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New application of pyridine compound

A technology of compounds and pyridines, applied in new application fields of compounds, can solve the problems of small number of small molecular compounds and poor specificity

Pending Publication Date: 2019-11-19
TIANJIN UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Some compounds that promote TFEB expression have been used in clinical trials, but so far, the number of small molecule compounds that can induce TFEB activation has been found, and the specificity is poor

Method used

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  • New application of pyridine compound
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  • New application of pyridine compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Screening of Drugs to Promote TFEB Nuclear Importation

[0024] ① When the TFEB-GFP stable cell line grows to the required density in the 6cm culture dish, the 96-well plate can be plated. Cells were collected, counted on a hemocytometer, and the concentration of the cell suspension was adjusted. 100 μL of the cell suspension was added to each well, plated so that the density of the cells to be tested was 8000 / well, and the edge of the 96-well plate was filled with PBS.

[0025] ②5% CO 2 After incubating at 37°C for 24 h, a final concentration of 10 μM was added (i.e. compound I 8-chloro-6,11-dihydro-11-(4-piperidinyl)-5H-benzo[5,6]cyclohepta base[1,2-b]pyridine).

[0026] ③ 6 hours after dosing, fix with 4% paraformaldehyde at room temperature for 15-20 minutes.

[0027] ④ Discard 4% paraformaldehyde, wash with PBS three times, take photos with a fluorescent microscope or store at 4°C for subsequent photos.

[0028] like figure 1 The results show that compound I c...

Embodiment 2

[0030] Screening for autophagy activators

[0031] ① When the GFP-LC3 stable cell line grows to the desired density in the 6cm culture dish, the 96-well plate can be plated. Cells were collected, counted on a hemocytometer, and the concentration of the cell suspension was adjusted. 100 μL of the cell suspension was added to each well, plated so that the density of the cells to be tested was 8000 / well, and the edge of the 96-well plate was filled with PBS.

[0032] ②5% CO 2 , after 24 hours of incubation at 37°C, a final concentration of 10 μM of the drug (i.e. compound I8-chloro-6,11-dihydro-11-(4-piperidinyl)-5H-benzo[5,6]cycloheptyl [1,2-b]pyridine).

[0033] ③ 6 hours after dosing, fix with 4% paraformaldehyde at room temperature for 15-20 minutes.

[0034] ④ Discard 4% paraformaldehyde, wash with PBS three times, take photos with a fluorescent microscope or store at 4°C for subsequent photos.

[0035] like figure 2 The results showed that compound I could significant...

Embodiment 3

[0037] Effects of Compounds on Nuclear Importation Level of TFEB in HeLa Cells Detected by Nuclear Plasma Separation Technique

[0038] Using the cytoplasmic protein extraction reagents CER I and CER II, under the condition of low osmotic pressure, the cells are fully expanded, and then the cell membrane is destroyed to release the cytoplasmic protein, and then the nucleus is precipitated by centrifugation. The precipitate is the nucleus and the supernatant for cytoplasmic proteins.

[0039] ① Inoculate an appropriate amount of cells in a 6-well plate and place at 37°C, 5% CO 2 conditions overnight.

[0040] ②Treat the cells with small molecule compounds and place at 37°C, 5% CO 2 Conditions continue to grow.

[0041] ③For adherent cells, digest the cells with trypsin containing EDTA, then add complete medium to stop the digestion, transfer to a 1.5mL centrifuge tube, centrifuge at 3000rpm for 5min, and collect the cells.

[0042] ④ Wash the collected cells once with PBS, ...

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Abstract

The invention provides new application of a pyridine compound. The compound is 8-chloro-6,11-dihydro-11-(4-piperidinyl)-5H-benzo[5,6]suberyl[1,2-b]pyridine, can effectively promote ranscription factorTFEB nuclear translocation, and can effectively promote the autophagy of cells, and the process does not depend on an mTOR signal channel. The compound can serve as a transcription factor TFEB and acell autophagy activator and be used for treatment of related diseases.

Description

technical field [0001] The present invention relates to a new application of a compound, especially a new application of a pyridine compound. Background technique [0002] Transcription Factor EB (TFEB) is the first identified basic-helix-loop-helix leucine zipper (bHLH-Zip) class of the MiTF / TFE family Transcription factors play an important regulatory role in the biogenesis and metabolism of lysosomes. They are important regulators of autophagy and have a wide range of physiological functions. Studies have shown that the expression of many proteins that make up lysosomes is regulated by the transcription factor TFEB. Overexpression of TFEB enhanced the expression levels of 51 genes related to autophagy, while knockdown of TFEB downregulated their expression. TFEB regulates several key steps of the autophagy pathway, and has a direct regulatory effect on the activation of autophagy. [0003] Autophagy is a metabolic process ubiquitous in eukaryotic cells. It degrades and...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4545A61P25/28A61P35/00
CPCA61K31/4545A61P25/28A61P35/00
Inventor 刁爱坡刘振兴蔺洁茹
Owner TIANJIN UNIV OF SCI & TECH
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