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

Folic acid modification of chitosan nucleophilic NO donator and compounding method thereof

A chitosan and modified technology, applied in the field of medical engineering, can solve problems such as low utilization rate, and achieve the effects of preventing restenosis, long release half-life, and promoting wound healing.

Inactive Publication Date: 2008-07-23
SHANGHAI JIAO TONG UNIV
View PDF1 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the present invention, chitosan is modified by carboxylation to generate NH nucleophilic sites, and after reacting with NO, a series of [N(O)NO] containing [N(O)NO] - A new type of NO donor with functional groups, which solves the current problems (lower utilization) of this type of nucleophilic NO donor in clinical applications

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
  • Folic acid modification of chitosan nucleophilic NO donator and compounding method thereof
  • Folic acid modification of chitosan nucleophilic NO donator and compounding method thereof
  • Folic acid modification of chitosan nucleophilic NO donator and compounding method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the synthesis of folic acid (FA) modified 400,000 molecular weight chitosan (CS) / NO (molar ratio: FA / CS=2 / 1)

[0021] Accurately weigh 1.61g of chitosan (molecular weight: 400,000) sample, add 100ml of 1% acetic acid and stir until completely dissolved, adjust the pH value of the solution to 4.7, filter the solution with a disposable syringe filter and add it to a round bottom flask . Weigh 2.17g of folic acid and dissolve it in 30ml of dimethyl sulfoxide, stir it with magnetic force until it is completely dissolved, then add 0.5g of dicyclohexylcarbodiimide to the folic acid solution, and mix until it dissolves. The folic acid solution added with dicyclohexylcarbodiimide was added to the chitosan solution, and stirred and reacted in a water bath at 37° C. for 7 days. Adjust the pH value to 9.0 to terminate the reaction, dialyze the reaction product with a phosphate buffer solution with a pH value of 7.4 for 3 days, and then dialyze it with ultrapure wate...

Embodiment 2

[0024] Embodiment 2: the synthesis (molar ratio: FA / CS=1 / 1) of folic acid (FA) modified 1.24 million molecular weight chitosan (CS) / NO

[0025] Accurately weigh 1.61g of chitosan (molecular weight: 1.24 million) sample, add 100ml of 1% acetic acid and stir until completely dissolved, adjust the pH value of the solution to 4.7, filter the solution with a disposable syringe filter and add it to a round bottom flask . Weigh 4.34g of folic acid and dissolve it in 30ml of dimethyl sulfoxide, stir it with magnetic force until it is completely dissolved, then add 0.5g of dicyclohexylcarbodiimide to the folic acid solution, and mix until it dissolves. The folic acid solution added with dicyclohexylcarbodiimide was added to the chitosan solution, and stirred and reacted in a water bath at 37° C. for 7 days. Adjust the pH value to 9.0 to terminate the reaction, dialyze the reaction product with a phosphate buffer solution with a pH value of 7.4 for 3 days, and then dialyze it with ultr...

Embodiment 3

[0028] Embodiment 3: the synthetic (molar ratio: FA / CS=1 / 2) of folic acid (FA) modified 1.88 million molecular weight chitosan (CS) / NO

[0029] Accurately weigh 1.61g of chitosan (molecular weight 1.88 million) sample, add 100ml of acetic acid and stir until completely dissolved, adjust the pH value of the solution to 4.7, filter the solution with a disposable syringe filter and add it to a round bottom flask. Weigh 8.68g of folic acid and dissolve it in 30ml of dimethylsulfoxide, stir it with magnetic force until it is completely dissolved, then add 0.5g of dicyclohexylcarbodiimide to the folic acid solution, and mix until it dissolves. The folic acid solution added with dicyclohexylcarbodiimide was added to the chitosan solution, and stirred and reacted in a water bath at 37° C. for 7 days. Adjust the pH value to 9.0 to terminate the reaction, dialyze the reaction product with a phosphate buffer solution with a pH value of 7.4 for 3 days, and then dialyze it with ultrapure w...

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

PropertyMeasurementUnit
degree of graftingaaaaaaaaaa
degree of graftingaaaaaaaaaa
Login to View More

Abstract

The invention relates to a folic acid modified chitosan nucleophilic NO donor and a synthetic method for the folic acid modified chitosan NO donor and belongs to the field of medical engineering technology. The invention makes acylation modification to NH2 group on the chitosan to lead the NH2 to generate nucleophilic NH group which can react with NO; a secondary amine NH group on a folic acid modified chitosan molecule reacts with NO air molecules in methanol solution of sodium methylate to generate an (N(O)NO) <minus> group, and Na <plus> / NH is equal to 2 and a molecular structural formula of the obtained folic acid modified chitosan Nitric Oxide donor is provided. The nucleophilic NO donor of the invention provided with different NO release rates and longer half-life periods can overcome the weak points of non-specificity and targeting of the NO release, improve the utilization efficiency of NO and at the same time, the invention can overcome the cytotoxicity of nucleophilic agents (polyamines) and prevent the generation of carcinogenic by-product nitrosamine.

Description

technical field [0001] The invention relates to a medicine in the technical field of medical engineering and a synthesis method thereof, in particular to a folic acid modified chitosan nucleophilic NO donor and a synthesis method thereof. Background technique [0002] Nitric oxide (NO) is an endothelial-induced relaxation factor that plays an important role in regulating vascular tone, blood pressure, smooth muscle proliferation and platelet aggregation. Currently, controlled release of NO at the site of injury has been identified as one of the most promising approaches to prevent restenosis. An effective approach to treating patients with cardiovascular disease is the use of anticoagulant and antiplatelet agents that prevent further ischemic events and reduce the probability of death from thrombosis-related arterial disease. Contains nucleophilic nitric oxide donor [N(O)NO] - Compounds with functional groups are one of the most important NO donor drugs developed in recent...

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): A61K47/48A61K47/36C08B37/08A61K47/61
Inventor 万锕俊孙燕李慧丽张隐西
Owner SHANGHAI JIAO TONG UNIV
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