Shikonin compound and purpose thereof in preparing anticomplement medicines

A kind of technology of shikonin and compound, applied in the field of preparing anti-complement medicine

Inactive Publication Date: 2013-05-08
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 the chemical constituents of comfrey has mainly focused on the separation and structural identification, and some compounds such as benz

Method used

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  • Shikonin compound and purpose thereof in preparing anticomplement medicines
  • Shikonin compound and purpose thereof in preparing anticomplement medicines
  • Shikonin compound and purpose thereof in preparing anticomplement medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 prepares shikonin compound

[0023] 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 ethyl acetate extract, go through silica gel column chromatography, and elute with petroleum ether (60-90°C), petroleum ether (60-90°C)-acetone, acetone gradient, and the obtained fractions are subjected to repeated silica gel with different eluents. Column chromatography, SephadexLH-20 purification, separation of compounds shikonin (1), 2,3-dimethyl-2-pentenoylshikonin (2) and acetylshikonin (3), the specific steps are as follows :

[0024] 1. The obtained fractions were eluted with petroleum ether-acetone (...

Embodiment 2

[0027] Example 2 Anti-complement classical pathway test in vitro

[0028]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

[0029] Example 3 Anti-complement alternative pathway test in vitro

[0030] 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 purpose of a shikonin compound in preparing anticomplement medicines. According to the invention, the shikonin compound is extracted from an ethyl acetate 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 inhibition effect of the compound upon the classical pathway of the complement system is 0.16 (plus or minus 0.02)-0.63 (plus or minus 0.09)mM, and AP50 of the inhibition effect of the compound upon the alternative pathway of the complement system is 0.24 (plus or minus 0.04)-0.41 (plus or minus 0.04)mM. 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 the new application of shikonin compounds in the preparation of anti-complement drugs. The shikonin compounds include the compounds shikonin (1), 2,3-dimethyl-2- Pentenylshikonin (2) and acetylshikonin (3). Background technique [0002] Excessive activation of the complement system can lead to systemic lupus erythematosus, rheumatoid arthritis, acute respiratory distress syndrome and other diseases. Currently there is no ideal drug for the treatment of such diseases. Research on anti-complement drugs has been the focus and focus of world pharmaceutical research for many years. Studies have shown that the cost of 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. Therefore, in recent years, new drugs with anti-complement activity have ...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61P37/02C07C69/18C07C69/533C07C67/48
Inventor 陈道峰金家宏
Owner FUDAN UNIV
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