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Medicine use of cyclodextrin derivs. and medicine composition thereof

A technology of cyclodextrin and derivatives, applied in the fields of medicinal chemistry and pharmaceutical preparations, can solve the problems of poor water solubility and low activity

Inactive Publication Date: 2003-10-29
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a drug, the biggest disadvantage of PZ51 is its low activity and poor water solubility. In order to make up for the deficiency of PZ51 and solve the common problems of low activity and poor water solubility of GPX small molecule mimics, we chose cyclodextrin as the enzyme model and synthesized a A series of cyclodextrin derivatives to mimic GPX, we found that these cyclodextrin derivatives have a variety of pharmaceutical activities, can be used to treat a variety of diseases

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 100mg NaBH 4 Dissolve in a vial with 5ml of water, then slowly add 100mg of selenium powder to NaBH 4 In the solution, cover a plastic cover with a needle inserted, at this time, you can see that a large amount of gas is generated in the water, accompanied by heat release. Because the reaction is too violent, it needs to be carried out in an ice bath to control the reaction speed. The reaction equation is as follows: due to NaBH 4 with H + reaction, accompanied by a small amount of H 2 Se gas is produced, and it must be reacted in a fume hood to prevent poisoning. After the reaction, a large amount of salt precipitated out. NaHSe is very easy to oxidize, so N 2 save. Example 2: Synthesis of 2-Se-β-CD (i.e. 2-selenium bridged β-cyclodextrin) The synthetic route is as follows: (1). 2-position sulfonylation of β-CD (the product is β-CD-2-hydroxybenzenesulfonate, referred to as 2-OTs-β-CD):

Embodiment 2

[0019] 100mg NaBH 4 Dissolve in a vial with 5ml of water, then slowly add 100mg of selenium powder to NaBH 4 In the solution, cover a plastic cover with a needle inserted, at this time, you can see that a large amount of gas is generated in the water, accompanied by heat release. Because the reaction is too violent, it needs to be carried out in an ice bath to control the reaction speed. The reaction equation is as follows: due to NaBH 4 with H + reaction, accompanied by a small amount of H 2 Se gas is produced, and it must be reacted in a fume hood to prevent poisoning. After the reaction, a large amount of salt precipitated out. NaHSe is very easy to oxidize, so N 2 save. Example 2: Synthesis of 2-Se-β-CD (i.e. 2-selenium bridged β-cyclodextrin) The synthetic route is as follows: (1). 2-position sulfonylation of β-CD (the product is β-CD-2-hydroxybenzenesulfonate, referred to as 2-OTs-β-CD):

[0020] Dissolve 2.0g of β-CD in 100ml of NaOH (0.3mol / L) solution, ...

Embodiment 3

[0021] Dissolve 100mg of 2-OTs-β-CD in 50mM phosphate buffer, pass high-purity nitrogen to deoxygenate, add 100μl 1M NaHSe, react at 60°C for 36 hours, then fully expose the reaction system to oxidation in the air, centrifuge to remove selenium, and The supernatant was separated and purified by Bio-gel P-2 column (5.0×50cm), the first peak was collected by 254nm ultraviolet monitoring, freeze-dried, washed three times with acetone, and vacuum-dried to give the title compound 2-Se-β-CD as light yellow powder . Embodiment 3: 6-Se-β-CD (that is, 6-selenium-β-cyclodextrin) synthetic method The synthetic route is as follows: (1). Synthesis of 6-p-toluenesulfonyl-β-cyclodextrin (6-OTs-β-CD)

[0022] After β-CD was recrystallized, it was vacuum-dried at 120°C for one day, and the pyridine was refluxed with KOH for 17 hours, then dried with BaO overnight, and then distilled at atmospheric pressure. 3.6g of p-TsCl was dissolved in 10mL of pyridine, and the pyridine solution of p-TsC...

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Abstract

A cyclodextrin derivative for preventing and treating cardiovascular and cerebrovascular diseases, diabetes, liver injury, diseases in respiratory system, rheumatic and rheumatoid diseases, dermatopathy and tumor is disclosed. It is an artificial analogue enzyme with the activity of glutathion peroxidase.

Description

Technical field: [0001] The present invention relates to the fields of medicinal chemistry and pharmaceutical preparations, in particular, the present invention relates to new pharmaceutical uses of cyclodextrin derivatives and pharmaceutical compositions thereof. Background technique: [0002] Simulating the microenvironment of enzyme active sites at the molecular level, introducing factors that play a leading role in catalytic reactions in natural enzymes, and designing and synthesizing organic molecules with simple structures and stable activities as artificial simulated enzymes are the frontiers in the field of natural science today. one of the subjects. In view of the fact that the artificial enzyme molecule may have the same specificity and catalytic function as the natural enzyme, and has the advantages of stable physical and chemical properties, wide and easy access to raw materials, and simple preparation process, it indicates that it has great potential in the fiel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/718A61P1/16A61P3/10A61P9/10A61P11/00A61P17/00A61P29/00A61P35/00C08B37/16
Inventor 罗贵民阎岗林贾志丹牟颖任晓君刘俊秋张鲲沈家聪
Owner JILIN UNIV
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