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

Vanadium oxide complex as well as preparation method and application thereof

A technology of complexes and vanadyl, which is applied in the direction of pharmaceutical formulations, chemical instruments and methods, and medical preparations containing active ingredients, etc., can solve problems that have not been reported, and achieve easy-to-obtain raw materials, activity inhibition, and simple synthesis methods Effect

Inactive Publication Date: 2013-08-07
SHANXI UNIV
View PDF1 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to BMOV, some complexes with coordination forms of VO(N2O2), VO(O2S2), VO(N2S2), VO(N4), and VO(S4) also have insulin-like properties, but the coordination form is VO2( The insulin-like properties of NSO) complexes have not been reported, so we prepared and studied Schiff base vanadyl complexes with insulin-like properties based on the PTP1B target, which provides a new drug development approach for the treatment of diabetes

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
  • Vanadium oxide complex as well as preparation method and application thereof
  • Vanadium oxide complex as well as preparation method and application thereof
  • Vanadium oxide complex as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Preparation of complexes

[0026] (1) Synthesis of 4-amino-5-mercapto-1,2,4-triazole: Take 10mmol (1.06g) of bisthiosemicarbazide in a round bottom flask, add 10mL of formic acid solution, stir and reflux for 4h, cool to room temperature, Unreacted formic acid was distilled off under reduced pressure, washed with water to obtain a crude product, and recrystallized with water to obtain a white crystalline product;

[0027] (2) Synthesis of 5-chlorosalicylaldehyde-4-amino-5-mercapto-1,2,4-triazole Schiff base ligand: Take 5mmol (0.58g) of 4-amino-5-mercapto-1, Add 50ml of absolute ethanol to dissolve 2,4-triazole in a round bottom flask, add dropwise 5mmol (0.78g) of 5-chlorosalicylaldehyde in absolute ethanol solution 40ml and 0.4ml of concentrated sulfuric acid under stirring, a large amount of light Yellow precipitate, after heating to reflux for 4 hours, cooling, filtering, recrystallization of solid powder in absolute ethanol, and precipitation of light yellow micro...

Embodiment 2

[0038] Example 2 Detection of the inhibitory effect of the vanadyl complexes of the present invention on PTP1B.

[0039]The vanadyl complex crystals were dissolved in dimethyl sulfoxide (DMSO) to prepare 10 -2 The mother liquor of M was diluted with DMSO into solutions of different concentrations (10 -4 M, 10 -5 M, 10 -6 M, 10 -7 M, 10 -8 M, 10 -9 M, 10 -10 M). The enzyme activity inhibition test was carried out with 2mM p-nitrophenyl phosphate disodium salt (pNPP) as the reaction substrate in the MOPS buffer system [20mM morpholinopropanesulfonic acid (MOPS), 50mM NaCl] at pH 7.20 , the experimental method is as follows: this experiment is carried out in a 96-well plate, 83 μl of enzyme-containing buffer solution, 10 μl of inhibitors with different concentration gradients are sequentially added, and 2 μl (0.1M) of pNPP is used to start the reaction, and after standing for about 15 minutes, add 5 μl (2M) of NaOH was used to stop the reaction, and the degradation produc...

Embodiment 3

[0040] Example 3 Determination of the type of inhibition of PTP1B by the vanadyl complexes of the present invention.

[0041] The vanadyl complex crystals were dissolved in dimethyl sulfoxide (DMSO) to prepare 10 -2 The mother solution of M was diluted with DMSO into solutions of different concentrations (200nM, 100nM, 50nM, 25nM), and the concentrations of the substrate pNPP were 4mM, 2mM, 1mM, 0.5mM, 0.3mM, 0.2mM. The experimental reaction system is: 88 μl enzyme-containing (PTP1B) buffer solution containing: 20 mM morpholinopropanesulfonic acid (MOPS), 50 mM NaCl, 10 μl inhibitors with different concentration gradients, and 2 μl different concentrations of pNPP are added to the reaction system to start the reaction. Measure the change in light absorption. Measure the absorbance value of each inhibitor concentration to each substrate concentration, according to the formula A=εbc (b=1cm, ε=1.78×10 4 , A is the absorbance at 405nm, and C is the reactant concentration mol / L) ...

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 provides a vanadium oxide complexa and a preparation method thereof and an application of the complex as a protein tyrosine phosphatase 1B (PTP1B) inhibitor. The vanadium oxide complex provided by the invention is 5-chloro-salicyladehyde condens-4-amino-5-sulfydryl-1, 2, 4- triazole Schiff base vanadium oxide. The preparation method of the vanadium oxide complex comprises steps of: dissolving a 5-chloro-salicyladehyde condens-4-amino-5-sulfydryl-1, 2, 4- triazole Schiff base ligand into absolute ethyl alcohol; dripping triethylamine of the same molar weight; heating and stirring the ligand to be dissolved; and then adding the absolute ethyl alcohol solution with the dissolved triethylamine the molar weight of which is the same as that of absolute ethyl alcohol solution, stirring, refluxing, cooling, filtering, collecting a mother liquid and separating yellow massive crystals out. The complex is simple in synthesizing method, is prepared by easily obtained raw materials, and has an obvious inhibition function on the activity of PTP1B with nanomolar concentration; and the prepared complex can be used as the protein tyrosine phosphatase 1B inhibitor.

Description

technical field [0001] The invention relates to a transition metal complex, in particular to a vanadyl complex, a preparation method thereof, and an application of the complex as an inhibitor of protein tyrosine phosphatase 1B. Background technique [0002] Protein tyrosine phosphatases (PTPs) are a class of metal-free enzymes that widely exist in organisms. They work with protein kinases to regulate the reversible dynamic process of protein tyrosine phosphorylation. Phosphorylate proteins and protein kinases dephosphorylate proteins. In humans, more than 100 PTPs are thought to be involved in various pathways that enhance or inhibit signal transduction. PTPs can regulate the cell cycle and signal transduction. In terms of cell signal response, it can regulate the degree of protein tyrosine phosphorylation by combining with protein tyrosine phosphokinase. Aberrant regulatory pathways of these signaling systems have been found to be associated with many diseases. Abnormal ...

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
IPC IPC(8): C07F9/00A61K31/555A61P3/10A61P5/50
Inventor 袁彩霞卢丽萍朱苗力
Owner SHANXI 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