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Metal-ion-containing non-linear polymer, and preparation and application thereof

A technology of metal ions and polymers, applied in medical preparations of non-active ingredients, preparations for in vivo tests, organic chemistry, etc., can solve problems such as troubles, changes in protein structure, and inability to screen for activity

Inactive Publication Date: 2014-12-17
韩文毅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Protein drugs are very important clinical drug treatments in the future, but at present, due to the stability and short half-life of protein drugs and many other shortcomings, it is impossible to effectively screen the activity in vivo after the potential effectiveness of protein drugs is determined in vitro.
Some scholars use polyethylene glycol to covalently link proteins for in vivo screening or treatment, but linking proteins in this way will change the protein structure, and it will be time-consuming, labor-intensive and expensive, which is very troublesome, especially the reaction time of covalent linking for hours, even days

Method used

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  • Metal-ion-containing non-linear polymer, and preparation and application thereof
  • Metal-ion-containing non-linear polymer, and preparation and application thereof
  • Metal-ion-containing non-linear polymer, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Dissolve 500mg of compound A (commercially available) in 6ml of water, put 600mg of sodium bicarbonate and 500mg of compound B (commercially available) in the same beaker for 15 hours, heat to 70 degrees and cool down, adjust the pH of the solution to 3 with acetic acid, and concentrate under reduced pressure , washed in ethanol, crystallized to obtain compound C, filtered with ethanol and washed again, and dried, 400 mg of compound D (commercially purchased) was dissolved in phosphate buffer at pH 7.5, and stirred with compound C for 2 hours, concentrated under reduced pressure, washed with ethanol , filtered and washed again, and dried to obtain compound E. Compound E and commercially available Y-type compound F containing polyethylene glycol were stirred in methanol solution for 6 hours to obtain compound G. Compound G was reacted with 2Mol NiCl2 to obtain Compound H.

[0078]

Embodiment 2

[0080] Dissolve 1000mg of compound A (commercially available) in 6ml of water, put 900mg of sodium bicarbonate and 1200mg of compound B (commercially available) in the same beaker for 24 hours, heat to 75 degrees and cool down, adjust the pH of the solution to 3.3 with acetic acid, and concentrate under reduced pressure , washed in ethanol, and crystallized to obtain compound C, which was filtered by ethanol and then washed and dried. 800 mg of compound D (commercially purchased) was dissolved in phosphate buffer at pH 7.5, and stirred with compound C for 2 hours, concentrated under reduced pressure, washed with ethanol , filtered and washed again, and dried to obtain compound E, compound E and commercially available Y-type compound F containing polyethylene glycol, stirred in methanol solution for 8 hours, reacted to obtain compound G, compound G and 3Mol NiCl 2 Compound H is obtained in the reaction.

[0081] The effect experiment is as follows:

[0082] For example TRAIL (...

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PUM

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Abstract

The invention discloses a new metal-ion-containing non-linear polymer, and a preparation method and application of the new non-linear polymer. The non-linear new compound is constructed by utilizing a compound with a branch structure, and by combining the new structure non-covalent bond and correlated protein possessing potential treatment effect and to be subjected to in-vivo screening, protein with potential treatment activity is rapidly conveniently screened in vivo by combining an animal model. When being used for screening protein, the new non-linear compound containing a metal ion structure comprises the following characteristics that 1, screening is rapid and convenient, the time for combining protein for in-vivo activity screening is less than 15 min; and 2, the in-vivo screening process does not change the protein structure, and the new non-linear compound does not have a covalent linkage reaction with protein when screening is performed.

Description

technical field [0001] The invention discloses a non-linear polymer containing a metal ion structure as well as a preparation method and application of the polymer. Background technique [0002] Protein drugs are very important clinical drug treatments in the future, but at present, due to the stability and short half-life of protein drugs and many other shortcomings, it is impossible to effectively screen the activity in vivo after the potential effectiveness of protein drugs is determined in vitro. Some scholars use polyethylene glycol to covalently link proteins for in vivo screening or treatment, but linking proteins in this way will change the protein structure, and it will be time-consuming, labor-intensive and expensive, which is very troublesome, especially the reaction time of covalent linking As many as several hours, even days. In the present invention, a new nonlinear compound containing a metal ion structure is prepared, and a compound with a branched structure...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G65/48C07D207/416A61K49/00A61K47/48
Inventor 韩文毅丁镇
Owner 韩文毅
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