Application of diphenol compounds in preparation of anti-complement medicaments

A kind of compound, the technology of hydroquinone, applied in the new use field in the preparation of anti-complement medicine

Inactive Publication Date: 2011-05-11
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, the research on Caoguo has only focused on the separation and structural identification of chemical components, and some flavonoids and phenolic compounds have been isolated from it, but so far there have been no reports of compounds that have an inhibitory effect on the complement system

Method used

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  • Application of diphenol compounds in preparation of anti-complement medicaments
  • Application of diphenol compounds in preparation of anti-complement medicaments
  • Application of diphenol compounds in preparation of anti-complement medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1 Preparation of n-butanol extract to obtain hydroquinone compounds

[0023] Take 15kg of dried and mature Tsao Kuo fruit, cold-soak 50L×10 times with ethanol at room temperature, combine the extracts and concentrate until there is no alcohol smell, dilute the extracts with water to 2L, and extract 2L× each with petroleum ether, ethyl acetate, and n-butanol in sequence 3 times, the combined n-butanol extracts were concentrated to dryness to obtain 86.2 g of n-butanol extracts. The n-butanol part was treated with AB-8 macroporous adsorption resin, and the 50% ethanol elution part (21.3g) was subjected to silica gel column chromatography, and was eluted with petroleum ether (60-90°C), petroleum ether-acetone, and acetone gradient. Specific steps are as follows:

[0024] 1. The resulting fractions were eluted with petroleum ether-acetone (3:1), followed by repeated silica gel column chromatography with chloroform-acetone (5:1) to obtain compounds (1) (10 mg), (3) ...

Embodiment 2

[0026] Example 2 Anti-complement classical pathway test in vitro

[0027]Take 0.1ml of complement (guinea pig serum), add BBS to prepare a 1:5 solution, and dilute it to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:320 with BBS 640 solution. Dissolve 1:1000 hemolysin, 0.1ml of each concentration of complement and 2% SRBC in 0.3ml BBS, mix well, put in a low-temperature high-speed centrifuge after 30min in a 37°C water bath, 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. A full hemolysis group (0.1ml 2% SRBC dissolved in 0.5ml 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. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of complement is plotted as the Y-axis. ...

Embodiment 3

[0028] Example 3 Anti-complement alternative pathway test in vitro

[0029] Take 0.2ml of complement (human serum), add AP diluent to prepare a 1:5 dilution solution, and double-dilute to 1:10, 1:20, 1:40, 1:80, 1:160, 1:320 and 1:640 solution. Take 0.15ml of complement of each concentration, 0.15ml of AP diluent and 0.20ml of 0.5% RE, mix well, place in a low-temperature high-speed centrifuge after 30 minutes in a 37°C water bath, and centrifuge at 5000rpm and 4°C for 10 minutes. 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. Taking the dilution of complement as the X-axis, the percentage of hemolysis caused by each dilution of compl...

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Abstract

The invention belongs to the field of Chinese medicinal pharmacy, and relates to new medicinal application of diphenol compounds of a formula 1. The diphenol compounds serving as active substances are extracted from Amomum tsao-ko Crevost et Lemaire fruits, and in vitro anti-complement activity evaluation experiments prove that the diphenol compounds have remarkable inhibiting effect on a classical pathway and an alternative pathway of a complement system. The inhibiting effect CH50 of the compounds on the classical pathway of the complement system is 61+/-12 to 91+/-19mug/ml, and the inhibiting effect AP50 on the alternative pathway is 58+/-17 to 121+/-18mug/ml. The diphenol compounds can be used for preparing anti-complement medicaments.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to a new application of quinone compounds in Tsao Kuo in preparing anti-complement drugs. Background technique [0002] Excessive activation of the complement system can lead to systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases. The study of anti-complement drugs has been the focus and focus of the world's pharmaceutical research for many years. At present, there is no ideal drug for the treatment of such diseases, so there is an urgent need for a new type of complement inhibitor with high efficiency, low toxicity and specificity in clinical practice. The cost of researching and developing complement inhibitors directly from natural products is low, and most active ingredients can be directly digested and absorbed by the body as part of natural products. more and more attention. Scholars at home and abroad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/05A61K31/085A61P37/02A61P29/00
Inventor 陈道峰金家宏
Owner FUDAN UNIV
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