Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Use of deuterium oxide as an elastase inhibitor

A technology of elastase and deuterium oxide, applied in the field of deuterium oxide, can solve the problems of limited application due to molecular size, low bioavailability, non-specificity, etc.

Inactive Publication Date: 2011-04-13
D2 BIOSCI GROUP
View PDF5 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One risk is their non-specific proteolysis by other proteases (e.g. cysteine ​​proteases or metalloproteases), and the products of this reaction may introduce side effects (see Attucci et al., EP1-hNE4, a Proteolysis-Resistant Inhibitor of Human Neutrophil Elastase and Potential Anti-Inflammatory Drug for Treating Cystic Fibrosis, JPET318: 803-809, 2006)
In addition, such larger molecular HNE inhibitors have limited applications due to their molecular size, since specific inhibition of HNE requires a flexible configuration of the functional group in the inhibitor / substrate that binds to the catalytic triad of the enzyme
[0009] The disadvantages of the elastase inhibitors and in particular HNE inhibitors known in the prior art are mainly non-specific effects, undesired side effects, racemization, oxidation in strongly oxidative environments, very low bioavailability and risk of proteolysis by other proteases, thereby preventing its inhibitory activity or rendering it inactive

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Use of deuterium oxide as an elastase inhibitor
  • Use of deuterium oxide as an elastase inhibitor
  • Use of deuterium oxide as an elastase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0167] Example 1: Preparation of acrylic acid-based hydrogels

[0168] 2.0% by weight of Carbopol 980 (manufacturer: Noveon, Inc., 9911 Brecksville Rd., Cleveland, OH 44141-3247, USA) was dissolved in neat D by stirring in divided portions. 2 O, pure H 2 O or by D 2 O and H 2 O in the mixture, then titrated to pH 6.8 by titrating 10 M NaOH solution. The carboxyl groups of the polyacrylic acid are then crosslinked with the basic hydroxyl groups by the addition of NaOH, resulting in a colorless, transparent and optically clear acrylic gel (Carbopol gel) (D 2 O-Carbopol gel, H 2 O-Carbopol gel, D 2 O / H 2 O-Carbopol gel) was stored at room temperature for at least 24 hours until further application.

Embodiment 2

[0169] Embodiment 2: Preparation of hydrogel based on siloxane (Silicon)

[0170] 3.0% by weight of hexamethyldisiloxane (trade name SILMOGEN CARRIER from DOW Corning) and 1% by weight of ethanol were dissolved in neat D 2 O, pure H 2 O or by D 2 O and H 2 in a mixture of O. The above solution was then immediately mixed with the gel prepared according to Example 1 (Carbopol gel) in a weight ratio of 1:2 (silicone solution:Carbopol gel) under vigorous stirring until an optically clear gel was produced. (silicone gel) (D 2 O silicone gel, H 2 O silicone gel, D 2 O / H 2 O silicone gel). Store the gel at room temperature for at least 24 hours until further use.

Embodiment 3

[0171] Example 3: Preparation of alginate-based hydrogels

[0172] 4.0% by weight of sodium alginate (sodium alginate) (manufacturer: GmbH Armstadt, Deutschland) dispersed in pure D in divided portions by stirring 2 O, pure H 2 O or by D 2 O and H 2 O in the mixture, then titrated to pH 7.0 by titrating 10 M NaOH solution. The resulting tan, transparent gel (alginate gel) (D 2 O alginate gel, H 2 O alginate gel, D 2 O / H 2 O alginate gel) was stored at room temperature for at least 24 hours until further application.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to the use of deuterium oxide (D2O) as an elastase inhibitor and especially as an inhibitor of the human neutrophil elastase (HNE). The invention also relates to the use of deuterium oxide for the prophylaxis and / or treatment of HNE-related diseases.

Description

technical field [0001] The present invention relates to deuterium oxide (D 2 O) Use as an elastase inhibitor, in particular an inhibitor of human neutrophil elastase (HNE). The present invention also relates to the use of deuterium oxide for preventing and / or treating HNE-related diseases. Background technique [0002] Elastase belongs to the family of serine proteases that cleave the amide bond, thereby 2 Cleavage of peptides and proteins as well as esters under O conditions. Human elastase is encoded by six different genes, including humane Leukozyten-Elastase (HLE), also known as human neutrophil Elastase (HNE), (EC3.4.21.37 ). Human neutrophil elastase (HNE) is a glycolytic alkaline serine protease with a molecular weight of approximately 33 kDa and 218 amino acids. HNE is present in the azurophilic cyanogranules of human polymorphonuclear leukocytes (PMN). The intracellular physiological function of HNE is to degrade organic impurity particles ingested through pha...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/00A61P29/00A61P37/08A61P11/00A61P9/00
CPCA61K33/00A61P11/00A61P11/06A61P11/08A61P17/00A61P29/00A61P37/06A61P37/08A61P9/00
Inventor 托马斯·拜尔
Owner D2 BIOSCI GROUP
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com