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

Luteolin and application of pharmaceutical composition thereof

A technology of luteolin and composition, applied in the field of medicine, can solve the problems of restricting the clinical application of neurodegenerative disease treatment, difficult to penetrate NGF, etc., and achieve the effect of good clinical application prospect and function improvement effect.

Pending Publication Date: 2022-04-01
THE HONG KONG UNIV OF SCI & TECH
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, NGF is difficult to penetrate the blood-brain barrier, which restricts its clinical application in the treatment of neurodegenerative diseases

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
  • Luteolin and application of pharmaceutical composition thereof
  • Luteolin and application of pharmaceutical composition thereof
  • Luteolin and application of pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1: Luteolin combined with NGF

[0063] 1. Method: using Schrödinger molecular docking software ( The company's Maestro software ver.11.9) was used to analyze the combination of luteolin and NGF. Import the 3D crystal structure of NGF into the software, and use the software's protein preparation program to delete water molecules, fill in missing residues, and optimize hydrogen atoms. Potential binding sites were then detected and docked boxes generated. Luteolin as a ligand was docked with the box using the Glide program after 3D processing. The results are as follows figure 1 As shown in A.

[0064] The direct binding of luteolin to NGF was detected by ultrafiltration. In 500 μL of 10 mM Tris-HCl buffer (pH 7.4), 1 μM luteolin was incubated with 100 nM NGF at 4° C. for 1 hour, and the control group was not added with NGF. The solution was then transferred to an ultrafiltration tube (Vivacon 500; cut-off 2000MW; Sartorius Stedim Biotech), and NGF was retai...

Embodiment 2

[0067] Example 2: Luteolin synergizes with NGF to activate neurofilament-encoding gene promoters

[0068] 1. Method: put 8×10 4 cells / mL The rat adrenal medulla pheochromoma differentiated cell line (PC12 cells) was planted on a 24-well cell culture plate, and the medium was DMEM medium, 6% fetal bovine serum + 6% horse serum. After 24 hours, luciferase reporter gene vectors pNF68-Luc and pNF200-Luc containing neurofilament-encoding gene promoters were transfected into PC12 cells. After 4 hours, change to low serum medium (DMEM medium, 1% fetal calf serum + 1% horse serum), then add figure 2 Each figure shows different final concentrations of luteolin and NGF. After 48 hours, the cell culture medium was removed and rinsed with PBS. After the lysate (100 mM PBS, 1 mM DTT, 0.2% Triton X-100, pH 7.8) was lysed, it was centrifuged at a high speed of 12000 g for 15 minutes to obtain a cell lysate containing luciferase. 50 μL of the cell lysate was transferred to a light-tight ...

Embodiment 3

[0070] Example 3: Luteolin can cooperate with NGF to promote the expression of neurofilaments

[0071] 1. Method: In order to study the expression of neurofilament, 8×10 4cells / mL PC12 cells were inoculated into 12-well plates, cultured with normal serum (DMEM medium, 6% fetal calf serum + 6% horse serum) for 24 hours, and then transferred to low serum medium (DMEM medium, 1% fetal bovine serum) Serum + 1% horse serum) for 24 hours, then add luteolin with a final concentration of 5 μM and NGF with a final concentration of 0.5ng / mL for 48 hours, to add a final concentration of 50ng / mL NGF alone, add a final concentration of NGF alone 5μM luteolin, NGF with a final concentration of 0.5ng / mL alone, no luteolin and NGF were used as the control group. After the lysate (10×cell lysis buffer, #9803Cell signaling technology company) was lysed, the cell debris was removed by high-speed centrifugation at 12000g, the total protein concentration in the supernatant was determined, and the...

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 an application of luteolin in preparation of a medicine for enhancing the function of a nerve growth factor, a pharmaceutical composition containing the luteolin and an application of the pharmaceutical composition. The invention finds a new application of luteolin in promoting the function of the nerve growth factor, and the luteolin can cooperate with the nerve growth factor to induce nerve cell differentiation and is used for preparing medicines for treating and preventing nerve growth factor dependent nervous system diseases such as Alzheimer's disease, Parkinson's disease, depression, brain injury, spinal cord injury and the like. The clinical application prospect is good.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular, it relates to a new application of luteolin, a pharmaceutical composition and its application. Background technique [0002] Neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and depression are worldwide public health problems. Nerve growth factor (NGF) is a key regulator of neuron development, growth, maintenance and plasticity regulation, and has been proven to be used in the treatment of neurodegenerative diseases. Mature nerve growth factor is a dimer composed of two subunits of about 13.5kDa non-covalently bound, each subunit is composed of two pairs of antiparallel β-strands, including 3 pairs of disulfide bonds . NGF interacts with its high-affinity receptor tyrosine kinase receptor A (TrkA), and promotes neuronal differentiation and maintenance through various signaling cascades. [0003] However, because NGF is difficult to penetrate the bloo...

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): A61K31/352A61K38/18A61P25/28A61P25/16A61P25/24A61P25/00
Inventor 詹华强高雄董婷霞
Owner THE HONG KONG UNIV OF SCI & TECH
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