Application of alkannin derivant

A derivative, shikonin technology, applied in the field of application of shikonin derivatives, can solve problems such as no discovery, modification and optimization, and unclear anti-tumor effect

Inactive Publication Date: 2010-03-31
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
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  • Application of alkannin derivant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 And preparation of shikonin derivatives

[0029] Weigh 20 kg of Liaoning Lithospermum (commercially available), grind and pass through an 80-mesh sieve, collect the comfrey powder obtained after sieving, and perform percolation extraction with 95% ethanol at room temperature until the extract is nearly colorless.

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

[0031] After filtering to remove the insoluble matter, add concentrated HCl to acidify the solution until the solution turns from blue to purple-red, at which time a large amount of precipitation is formed, and let it stand overnight.

[0032] Dissolve the crude product with chloroform, add 17 grams of 200-300 mesh silica gel per 50 milliliters, and stir evenly on the column. As the eluent, petroleum ether (60-90° C.)-acetone and petroleum ether (1:1)-acetone-chloroform (1:1) we...

Embodiment 2

[0036] Example 2 , Shikonin derivatives inducing the expression of Nur77

[0037] 2.1, cell culture

[0038] Select lung cancer cell NIH-H460 (ATCC, HTB-177) and cervical cancer cell HeLa (ATCC, CCL-2), use RPM1640 medium (purchased from Hyclone), culture in a 24-well plate at 37℃ and 5% carbon dioxide incubator In the tissue culture plate, the medium was changed after 24 hours, and the drug (without serum) was treated after 16 hours of starvation. Shikonin derivatives are dissolved in DMSO (final concentration of DMSO <0.1%), and the control group is treated with the same concentration of DMSO. The specific treatment is as follows:

[0039] (1) Control group (DMSO)

[0040] (2) SK03 group

[0041] (3) SK06 group

[0042] (4) SK07 group

[0043] 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 relations...

Embodiment 3

[0064] Example 3 , Shikonin derivatives induce tumor cell apoptosis

[0065] 3.1 Shikonin derivatives induce NIH-H460 cell apoptosis

[0066] Select lung cancer cells NIH-H460 (ATCC, HTB-177), use RPM1640 medium (purchased from Hyclone), culture in a 24-well tissue culture plate at 37°C and 5% carbon dioxide incubator, change the medium and proceed after 24 hours Dosing (without serum) treatment. Shikonin derivatives are dissolved in DMSO (final concentration of DMSO <0.1%), and the control group is treated with the same concentration of DMSO. The specific treatment is as follows:

[0067] (1) Control group (DMSO)

[0068] (2) SK03 group

[0069] (3) SK06 group

[0070] (4) SK07 group

[0071] The total volume of each well solution in the reaction plate is 1ml, and the concentrations of SK03, SK06 and SK07 are all 5μM.

[0072] After 24 hours of treatment, the cells were digested with 0.5% trypsin, washed with 0.1M PBS, fixed with 4% paraformaldehyde, stained with 1μg / ml DAPI, and obser...

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PUM

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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 present invention relates to the field of Chinese herbal medicine, in particular to the application of shikonin derivatives. Background technique [0002] The 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 whose expression can be affected by serum, growth factors, myristyl phorbol acetate -13 (TPA) and calcium signals 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 considered as a cell survival factor, which can mediate a variety of survival signal pathways, including protein kinase A, protein kinase C, MAPK and NF-κB pathways. The growth-promoting effect of Nur77 expression has been confirmed in a variety of tumors (Chen GQ, et.al., Int J Cancer 2002; 99: 171-8; Wu Q, et.al, Carcinogenesis 2002; 23: 1583-92. ), it has been reported that the expression le...

Claims

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Application Information

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Patent Type & Authority Applications(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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