Application of 2, 2, 3, 3- tetramethyl cyclopropyl carbonyl thiourea in the process for preparing antitumor medicine

A technology of tetramethylcyclopropionyl thiourea and antitumor drug, which is applied in the application field of 2,2,3,3-tetramethylcyclopropionylthiourea in the preparation of antitumor drugs, and can solve the antitumor effect No reports yet

Inactive Publication Date: 2012-05-23
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007]Foreign Sobol et al. J Med Chem, 2004, 47 (17): 4316-4326) only carried out the anticonvulsant effect of 2,2,3,3,-tetramethylcyclopropionyl urea modified by zinc ion binding region Research, the anti-tumor effect of similar modifications has not been reported

Method used

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  • Application of 2, 2, 3, 3- tetramethyl cyclopropyl carbonyl thiourea in the process for preparing antitumor medicine
  • Application of 2, 2, 3, 3- tetramethyl cyclopropyl carbonyl thiourea in the process for preparing antitumor medicine
  • Application of 2, 2, 3, 3- tetramethyl cyclopropyl carbonyl thiourea in the process for preparing antitumor medicine

Examples

Experimental program
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Effect test

Embodiment 1

[0024] Example 1. The effect of 2,2,3,3-tetramethylcyclopropionylthiourea on the growth and proliferation of U251 cells

[0025] 1. Experimental materials and instruments

[0026] Cell line and drug: The human astroglioma cell line U251 was derived from the Sun Yat-sen University Affiliated Tumor Hospital, and 2,2,3,3-tetramethylcyclopropionylthiourea was combined by this experimental subject.

[0027] Main reagents: RPMI 1640 medium, premium fetal bovine / calf serum (FBS / CS), trypsin, dimethyl sulfoxide (DMSO), valproic acid (VPA), tetrazothiazole (MTT) powder.

[0028] Main working solution: Cell dry powder RPMI 1640 medium, double antibody storage solution (100×) (weigh 0.625g penicillin sodium, 1.000g streptomycin, add about 80ml PBS, stir well to dissolve, and dilute to 100ml. 0.22μm filter membrane Sterilize by filtration and dispense into multiple 1.5ml Ep tubes, store at -20℃, and dilute 100 times when used), phosphate buffered saline (PBS), cell digestion solution (0.25%tryp...

Embodiment 2

[0034] Example 2.2 The effect of 2,2,3,3-tetramethylcyclopropionylthiourea on the mRNA expression of U251 cell cycle factors p21WAF1 / CIP1, CyclinD1

[0035] 1. Experimental materials and instruments

[0036] Cell line and drug: The human astroglioma cell line U251 was derived from the Sun Yat-sen University Affiliated Tumor Hospital, and 2,2,3,3-tetramethylcyclopropionylthiourea was combined by this experimental subject.

[0037] Main reagents: RPMI 1640 medium, premium fetal bovine serum, PAA (stored at -20°C), trypsin, dimethyl sulfoxide (DMSO), valproic acid (VPA), TRNzol-A + Extraction reagents, Quant one-step RT-PCR kit, DEPC, EB, TBE, 6× loading buffer.

[0038] Main working solution: Cell dry powder RPMI 1640 medium, double antibody storage solution (100×) (weigh 0.625g penicillin sodium, 1.000g streptomycin, add about 80ml PBS, stir well to dissolve, and dilute to 100ml. 0.22μm filter membrane Sterilize by filtration and dispense into multiple 1.5ml Ep tubes, store at -20°C...

Embodiment 3

[0051] Example 3 Effect of 2,2,3,3-tetramethylcyclopropionylthiourea on the protein expression of HDAC3 / HDAC4 and cyclic factors p21 and CyclinD1 in U251 cells

[0052] 1. Experimental materials and instruments

[0053] Cell line and drug: The human astroglioma cell line U251 was derived from the Sun Yat-sen University Affiliated Tumor Hospital, and 2,2,3,3-tetramethylcyclopropionylthiourea was combined by this experimental subject.

[0054] Main reagents: RPMI 1640 medium, premium fetal bovine serum, PAA (stored at -20°C), trypsin, dimethyl sulfoxide (DMSO), valproic acid (VPA), nuclear protein extraction kit, p21waf1 / cip1 Antibody (I antibody), HDAC3 antibody (I antibody), HDAC4 antibody (I antibody), β-actin reference antibody (I antibody), HRP-labeled goat anti-mouse antibody (Goat anti-mouse antibody, II antibody), Protein weight Marker.

[0055] Main working solution: dry cell powder RPMI 1640 medium, double antibody storage solution (100×) (weigh 0.625g penicillin sodium, 1.0...

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PUM

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Abstract

The invention discloses an application of 2, 2, 3, 3-tetramethyl cyclopropyl carbonyl thiourea (TCCT) in the process for preparing an antitumor medicine. The tumor is human astrocytoma. The antitumor medicine comprises an up-regulating tumor suppressor gene p21<WAF1 / CIP1> medicine, a down-regulating cyclin D1 medicine or a down-regulating HDAC3 and HDAC4 expression medicine. The invention confirms that 2, 2, 3, 3-tetramethyl cyclopropyl carbonyl thiourea (TCCT for short) possesses inhibitory effect on the growth of U251 human glioma cells by using a molecular biology method, the 2, 2, 3, 3-tetramethyl cyclopropyl carbonyl thiourea provided in the invention interferes the cell cycle through the effect of p21<WAF1 / CIP1> and CyclinD1 expression, so as to exert the effect of inhibition, whichhas the obvious effect.

Description

technical field [0001] The invention relates to the application of 2,2,3,3-tetramethylcyclopropionylthiourea in the preparation of antitumor drugs. Background technique [0002] Histone is the basic unit of eukaryotic chromatin—the main structural element of the nucleosome. Its amino-terminus is rich in lysine residues. The acetylation modification of the site can affect the binding of DNA to the transcriptional regulatory complex , regulate DNA replication and repair, affect the structure of chromatin and the expression of related genes, and then regulate the transcriptional behavior of cells. The acetylation status of histones is regulated by two classes of enzymes: histone acetyltransferase (HAT) and histone deacetylase (HDAC). Generally speaking, HAT can transfer the acetyl group on the acetyl-CoA to the lysine residue at the N-terminal of the nucleosome core histone, acetylating its ε-amino group, and neutralizing the positive charge of the histone , Weaken its electr...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/17A61P35/00
Inventor 冯冰虹陈宗元夏靖
Owner GUANGDONG PHARMA UNIV
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