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Application of ZSTK474 to preparation of medicine for treating autoimmune diseases

A technology for autoimmune and inflammatory diseases, applied in sexual diseases, allergic diseases, metabolic diseases, etc., can solve problems such as test doses that do not show toxicity

Inactive Publication Date: 2012-05-02
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, ZSTK474 did not show significant toxicity at the doses tested.

Method used

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  • Application of ZSTK474 to preparation of medicine for treating autoimmune diseases
  • Application of ZSTK474 to preparation of medicine for treating autoimmune diseases
  • Application of ZSTK474 to preparation of medicine for treating autoimmune diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1.1 Isolation of human peripheral blood mononuclear cells

[0032] (1) Go to the blood station to get fresh blood (approved by the health management department). Approximately 40 mL.

[0033] (2) Dilute with 3 times the volume of PBS (the more diluted blood samples, the better the purification of monocytes). Add 15 mL of Ficoll Paque to a 50 mL centrifuge tube for a total of 160 mL. The centrifuge tube is tilted at 45°, absorb 35 mL of diluted blood, and superimpose on the separation liquid along the tube wall at a distance of 1 cm from the separation liquid surface. Do not damage the separation interface. (Divide into 4 tubes, first add 35 mL of blood to 15 mL of Ficoll Paque in each tube, and then average the remaining blood)

[0034] (3) Centrifuge at 400g at room temperature for 30 minutes, decelerate slowly, and do not set the brake gear.

[0035] (4) Take out the centrifuge tube smoothly, the bottom layer is red blood cells and granulocytes, the middle layer is...

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Abstract

The invention discloses application of 2-(2-difluoromethyl benzimidazole-1-yl)-4,6-dimorpholinyl-1,3,5-triazine (ZSTK474 for short) to preparation of a medicine for treating autoimmune and inflammatory diseases. Experimental results prove that the ZSTK474 can inhibit the differentiation of human immune dendritic cells, the maturity of the lipopolysaccharide (LPS) activated human immune dendritic cells, the antigen uptake capacity of immature dendritic cells, the antigen presenting capacity of mature dendritic cells and T cell proliferation reaction stimulated by the dendritic cells, and particularly can reduce the morbidity degree of mouse experimental autoimmune encephalomyelitis, so the ZSTK474 is expected to become a medicine for treating autoimmune and inflammatory diseases such as multiple sclerosis, acute disseminated encephalomyelitis and the like clinically.

Description

technical field [0001] The invention belongs to the technical field of new use of old drugs, and relates to 2-(2-difluoromethylbenzimidazol-1-yl)-4,6-dimorpholinyl-1,3,5-triazine (ZSTK474) Application in the preparation of medicines for treating autoimmune and inflammatory diseases. Background technique [0002] Dendritic cells (DC) are known to be the most powerful antigen-presenting cells (APCs) in the body, and they are also the only APCs that can directly activate naive T cells. [1] . When inflammation occurs, DC first contacts with the antigen and then captures the antigen. After processing, the antigen peptide is combined with MHC molecules and presented on the surface of other immune cells, causing the secretion of cytokines. Under the joint action of the first and second signals, Activate T lymphocytes to generate a specific immune response; on the other hand, DC can differentiate into regulatory cells, maintain self-tolerance, and become a key factor in mediating ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61P37/02A61P29/00A61P25/00A61P27/02A61P19/04A61P9/10A61P3/10A61P7/06A61P15/08A61P21/04A61P1/16A61P13/12A61P1/00A61P17/00A61P21/00
Inventor 张荣信薛振毅
Owner TIANJIN MEDICAL UNIV
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