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Shikonin tetramer compound and purpose thereof in pharmacy

A compound, shikonin technology, applied in organic chemistry, anti-tumor drugs, drug combinations, etc., can solve the problems of anti-complement and anti-tumor effects of shikonin tetramer compounds that have not been reported

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

Looking at the research at home and abroad, there are no reports of shikonin tetramer compounds and their anti-complement and anti-tumor effects.

Method used

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  • Shikonin tetramer compound and purpose thereof in pharmacy
  • Shikonin tetramer compound and purpose thereof in pharmacy
  • Shikonin tetramer compound and purpose thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1 prepares shikonin tetramer compound

[0036] 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 180 g of ethyl acetate extract, and go through silica gel column chromatography, eluting with petroleum ether (60-90°C), petroleum ether (60-90°C)-acetone gradient to obtain 7 fractions Fr1-Fr.7. Fr.5 was subjected to silica gel column chromatography, using chloroform-methanol (20:1) as the eluent to obtain 12 fractions Fr.5-1~Fr.5-12, and the resulting fraction Fr5-3 was subjected to preparative chromatography to obtain Chloroform-methanol (15:1) was used as developing solvent to obtain 1 (13 mg); Fraction F...

Embodiment 2

[0037] Embodiment 2 in vitro antitumor test (SRB method)

[0038] Lung cancer cell line A549, prostate cancer cell line DU145, nasopharyngeal carcinoma cell line KB, and KB drug-resistant strain KBvin were treated with 10% of 25mM HEPES, 0.2% (w / v) sodium bicarbonate and 100μg / ml kanamycin. Calf serum RPMI1640 medium 4ml in a T-25 flask, 37°C, 5% CO 2 cultivated under conditions. The cell suspension digested by trypsin was added to a 96-well plate, and the cell concentration was 0.25-1×10 4 / hole. Tumor cells were added different concentrations of shikonin tetramer compounds and cultured at 37°C for 72 hours, fixed with ice-cold 50% trichloroacetic acid and stained with 0.4% (SRB), after the dye was dissolved, the absorbance was measured at 562nm . ED 50 Conversion was performed according to dose-effect data. Each experiment was repeated three times with less than 5% difference in absorbance values, ED 50 The difference is less than 30%. The results showed that the com...

Embodiment 3

[0039] Example 3 Anti-complement classical pathway test in vitro

[0040] 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. ...

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Abstract

The invention belongs to the field of pharmacy, and relates to a purpose of a shikonin tetramer compound in preparing medicines. According to the invention, the shikonin tetramer 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 and cytotoxic effect upon classical pathway and alternative pathway of a complement system. The compound provided by the invention has both inhibition effects upon classical pathway and alternative pathway of a complement system. The CH50 of the compound is 0.14 (plus or minus 0.01)-0.57 (plus or minus 0.11)mM, and AP50 is 0.06 (plus or minus 0.01)-0.16 (plus or minus 0.02)mM. The novel shikonin E in the compound has substantial inhibition effects against lung cancer cells (A549), prostate cancer cells (DU145), nasopharynx cancer cells (KB), and KB resistant strains (KBvin), wherein ED50 are respectively 5.00mM, 5.42mM, 3.71mM and 4.57mM. The compound can be used for preparing anti-complement or antitumor medicines.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and relates to shikonin tetramer compounds and their use in pharmacy, especially the use in preparing anti-complement or anti-tumor drugs. Background technique [0002] It has been reported that overactivation of the complement system can lead to various diseases such as systemic lupus erythematosus, rheumatoid arthritis, and acute respiratory distress syndrome. At present, there is no ideal drug for the treatment of these diseases clinically. 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 natural products. Drugs are getting more and more attention. Scholars at home and abroad have isolated a large number of monomeric compounds with inhibitory effects on the complement system from natural products including mari...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C50/32C07C46/10C07C69/738C07C67/48A61K31/216A61K31/122A61P37/02A61P35/00
Inventor 陈道峰金家宏李国雄
Owner FUDAN UNIV
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