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Application of active ingredients of thunder god vine for regulating heat shock protein and retinol X receptor Alpha

A heat shock protein and active ingredient technology, which is applied in the application field of Tripterygium wilfordii active ingredients regulating heat shock protein and retinol X receptor alpha, can solve the problem of not finding a clear, modified and optimized, and unknown mechanism of anti-tumor effect. wait for the problem

Inactive Publication Date: 2009-11-11
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 its anti-tumor effect is still unclear, and a clear target has not been found, so it is difficult to effectively modify and optimize the structure, which is the main reason restricting its further development as an anti-cancer drug

Method used

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  • Application of active ingredients of thunder god vine for regulating heat shock protein and retinol X receptor Alpha
  • Application of active ingredients of thunder god vine for regulating heat shock protein and retinol X receptor Alpha
  • Application of active ingredients of thunder god vine for regulating heat shock protein and retinol X receptor Alpha

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 , the preparation of Tripterygium wilfordii extract

[0038] Weigh 100g tripterygium twig root (commercially available), add 5 times the amount of 95% ethanol after grinding, reflux twice, each time for 3 hours, combine the extracts, extract the extracts with chloroform, and concentrate and dry the extracts to obtain 0.36g Chloroform extract, which is an active component, is then dissolved in dimethyl sulfoxide (DMSO) to prepare a solution of Tripterygium wilfordii extract with a concentration of 50 mg / ml.

Embodiment 2

[0039] Example 2 , Tripterygium twig extract on the regulation of RXRα transcriptional activity

[0040] Experiment with the tripterygium wilfordii extract prepared in Example 1. CV-1 cells (ATCC, CCL-70) were taken and cultured overnight in a 48-well tissue culture plate.

[0041] Then, the overnight cultured CV-1 cells were transfected with plasmids RXRα and (TREpal) 2 -tk-CAT, and the plasmid β-gal was used as an internal control.

[0042] The medium was changed 6 hours after transfection, and in the presence of compounds known to up-regulate RXRα transcriptional activity, such as 9cis-RA, the cells were treated with or without Tripterygium wilfordii extract for 20 hours (wherein, the concentration of added tripterygium wilfordii extract was 0.125 , 0.25, 0.5, 1.0, 2.0 μg / ml), then use RLB (reporter lysis buffer, purchased from Promega) to lyse the cells, then, according to the method of the product manual, measure the β-gal value and CAT value of the lysate, and use D...

Embodiment 3

[0044] Example 3 , Tripterygium wilfordii extract inhibits cancer cell growth and its correlation with RXRα

[0045] 3.1. Tripterygium wilfordii extract inhibits the growth of cancer cells

[0046] Using the MTT method to detect the inhibition of cell growth by the tripterygium wilfordii extract, the specific process is as follows:

[0047] Take H460 lung cancer cells (ATCC, HTB-177) and MGC803 gastric cancer cells (purchased from the Shanghai Cell Bank of the Chinese Academy of Sciences), and add them to RPMI 1640 medium (purchased from Hyclone) containing 10% fetal bovine serum, respectively. At the same time, take SMMC7721 liver cancer cells Cells (Shanghai Cell Bank, Chinese Academy of Sciences, TChu13) were added to DMEM medium (purchased from Hyclone) containing 10% calf serum, and cultured on a 96-well tissue culture plate in a 5% carbon dioxide incubator at 37°C. 24 hours, then add different concentrations (respectively 0.125, 0.25, 0.5, 1.0, 2.0, 4.0μg / ml) of tript...

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Abstract

The invention provides a thunder god vine extract and active ingredients thereof, which are used for preparing a drug for regulating the activity and the function of a retinol X receptor. The retinol X receptor is used for selecting the thunder god vine extract and the active ingredients contained therein and guiding the application of structural modification of the active ingredients contained in thunder god vine. Meanwhile, the invention discloses an application of the active ingredients of the thunder god vine for adjusting the transcription activity of RXR Alpha on which HSP70 depends on by inducing the mutual action between the heat shock protein HSP70 and the nuclear receptor RXR Alpha, thereby providing a new selection way for selecting drugs relevant to the activity of the RXR Alpha.

Description

technical field [0001] The invention relates to the field of Chinese herbal medicine, in particular to the application of Tripterygium wilfordii, and more specifically to the application of the active ingredients of Tripterygium wilfordii to regulate heat shock protein and retinol X receptor α. Background technique [0002] Many life activities of the human body are regulated by a class of fat-soluble hormones and vitamins, such as glucocorticoids, mineralocorticoids, androgens, estrogens, thyroid hormones, vitamin A and vitamin D, etc. These fat-soluble hormones and vitamins can pass through The cell membrane enters the cell and functions through the mediation of nuclear receptors. Because these receptors are very similar in structure, people group all such receptors into a large family, collectively called the hormone nuclear receptor superfamily. This is a ligand-dependent transcription factor with many members, including 29 subfamilies with more than 200 members (Novac ...

Claims

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Application Information

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IPC IPC(8): A61K36/37A61P35/00A61K127/00A61K125/00A61K133/00
Inventor 陆炯明陈洁曾锦章张晓坤
Owner SHANGHAI INST OF BIOLOGICAL SCI CHINESE ACAD OF SCI
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