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Application of cholecystokinin receptor inhibitor-Devazepide in preparation of anti-fibrosis pharmaceutical preparations

A receptor inhibitor, cholecystokinin technology, which is used in the preparation of anti-myofibroblast proliferation and anti-fibrosis therapeutic drugs.

Active Publication Date: 2016-06-22
WUXI PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on Devazepide used to inhibit the proliferation and fibrosis of myofibroblasts has not been reported in the literature.

Method used

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  • Application of cholecystokinin receptor inhibitor-Devazepide in preparation of anti-fibrosis pharmaceutical preparations
  • Application of cholecystokinin receptor inhibitor-Devazepide in preparation of anti-fibrosis pharmaceutical preparations
  • Application of cholecystokinin receptor inhibitor-Devazepide in preparation of anti-fibrosis pharmaceutical preparations

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Devazepide inhibits the proliferation of myofibroblast WPMY-1.

[0029] Purchase prostate tissue-derived myofibroblast WPMY-1 (ATCC), culture WPMY-1 cells in DMEM medium containing 10% FBS and a cell incubator with 5% CO2 at 37 degrees, and when the cells are in good condition, follow the daily Hole 1*10 4 Cells were inoculated into 96-well cell culture plates at a density of 24 h, and the cells were treated with different concentrations of Devazepide ( figure 1 ), using the CCK-8 cell proliferation detection kit to detect cell proliferation activity 48h after drug treatment ( figure 2 ).

[0030] WPMY-1 cells in good condition were used to make cell slides, the cells were treated with Devazepide (25uM), and the expression of KI-67 related to WPMY-1 cell proliferation was detected by immunofluorescence ( image 3 ). At the same time, the RNA of WPMY-1 in myofibroblasts treated with Devazepide (25uM) for 24 hours was extracted, and the expressions of KI-67...

Embodiment 2

[0031] Example 2 Devazepide induced myofibroblast WPMY-1 cell cycle G2 / M arrest.

[0032] Cultivate WPMY-1 cells in vitro, and inoculate 6-well cell culture plates when the cell viability is good. After the cells adhere to the wall, treat WPMY-1 cells with 25uM Evazepide, harvest the cells at 24 and 48 hours after treatment, and fix with 70% ice ethanol 48h, after further processing, the cell cycle was detected by flow cytometry ( Figure 5 ). The expression of cell cycle-related proteins was detected by immunoblotting ( Image 6 ). In summary, it was confirmed that Devazepide caused WPMY-1 cell cycle G2 / M phase arrest, and up-regulated the expression of p-Chk1 and p-Chk2.

Embodiment 3

[0033] Example 3 Devazepide promotes apoptosis of myofibroblast WPMY-1.

[0034] WPMY-1 cells were cultured in vitro, and when the cells were in good condition, the cells were treated with Devazepide (25uM), and the apoptosis was detected by AnnexinV-FITC / PI double staining after treatment ( Figure 7 , Figure 8 ); extract the total protein of cells treated with Devazepide, detect the expression of apoptosis-related proteins, and up-regulate the expression of activated Caspase3 ( Figure 9 ). In summary, it is confirmed that Devazepide induces the apoptosis of myofibroblast WPMY-1.

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Abstract

The invention discloses the application of a cholecystokinin receptor inhibitor-Devazepide in preparation of anti-fibrosis pharmaceutical preparations. The cholecystokinin receptor inhibitor-Devazepide is capable of effectively inhibiting and killing myofibroblast which is closely related to the fibrosis of tissues and organs of a human body and is also capable of inhibiting the contractility of the myofibroblast. On this basis, the cholecystokinin receptor inhibitor-Devazepide is applied to the pharmaceutical preparations used for resisting the myofibroblast and fibrosis, and is used for inhibiting the growth of the myofibroblast and blocking the fibrosis progress.

Description

technical field [0001] The invention relates to a new application of cholecystokinin receptor inhibitor Devazepide, that is, the application of Devazepide in the preparation of anti-myofibroblast proliferation and anti-fibrosis therapeutic drugs. Background technique [0002] Fibrosis is a multifactorial disease. How to prevent and effectively treat fibrosis is a difficult problem in the medical field. Studies have found that fibrosis can occur in multiple organs throughout the body, including the prostate, heart, liver, lungs, and kidneys. The pathological changes of fibrosis are mainly manifested by the increase of fibrous connective tissue and the decrease of parenchymal cells in tissues and organs. As the disease progresses, it will eventually seriously affect the functions of related tissues and organs. The latest research shows that the fibrosis of the prostate tissue around the urethra can increase tissue stiffness and reduce the contractility of the surrounding uret...

Claims

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Application Information

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IPC IPC(8): A61K31/5513A61P13/08A61P9/00A61P1/16A61P11/00A61P13/12
CPCA61K31/5513
Inventor 卫冰冰胡强王志荣阮钧诸明宣枫张坚
Owner WUXI PEOPLES HOSPITAL
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