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mir-21 small molecule inhibitor and its application

A small molecule inhibitor, the technology of 1.mir-21, is used in medical preparations containing active ingredients, organic active ingredients, organic chemistry, etc., which can solve the problems of high price and no real clinical application.

Active Publication Date: 2016-08-03
GENERAL HOSPITAL OF TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to solve the problem that the current method of down-regulating miR-21 is expensive and not really applied in clinical practice, and to provide a new method for down-regulating miR-21, that is, a small molecule inhibitor of miR-21

Method used

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  • mir-21 small molecule inhibitor and its application

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1: miR-21 small molecule inhibitor inhibits glioma cells

[0033] Take 42mg of the compound 2,4-diamino-1,3-diazepine-5-carbonitrile and dissolve it in 3ml of DMSO to obtain a mother solution with a concentration of 0.1M. Inoculate U87 and LN229 glioma cells in 6-well plates respectively, the number of cells is about 100,000-150,000, and after culturing in DMEM containing 10% FBS for 24 hours, add 2,4-diamino-1,3-diazepine The final concentration of cyclo-5-nitrile mother solution was 1.5, 7.5, 15, 30, and 75 μM, respectively, and after 0.5, 1, 2, 6, 24, and 48 hours of culture, real-time PCR was used to detect the expression of miR-21 and other miRNAs, and the cell cycle was paralleled and cell apoptosis detection. The specific method of real-timePCR: use the RNA extraction kit to extract the total RNA in the cells, and perform reverse transcription with AMV reverse transcriptase. The SYBRGreen fluorescent dye incorporation method was used for Real-time PCR, ...

Embodiment 2

[0034] Example 2: miR-21 small molecule inhibitor inhibits breast cancer cells

[0035] Take 42mg of the compound (referring to the small molecule inhibitor of miR-21) 2,4-diamino-1,3-diazepine-5-carbonitrile, and dissolve it in 3ml of DMSO to obtain a mother solution with a concentration of 0.1M. Inoculate MCF-7 breast cancer cells in 6-well plates, the number of cells is about 100,000-150,000, and after 24 hours of culture in DMEM containing 10% FBS, add 2,4-diamino-1,3-diazepine The final concentration of -5-nitrile mother solution was 1.5, 7.5, 15, 30, and 75 μM, respectively. After culturing for 0.5, 1, 2, 6, 24, and 48 hours, real-time PCR was used to detect the expression of miR-21 and other miRNAs, and the cell cycle and Apoptosis detection. The specific method of real-timePCR: use the RNA extraction kit to extract the total RNA in the cells, and perform reverse transcription with AMV reverse transcriptase. The SYBRGreen fluorescent dye incorporation method was used ...

Embodiment 3

[0036] Example 3: miR-21 small molecule inhibitor inhibits gastric cancer cells

[0037]Take 42mg of the compound 2,4-diamino-1,3-diazepine-5-carbonitrile and dissolve it in 3ml of DMSO to obtain a mother solution with a concentration of 0.1M. Inoculate SCG7901 gastric cancer cells in 6-well plates, the number of cells is about 100,000-150,000. After culturing in DMEM containing 10% FBS for 24 hours, add 2,4-diamino-1,3-diazepine-5- The final concentrations of the nitrile mother solution were 1.5, 7.5, 15, 30, and 75 μM, respectively. After 0.5, 1, 2, 6, 24, and 48 hours of culture, real-time PCR was used to detect the expression of miR-21 and other miRNAs, and parallel cell cycle and apoptosis detection. The specific method of real-timePCR: use the RNA extraction kit to extract the total RNA in the cells, and perform reverse transcription with AMV reverse transcriptase. The SYBRGreen fluorescent dye incorporation method was used for Real-time PCR, U6 was used as an internal...

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Abstract

The invention relates to an miR-21 small molecule inhibitor and an application The medicament of the invention can specifically inhibiting the expression of miR-21, thereby promoting a compound 2,4-diamino-1,3-diazacyclohexane-5-nitrile which can induce various tumor cell apoptosis. The binding capability of 2,4-diamino-1,3-diazacyclohexane-5-nitrile is that: Ki=1.49nM, deltaG=-12.04kcal / mol. The preparation method comprises: dissolving 2,4-diamino-1,3-diazacyclohexane-5-nitrile in deionized water to prepare mother solution, adding the mother solution into a tumor cell (colloid tumor, stomach cancer and breast cancer) culturing system according to a certain proportion. The medicament can specifically inhibit the expression of miR-21 without affecting the expression of miRNA. The cell cycle appearances G0 / G1 phase arrest, the cell apoptosis proportion is obviously increased, and more effective inhibition to tumour can be implemented.

Description

technical field [0001] MicroRNA (microRNA or miRNA) refers to a family composed of some special small non-coding RNAs with a length of about 21-25nt. These miRNAs can recognize specific target mRNAs and promote the degradation of target mRNAs and / or Inhibition of translation process negatively regulates the process of gene expression, and is closely related to individual development, stem cell differentiation and disease occurrence. The initial transcription structure of miRNA is a pri-miRNA with a hairpin structure, which is processed by Drosha enzyme to obtain pre-miRNA, and the pre-miRNA is transported out of the nucleus through the transport mechanism relying on RanGTP / exportin5 (Exp5), and the pre-miRNA is digested by Dicer. -The miRNA is degraded into a single-stranded RNA of about 22nt to form a mature miRNA; the mature miRNA can recognize the 3'UTR region of a specific target mRNA in RISC. Each miRNA has dozens or even more protein expression regulatory targets, and e...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/04A61K31/505A61P35/00
Inventor 康春生张军霞史振东韩磊浦佩玉
Owner GENERAL HOSPITAL OF TIANJIN MEDICAL UNIV
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