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Application of alkannin derivant

A derivative, shikonin technology, applied in the application field of shikonin derivatives, can solve problems such as modification and optimization, not found, and unclear anti-tumor effect

Inactive Publication Date: 2013-01-30
XIAMEN UNIV
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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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  • Application of alkannin derivant
  • Application of alkannin derivant
  • Application of alkannin derivant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] The extracts were combined, concentrated under reduced pressure until the solution turned purple, and about 250 g of crude product of purple-brown oil was obtained.

[0031] 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.

[0032] Dissolve the crude product in chloroform, add 17 grams of 200-300 mesh silica gel per 50 ml, stir evenly and put it on the column. The eluent was respectively petroleum ether (60-90°C)-acetone and petroleum ether (1:1)-acetone-chloroform (1:1), and the eluents were collected in sequence.

[0033] Concentrate the eluate until the precipitate is separated out, and then recrystallize (recrystallization method refers to the Chinese patent No. 02114973.9), purify the shikonian compound, and the product is determined to be acetylshikonin by MNR, MSUV and elemental analysis data, ...

Embodiment 2

[0043] Select lung cancer cells NIH-H460 (ATCC, HTB-177) and cervical cancer cells HeLa (ATCC, CCL-2), use RPM1640 medium (purchased from Hyclone), and culture them in 24-well plates at 37°C and 5% carbon dioxide incubator In the tissue culture plate, the medium was changed after 24 hours, and the drug (without serum) was added after 16 hours of starvation. Shikonin derivatives were dissolved in DMSO (DMSO final concentration<0.1%), and the control group was treated with the same concentration of DMSO, and the specific treatment was as follows:

[0044] (1) Control group (DMSO)

[0045] (2) SK03 group

[0046] (3) SK06 group

[0047] (4) SK07 group

[0048] The concentrations of SK03, SK06, and SK07 were all 5 or 10 μM, and the treatment time was 12 or 24 hours. NIH-H460 cells and HeLa cells without any treatment were used as controls. In order to confirm the time-effect and dose-effect relationship, NIH-H460 cells were treated with SK07 at a concentration of 1, 5 or 10 μM...

Embodiment 3

[0071] Select lung cancer cell NIH-H460 (ATCC, HTB-177), use RPM1640 medium (purchased from Hyclone), and cultivate it in a 24-well tissue culture plate at 37 ° C and 5% carbon dioxide incubator, change the medium and carry out after 24 hours Dosing (without serum) treatment. Shikonin derivatives were dissolved in DMSO (DMSO final concentration <0.1%), and the control group was treated with the same concentration of DMSO, and the specific treatment was as follows:

[0072] (1) Control group (DMSO)

[0073] (2) SK03 group

[0074] (3) SK06 group

[0075] (4) SK07 group

[0076]The total volume of each well solution in the reaction plate is 1 ml, and the concentrations of SK03, SK06 and SK07 are all 5 μM.

[0077] After 24 hours of treatment, the cells were digested with 0.5% trypsin, washed with 0.1M PBS, fixed with 4% paraformaldehyde, stained with 1 μg / ml DAPI, and observed the morphology of the nucleus with a fluorescence microscope (Carl Zeiss). The results are as follo...

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Abstract

The invention provides an application of alkannin derivant for preparing drug treating cancers, and the drug takes orphan receptor Nur77 as an effect target. The invention also provides the application of the orphan receptor Nur77 which serves as an effect target to screen alkannin derivant. The alkannin derivant of the invention clarifies the mechanism of the anti-tumour effect of alkannin derivant via a great discovery that tumour cells are induced to apoptosis by acting on the orphan receptor Nur77, and provides effective target spots for decorating and optimizing the structure.

Description

technical field [0001] The invention relates to the field of Chinese herbal medicines, in particular to the application of shikonin derivatives. Background technique [0002] Orphan receptor Nur77 (also known as TR3 or NGFI-B), is an important member of the nuclear receptor superfamily, it is also an immediate early gene, its expression can be controlled by serum, growth factors, myristyl phorbol acetate -13(TPA) and calcium signaling are rapidly induced (Zhang XK. et. al., Expert Opin Ther Tar 2007; 11: 69-79; Moll UM, et. al., Oncogene 2006; 25: 4725-43.). [0003] Nur77 was originally recognized as a cell survival factor that mediates multiple survival signaling pathways, including protein kinase A, protein kinase C, MAPK, and NF-κB pathways. The growth-promoting effect of Nur77 expression has been confirmed in various tumors (Chen GQ, et.al., Int J Cancer2002; 99:171-8; Wu Q, et.al., Carcinogenesis2002; 23:1583-92.) , It has been reported that the expression level of N...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/215A61P35/00
Inventor 曾锦章张晓坤刘婕李绍顺周文王光辉
Owner XIAMEN UNIV
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