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

Application of calycosin derivative to preparation of medicines for restraining proliferation of endothelial cells

An endothelial cell proliferation and drug technology, applied in the field of medicine, can solve the problems of large effective concentration and unclear target

Active Publication Date: 2020-05-19
GUILIN MEDICAL UNIVERSITY
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Existing studies have shown that calycosin has the functions of anti-oxidative stress, anti-virus and regulation of cell apoptosis, but its disadvantage is that its effective concentration is relatively large and its target is not clear

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
  • Application of calycosin derivative to preparation of medicines for restraining proliferation of endothelial cells
  • Application of calycosin derivative to preparation of medicines for restraining proliferation of endothelial cells
  • Application of calycosin derivative to preparation of medicines for restraining proliferation of endothelial cells

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1: Synthesis of the compound represented by formula (I) used in the following experimental examples of this application:

[0028] Specifically synthesized according to the following synthetic route:

[0029]

[0030] Among them, the chemical name of compound 1 is: 7-hydroxy-3-(3-hydroxy-4-methoxy)-4H-benzopyran-4-one, and compound 2 is ethyl chloroacetate.

[0031] The specific synthesis method is:

[0032] Take 1g (3.52mmol) of compound 1 (mullin isoflavone) in a 50ml round bottom flask and dissolve it with 40ml of acetone, then add 3g of anhydrous K 2 CO 3 And 0.5g of NaI, stirred at room temperature for 1h, then added 0.91g (7.43mmol) of compound 2 (ethyl chloroacetate) dropwise, then placed in a water bath at 45°C and stirred at reflux for 4h (TCL monitors the reaction, the developing solvent is chloroform: methanol=60: 1. Volume ratio); then stop heating and continue stirring until cooling. Add ice water to the cooled reaction, filter, collect the precipitate, dis...

experiment example 1

[0043] Experimental example 1: MTT method to detect endothelial cell proliferation

[0044] Take HUVECs that grow to 90% confluence, wash and digest them to prepare cell suspension. After counting, press 5x10 3 / Well inoculated in 96-well plate. After the cells were fully adhered to the wall after 24 hours of culture, the upper layer of culture medium was removed, and 100 μl of low serum hormone-free culture medium (0.5% CS-FBS) was added to each well and cultured for 24 hours to synchronize the cell status. The experimental group was set up with different concentrations of CAG002 (0.1μM~32μM) dosing groups, each group had 6 multiple wells, and 200μl / well was added with drug-containing low serum culture medium. At the same time, a control was set. The blank control group was 0.1% DMSO culture solution, and the positive control was Calycosin.

[0045] MTT results showed that as the concentration of CAG002 increased, its inhibitory effect on HUVECs gradually increased. When the dru...

experiment example 2

[0046] Experimental example 2: Plate cloning experiment

[0047] HUVEC was seeded in a 6-well plate at low density (500 cells / well in triplicate) and cultured for two weeks. Then, the cells were washed twice with PBS, fixed with 4% paraformaldehyde for 15 minutes, and stained with Gram staining solution for 20 minutes. The experimental results showed that with the increase of the concentration of CAG002, the number of HUVECs cloned cells decreased significantly, and the effect was most obvious at 16μM.

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 discloses an application of a calycosin derivative to preparation of medicines for restraining proliferation of endothelial cells. Through experiment, the applicant finds that the calycosin derivative can effectively reduce the expression level of EWSAT1 and TRAF6, through comparison with past literature study results, a compound as shown in a formula (I) can better restrain the proliferation of the endothelial cells than calycosin, so that the compound hopefully becomes an estrogen substitute product. The calycosin derivative disclosed by the invention has the structure as shownin the formula (I): as shown in the description.

Description

Technical field [0001] The invention relates to the application of a verbasil derivative in the preparation of drugs for inhibiting the proliferation of endothelial cells, and belongs to the technical field of medicine. Background technique [0002] With the rapid development of society and economy, people's living standards have gradually improved, and the incidence of cancer has been increasing year by year, which has become the number one killer that seriously affects human health. Cancer cells have the ability to proliferate indefinitely. Their continuous proliferation requires a large amount of supply of nutrients and oxygen, and the supply of these nutrients and oxygen is achieved through the transportation of blood vessels. Blood vessel growth is a process called angiogenesis, a complex and coordinated process involving multiple cell cytokines and signal pathways. Various factors stimulate the proliferation, differentiation and metastasis of vascular endothelial cells, pr...

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): A61K31/352A61P35/00
CPCA61K31/352A61P35/00
Inventor 陈健王勇李鑫任倩瑶秦俭陈晓宇
Owner GUILIN MEDICAL UNIVERSITY
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