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Medicine target for preventing and treating cardiovascular and cerebrovascular diseases associated with inflammation and its inhibitor

A technology for cardiovascular and cerebrovascular diseases and inhibitors, which is applied in the field of drug targets and inhibitors for the prevention and treatment of inflammation-related cardiovascular and cerebrovascular diseases. question

Active Publication Date: 2008-02-20
TIANJIN TASLY PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the solid-phase specific elution method is easily affected by the dissociation speed of the "affinity column-target protein" complex, and it is necessary to prepare a control column with no active structure similar to the drug; the drug competition method will precipitate with the insoluble drug , which requires high drug solubility
Serial affinity chromatography is a new affinity chromatography method reported in 2006 that can overcome the above shortcomings, but it has not been applied to the target discovery of natural compounds so far

Method used

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  • Medicine target for preventing and treating cardiovascular and cerebrovascular diseases associated with inflammation and its inhibitor
  • Medicine target for preventing and treating cardiovascular and cerebrovascular diseases associated with inflammation and its inhibitor
  • Medicine target for preventing and treating cardiovascular and cerebrovascular diseases associated with inflammation and its inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Preparation and activity verification of EAH Sepharose 4B-RUS-2HS affinity column

[0020] 1. Experimental materials

[0021] 1.1 Cells and cell lines

[0022] ECV304 cell line, HL-60 cell line, and primary macrophages were obtained from the peritoneal fluid of healthy mice.

[0023] 1.2 Drugs and reagents

[0024] Ruscogenin (purity greater than 98%); succinic anhydride; EAH Sepharose 4B agarose gel (Amersham Biosciences); 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide ( EDC, Sigma); Dexamethasone Sodium Phosphate Injection; Nimotop; Recombinant Human Tumor Necrosis Factor-α; Hydrocortisone; Lipopolysaccharide; Thiazolium Blue.

[0025] 2 Experimental methods

[0026]The synthesis of ruscogenin succinate monoester (RUS-2HS) and the preparation of EAH Sepharose 4B-RUS-2HS affinity column, the preparation method can be found in the literature published by the inventor: using ruscogenin as ligand Preparation of affinity chromatography column and its application in an...

Embodiment 2

[0035] Searching for specific binding proteins of Ruscogenin in cells and tissues related to cardiovascular and cerebrovascular diseases by using series affinity chromatography

[0036] 1. Experimental materials

[0037] 1.1 Cells and cell lines

[0038] ECV304 cell line, primary human umbilical vein endothelial cells.

[0039] 1.2 Animals

[0040] Male SD rats, 250-340g.

[0041] 1.3 Drugs and reagents

[0042] The cell lysate and tissue protein lysate are general-purpose non-denatured protein lysates, and PMSF, leupeptin, aprotinin, trypsin inhibitor; BeadBuffer; BCA protein concentration determination kit (Beiyuntian) were added before use.

[0043] 2. Experimental method

[0044] 2.1 Preparation of cell and tissue protein solution

[0045] 2.1.1 Preparation of cell protein solution

[0046] Discard the cell culture medium, wash with PBS (containing 0.05mmol·L -1 PMSF) and washed twice. The cells were scraped off with a scraper, collected in a centrifuge tube of a...

Embodiment 3

[0058] Functional verification of Ruscogenin-specific binding protein MyH9

[0059] Numerous studies have shown that Ruscogenin has significant anti-inflammatory and antithrombotic activities. The present invention adopts: ① TNF-α-activated ECV304 cells adhere to HL-60 cells; ② TNF-α-activated ECV304 cells express tissue factor (TF) closely related to cardiovascular and cerebrovascular diseases; ③ lipopolysaccharide-induced macrophage Cell release NO experiment, to verify whether MyH9 is the target protein of Ruscogenin activity.

[0060] 1. Experimental materials

[0061] Human prothrombin complex (Hualan Bioengineering Co., Ltd.), Factor Xa Chromogenic substrate (Sigma), and others are the same as in Example 1.

[0062] 2. Experimental methods and results

[0063] 2.1 The effects of MyH9-specific inhibitors blebbistatin and Ruscogenin on the adhesion of TNF-α-activated ECV304 to HL-60 cells.

[0064] The experimental method for the effect of drugs on the adhesion of HL-6...

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Abstract

The present invention relates to a new drug target for the prevention and the treatment of cerebrovascular diseases related to inflammation and the medical usage of the inhibitors thereof, more particularly, the present invention relates to the nonmuscle myosin heavy chain 9(MyH9) used as the new drug target for the prevention and the treatment of cerebrovascular diseases related to inflammation and the usage of the inhibitors ruscogenin and the genin in the prevention and the treatment of the tumor differentiation and metastasis, glaucoma and other diseases.

Description

technical field [0001] The present invention relates to a new drug target for preventing and treating inflammation-related cardiovascular and cerebrovascular diseases and the medical use of its inhibitor, specifically, nonmuscle myosin heavy chain 9 (MyH9) as a therapeutic agent for preventing and treating inflammation-related cardiovascular and cerebrovascular diseases New drug targets for diseases and their inhibitors, ruscogenin and its glycosides, are used in the prevention and treatment of tumor differentiation and metastasis, glaucoma and other diseases. technical background [0002] Drug innovation research mainly includes two aspects, one is compound innovation, that is, discovering new structural types of active compounds based on existing targets; the other is drug target innovation, that is, the comprehensive application of chemical biology, molecular biology, pharmacology, bioinformatics, etc. Methods To discover new drug targets, new mechanisms of action and a s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/58A61K31/7048A61K31/437A61P9/06A61P9/10A61P29/00A61P27/06A61P35/00A61P35/04G01N33/68
Inventor 余伯阳寇俊萍黄娅琳蒋文雯刘吉华
Owner TIANJIN TASLY PHARMA CO LTD
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