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Boraginaceae phenol compound and purpose thereof in preparing anticomplement medicines

A technology of shikonol and compounds, applied in the field of traditional Chinese medicine pharmaceuticals, can solve problems such as the inhibitory effect of the complement system that has not yet been seen

Inactive Publication Date: 2014-07-09
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 comfrey has focused on the separation and structural identification of chemical components, and some compounds such as benzoquinones and shikonols have been isolated from them, but so far, there has been no information about the inhibition of shikonol compounds on the complement system. Reports of the role

Method used

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  • Boraginaceae phenol compound and purpose thereof in preparing anticomplement medicines
  • Boraginaceae phenol compound and purpose thereof in preparing anticomplement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Example 1 Preparation of shikonbutyrin (arnebiol D)

[0016] 20kg of dry root of Xinjiang comfrey, the coarse powder was repeatedly cold soaked and percolated with 95% ethanol at room temperature and extracted several times, and the solvent was recovered under reduced pressure to obtain 820g of extract, which was suspended in distilled water and mixed with petroleum ether and ethyl acetate. Ester and n-butanol extraction to obtain 420 g of ethyl acetate extract. Take 180g of the ethyl acetate extract, go through silica gel column chromatography, and use petroleum ether (60-90°C)-acetone gradient elution to obtain 7 fractions Fr.1~Fr.7, Fr.2 go through silica gel column Ether-chloroform (5:1) was used as the eluent to obtain 10 fractions Fr.2-1~Fr.2-10, and the obtained fraction Fr.2-6 was recrystallized by petroleum ether-acetone (4:1) Compound JAE-4 (15 mg) was obtained, which was identified as a shikonol compound with a new structure by spectroscopy and named as arne...

Embodiment 2

[0017] Example 2 Anti-complement classical pathway test in vitro

[0018] 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

[0019] Example 3 Anti-complement alternative pathway test in vitro

[0020] 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 pharmacy, and relates to a boraginaceae phenol compound and a purpose thereof in preparing anticomplement medicines. According to the invention, a boraginaceae phenol compound is extracted from an ethyl acetate part of an ethanol extract of a boraginaceae plant arnebia euchroma (Royle) Johnst. With an in-vitro complement activity evaluation test, it is verified that the compound has high inhibition effect upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.53 +- 0.10mM, and AP50 is 0.36 +-0.02mM. The compound can be used for preparing anti-complement medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to shikonol compounds and their application in the preparation of anti-complement drugs. Background technique [0002] The prior art discloses that excessive activation of the complement system can cause various diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. Over the years, the research on anti-complement drugs has been the focus and focus of the world's pharmaceutical research. At present, there is no ideal drug for the treatment of such diseases in clinical practice. Therefore, there is an urgent need for high-efficiency, low-toxicity, and specific new complement inhibitors in this field. Studies have shown that 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 na...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/91A61K31/343A61P37/02
Inventor 陈道峰金家宏
Owner FUDAN UNIV
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