Use of retinol X receptor used for screening alkannin and derivates thereof

A technology for retinol and derivatives, applied in the application field of retinol X receptor, screening shikonin and its derivatives, can solve the problems of modification and optimization, unclear anti-tumor effect, and no discovery

Inactive Publication Date: 2008-11-26
SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the mechanism of anti-tumor effect of shikonin and its derivatives is still unclear, and a clear target has not been found, so it is difficult to effectively modify and optimize the structure, which restricts its further development as an anti-tumor drug. Top reasons for cancer drugs

Method used

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  • Use of retinol X receptor used for screening alkannin and derivates thereof
  • Use of retinol X receptor used for screening alkannin and derivates thereof
  • Use of retinol X receptor used for screening alkannin and derivates thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1 , preparation of shikonin and its derivatives

[0026] Weigh 20kg of Sichuan Mihua Dianzicao (commercially available), grind it and pass it through a 20-mesh sieve, collect the Comfrey powder obtained after sieving, and carry out normal temperature percolation extraction with 95% ethanol until the extract is nearly colorless .

[0027] Combine the extracts, concentrate under reduced pressure until the solution turns purple, add 1 / 3 to 1 / 2 of the concentrated solution volume 2% NaOH to the concentrated solution until the solution changes from purple to blue.

[0028] After removing the insoluble matter by filtration, add concentrated HCl to acidify the solution until the solution changes from blue to purple, at this time a large amount of precipitates are formed, and stand overnight.

[0029] The precipitate was collected and washed with distilled water until neutral. The precipitate was dried and about 250 g of crude product was harvested as a powdery soli...

Embodiment 2

[0031] Example 2 , shikonin and its derivatives directly act on RXRα

[0032] Using the shikonin and its derivatives prepared in Example 1, respectively treat the RXRα-GST protein synthesized in vitro or in bacteria, and use ligand competition binding experiments to study the relationship between shikonin and its derivatives and RXRα receptors role relationship.

[0033] In the presence or absence of the test compound (i.e. shikonin and its derivatives described in Example 1), with [ 3 H] isotopically labeled [ 3 H]9cis-RA was incubated with RXRα protein at 4°C. Among them, 9cis-RA is a strong endogenous ligand of RXRα, so it can be used as a positive control.

[0034] After 24 hours, GST-agarose was added and placed at room temperature for 1 hour, washed three times with PBS, and the combination of the test compound and RXRα was analyzed with a liquid scintillation analyzer, and the results were as follows: figure 1 shown.

[0035] according to figure 1 As shown, RXRα...

Embodiment 3

[0037] Example 3 , Shikonin and its derivatives regulate the transcriptional activity of RXRα

[0038] CV-1 cells (ATCC, CCL-70) were taken and cultured overnight in a 24-well tissue culture plate.

[0039] The overnight cultured CV-1 cells were transfected with RXRα and (TREpal) 2 -tk-CAT or βRARE-tk-CAT, wherein β-gal is used as an internal control.

[0040] After 24 hours of transfection, the medium was changed, and in the presence of compounds known to up-regulate RXRα transcriptional activity, such as 9cis-RA, with or without the addition of test compounds (i.e., shikonin and its derivatives described in Example 1) to Treat cells. After 20 h, the cells were lysed with RLB (reporter lysis buffer, purchased from Promega), and then, according to the method in the product manual, the β-gal value and CAT value of the lysate were measured, and the relative value was obtained by dividing the CAT value by the β-gal value. The transcriptional activity value of , the experimen...

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PUM

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Abstract

The invention provides an alkannin and a derivative thereof that are used for preparing drugs for adjusting and controlling the activity and the function of a retinol X receptor, the retinol X receptor is used for screening the alkannin and the derivative thereof and the retinoid X receptor is served as a receptor target for guiding the structure modification of the alkannin and the derivative thereof. The retinol X receptor provided by the invention is used as the receptor target, which can be used for screening the alkannin and the derivative thereof to obtain a compound drug for adjusting the activity of RXR Alpha and also can be used for guiding the structure modification of the alkannin and the derivative thereof so as to obtain a compound with higher activity.

Description

technical field [0001] The present invention relates to the field of Chinese herbal medicine, in particular to the application of shikonin and its derivatives, more specifically to the application of retinol X receptors for screening shikonin and its derivatives. Background technique [0002] Many vital activities of the human body are regulated by a class of fat-soluble hormones and vitamins. These fat-soluble hormones and vitamins can enter cells through the cell membrane and play a role through the mediation of nuclear receptors. People collectively refer to all nuclear hormone receptors as the hormone nuclear receptor superfamily, which is a class of ligand-dependent transcription factors with many members, including 29 subfamilies with more than 200 members (Novac N, et al., Curr Drug Targets Inflamm Allergy, 2004; 3:335-46; Gronemeyer H, et al., Nat Rev Drug Discov. 2004 Nov; 3:950-64.). [0003] Nuclear receptors selectively combine with certain chemical substances t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/122A61P35/00A61K36/30
Inventor 张晓坤王力曾锦章
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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