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

Application of lactan compound to preparation of neuritis inhibiting drugs

A technology for lactams and neuroinflammation, applied to the application field of lactams in the preparation of drugs for inhibiting neuroinflammation, can solve the problems of complex pathogenesis of ND, special parts, lack of therapeutic drugs, etc., and achieves high clinical application value and Development prospects, effect of suppressing neuroinflammatory activity

Inactive Publication Date: 2018-05-11
NINGXIA MEDICAL UNIV
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the complex pathogenesis and special location of ND, there is still a lack of effective therapeutic drugs.

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 lactan compound to preparation of neuritis inhibiting drugs
  • Application of lactan compound to preparation of neuritis inhibiting drugs
  • Application of lactan compound to preparation of neuritis inhibiting drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Inhibitory effect of tamaractam on LPS-induced nitric oxide (NO) release from microglia by Griess colorimetry;

[0035] Cell line: mouse microglial cell line BV-2;

[0036] Drugs: LPS; tamaractam; minocycline (MINO).

[0037] method:

[0038] (1) Culture of mouse microglial cell line BV-2:

[0039] The cell culture solution was prepared based on DMEM medium, containing 10% FBS, 100 U penicillin and 100 U streptomycin, and 50 μM 2-mercaptoethanol (both final concentrations). at 5% CO 2 , under the condition of 37 ℃, the BV-2 microglial cells were divided into about 4×10 5 The cell density of cells / ml was cultured in a cell culture incubator, and the growth of the cells was observed regularly. When the area of ​​the cell adherence accounted for about 50-60% of the bottom area of ​​the culture flask, the cells were digested with trypsin and passaged, and then continued to culture. Take 3-7 generations of cells for experiments.

[0040] (2) Determination of nitrite co...

Embodiment 2

[0047] DCFH oxidation was used to investigate the effect of tamaractam on the release of reactive oxygen species (ROS) from microglia induced by LPS;

[0048] Cell line: mouse microglial cell line BV-2;

[0049] Drugs: LPS; tamaractam; MINO.

[0050] Experimental principle: DCFH-DA (2′,7′-dichlorodihydrofluororescein diacetate) can enter the cell and undergo a deacetylation reaction to generate DCFH. DCFH is a non-fluorescent substance, which can be oxidized by intracellular ROS to generate fluorescent substance DCF, and the amount of ROS release can be reflected by detecting the fluorescence intensity. The specific operation steps are as follows: DCFH-DA was dissolved in pure methanol to prepare a mother solution with a concentration of 10 mM, and the mother solution was diluted 500 times with Hank's balanced salt solution (HBSS) to a final concentration of 20 μM before use. Take the BV-2 cells after drug treatment, suck the supernatant, incubate with the 20 μM DCFH-DA solu...

Embodiment 3

[0054] The effects of tamaractam on LPS-induced release of tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) from microglial cells were investigated by ELISA;

[0055] Cell line: mouse microglial cell line BV-2;

[0056] Drugs: LPS; tamaractam; MINO.

[0057] Detection method: Take BV-2 cells in the logarithmic growth phase, inoculate the cells in a 6-well plate with fresh serum-free DMEM medium, and the cell density is 3×10 5 cells / ml, inoculum volume 600μl / well, placed in an incubator at 37°C, 5% CO 2 cultivated under conditions. After the cells adhered to the wall for 3 hours, the culture solution was carefully sucked out, and according to the experimental group, the cells were replaced with different drugs prepared in serum-free DMEM culture solution to incubate the cells. At the same time, a blank control group was set up, and each group was set with 3 replicate wells, and the drug addition to the cells continued. After culturing for 2-4 hours, collect the sup...

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 application of a lactan compound to preparation of neuritis inhibiting drugs. According to the application, the condition that a lactan compound tamaractam has remarkable neuritis inhibiting activity is proven through pharmacological experiments for the first time, and the tamaractam can be used for preparing the drugs for preventing and / or treating neuritis, thereby having a relatively high clinical application value and development prospect. The invention provides application of the lactan compound tamaractam in the aspect of neuritis inhibiting. Tamaractam has a structural formula represented by a formula I. Proven by the pharmacological experiments, the compound can be used for remarkably inhibiting the release of LPS induced microglia inflammatory mediators, i.e., NO, ROS, TNF-alpha and IL-1beta and has remarkable neuritis inhibiting activity. Therefore, the compound can be used for preparing the drugs for preventing and / or treating the neuritis and has arelatively high clinical application value and development prospect.

Description

technical field [0001] The invention relates to an application of a lactam compound in the preparation of drugs for inhibiting neuroinflammation. Background technique [0002] Neurodegenerative diseases (neurodegeneration disorders, ND) are a group of chronic progressive neurological diseases based on primary neuron degeneration, mainly including Alzheimer's disease (Alzheimer's disease, AD), Parkinson's disease (Parkinson's disease) , PD), multiple sclerosis (multiple sclerosis, MS), Huntington's disease (Huntington's disease, HD) and so on. With the aging of the world's population, the incidence of neurodegenerative diseases is on the rise. For example, the prevalence of AD in people over 60 years old in my country is 5.1%, and that in people over 85 years old is 30%. There are more than 8 million people, and there are about 35 million AD patients in the world. The prevalence of PD is second only to AD, and mainly occurs in people over middle age, with a prevalence rate o...

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): A61K31/4015A61P29/00A61P25/00A61P25/28
CPCA61K31/4015
Inventor 姚遥李娟王秀娟李玮琦
Owner NINGXIA MEDICAL 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