A61P37/02A61P29/00A61P19/02A61P11/00
Inventor 陈道峰宋伟华
Owner FUDAN UNIV
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