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Use of natural or artificial isorhodanate analog compound JC-5411 in preparing transcription factor SP1 inhibitor

A technology of JC-5411, ester compounds, applied in the field of medical applications, can solve problems such as uncertainty of curative effect, and achieve the effects of low production cost, inhibition of abnormal proliferation, and wide applicability

Inactive Publication Date: 2006-05-10
JC (WUXI) CO INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In my country, the treatment of benign prostatic hyperplasia is mainly Chinese herbal medicine, such as pollen, etc., and its curative effect is uncertain

Method used

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  • Use of natural or artificial isorhodanate analog compound JC-5411 in preparing transcription factor SP1 inhibitor
  • Use of natural or artificial isorhodanate analog compound JC-5411 in preparing transcription factor SP1 inhibitor
  • Use of natural or artificial isorhodanate analog compound JC-5411 in preparing transcription factor SP1 inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Embodiment 1, the synthesis of JC-5411:

[0059] Instruments and Reagents

[0060] 1 H-NMR spectrum is measured with BruckerAV-300 nuclear magnetic resonance instrument, internal standard TMS, solvent is CDCl 3 ; MS was determined with a Nicolet FTMS-2000 mass spectrometer; elemental analysis was determined with an Elementar Vario EL III instrument.

[0061] Thin-plate chromatography (TLC) was self-made with silica gel GF254 (produced by Qingdao Ocean Chemical Factory); all reagents were commercially available chemically pure or analytically pure products, and were used directly without treatment.

[0062] Preparation and Inspection of JC-5411 (Phenethyl Isothiocyanate)

[0063] Into a 50 mL round bottom flask was added 15 mL of CH 2 Cl 2 and 3 mL (40 mmol) of thiophosgene, stirred, cooled to 0 ° C, and slowly added dropwise an equivalent amount of triethylamine (4.04 g, 40 mmol) and phenethylamine (4.85 g, 40 mmol) with a constant pressure dropping funnel. Mixe...

Embodiment 2

[0068] Example 2, JC-5411 inhibits the activity of transcription factor SP1:

[0069] Materials and methods:

[0070] Reagent: Take the JC-5411 product synthesized above to make a solution in DMSO. Sp1-luc and mtSp1-luc are composed of the luciferase gene and the corresponding mutant gene whose promoter contains 3 repeats of the SP1 regulatory sequence, and are used to measure the activity of the SP1 transcription factor (40) . Effectene Transfection Reagent and Luciferase Assay Kit were purchased from Qiagen (Valencia, CA) and Promega (Madison, WI), respectively. Western Blot ELC Kit was purchased from Amersham Biosciences (Buckingamshire, England). Polyacrylamide gel reagents for protein electrophoresis, SDS, electrophoresis buffer, and protein electrotransfer buffer were purchased from Bio-Rad Life Sciences, USA. Unless otherwise specified, other chemical reagents used in the experiment were purchased from Sigma Chemical Reagent Company in the United States.

[0071] C...

Embodiment 3

[0078] Example 3, Inhibition of JC-5411 on Androgen Receptor Transcription and Expression

[0079] Materials and Methods

[0080] Reagent: JC-5411, same as Example 2. AR transfection gene see reference (5) . SP1-specific androgen receptor (AR)-luciferase transfection gene (pAR-Sp1-3-O, see figure 1 ), by inserting 3 repeats of the SP1 sequence (located at +429~+442 of the AR promoter) or the corresponding mutant sequence in the luciferase basic gene pGL3 (no promoter), the sequence of which was analyzed by DNA sequence to ensure Exactly. Effectene Transfection Reagent and Luciferase Assay Kit were purchased from Qiagen (Valencia, CA) and Promega (Madison, WI), respectively. AR, PSA and β-actin were purchased from Santa Cruz Biotechnology, Inc. (Santa Cruz, CA). Western Blot ELC Kit was purchased from Amersham Biosciences (Buckingamshire, England). Polyacrylamide gel reagents for protein electrophoresis, SDS, electrophoresis buffer, and protein electrotransfer buffer we...

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Abstract

The invention relates the isosulfocyanate compounds (ISOTHIOCYANATES), in other word, JC-5411 compounds, which can adjust the expression of androgen acceptor gene in cell by suppressing the expression of gene transcription factor SP1, and suppress the abnormal breeding function of prostate gland cell. With the little compound, it can suppress hamster benign hypertrophy of the prostate (BPH), which is induced by suppressed male sex hormone, and the growth of prostate gland cancer cell. The invention provides the new method of effectively preventing and treating the hypertrophy of the prostate and prostate gland cancer. The compound possesses the low side effect, steady chemical biology nature, low cost of manufacture, and broad adaptability.

Description

technical field [0001] The invention belongs to the field of medical applications, and relates to JC-5411 series compounds, which use isothiocyanate as the core structure, including natural and artificially synthesized isothiocyanates. This invention uses the latest molecular biology technology to prove for the first time that JC-5411 series compounds can regulate the expression of androgen receptor gene in cells and inhibit the abnormal proliferation of prostate cells. Rat benign prostatic enlargement (BPH), and growth of prostate cancer cells. Furthermore, the present invention provides a brand-new method for preventing and treating prostatic enlargement and prostate cancer that is effective. The series of compounds also have the advantages of low toxic and side effects, stable chemical and biological properties, low production cost, etc., and have wide applicability. Background technique [0002] BPH, also known as benign prostatic enlargement (BPH), and prostate cancer...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C331/24A61K9/02A61K9/06A61K9/08A61K9/20A61K9/48A61K31/26A61P13/08
Inventor 乔仁伟王龙贵程景才
Owner JC (WUXI) CO INC
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