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

Anti-acetylcholinesterase active composition in Chinese mahonia stem, and screening method and application of anti-acetylcholinesterase active composition

A technology of acetylcholinesterase and composition, which is applied in the field of medicine and can solve problems such as complicated operation, low degree of automation, and long cycle

Active Publication Date: 2019-10-29
SHENZHEN INST FOR DRUG CONTROL SHENZHEN TESTING CENT OF MEDICAL DEVICES
View PDF3 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether the medicinal effects of genuine gongluomu and gongluomu substitutes are the same, there is no definite conclusion
[0005] Preliminary studies have shown that the extract of Gongluomu has a good activity of inhibiting acetylcholinesterase (AChE), but the specific types of active substances need to be further studied
Due to the complex and diverse components of Gongluomu extract, it greatly increases the difficulty of screening and research of active substances
At present, the methods for studying the active substances of traditional Chinese medicine mainly include tracking separation method, ultrafiltration method and magnetic microsphere fishing method. Although these methods can effectively find active ingredients, they have defects such as long cycle, high cost, complicated operation, and low degree of automation.

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
  • Anti-acetylcholinesterase active composition in Chinese mahonia stem, and screening method and application of anti-acetylcholinesterase active composition
  • Anti-acetylcholinesterase active composition in Chinese mahonia stem, and screening method and application of anti-acetylcholinesterase active composition
  • Anti-acetylcholinesterase active composition in Chinese mahonia stem, and screening method and application of anti-acetylcholinesterase active composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] The preparation of embodiment 1 acetylcholinesterase reactor

[0065] (1) Capillary pretreatment

[0066] Take a quartz capillary with a length of about 2 m and an inner diameter of 400 μm, wash it with NaOH (1moL / L) solution for 20 min; seal both ends of the capillary filled with NaOH with rubber stoppers, and react in a water bath at 100°C for 2 h; take out the capillary, Rinse the capillary with distilled water until the effluent is neutral (pH test paper test), rinse the capillary with MeOH for 30 min; dry with nitrogen for 2 h, then perfuse the mixture of γ-MAPS / MeOH (50 / 50, v / v) until it is dry The capillary was sealed with a rubber stopper and placed in a water bath at 60°C for 12 h; the capillary was rinsed with methanol and distilled water for 30 min each, and finally the capillary was fully dried with nitrogen.

[0067] As shown in Figure 1(A), by activating the inner wall of the quartz capillary, alkenyl groups are modified on the inner wall of the capillary...

Embodiment 2

[0077] The characterization of embodiment 2 acetylcholinesterase reactor

[0078] (1) Infrared spectrum characterization

[0079] The AChE, poly(GMA-co-EDMA) monolithic matrix material without immobilized enzyme and the AChE reactor AChE-ICER were characterized by infrared spectrometer.

[0080] Such as figure 2 As shown, 1725cm -1 Stretching vibration absorption for poly(GMA-co-EDAM) integral matrix C=O, 1544cm -1 For the bending vibration of the N-H bond of the peptide bond, 1666cm -1 For the C=O stretching vibration absorption in the peptide bond, FT-IR results show that AChE has been successfully modified on the poly(GMA-co-EDAM) monolithic matrix carrier.

[0081] (2) SEM characterization

[0082] In this example, an Ultra-55 field emission scanning electron microscope was used to visually characterize the morphology and structure of the poly(GMA-co-EDMA) monolithic matrix material and the cross-section of the AChE reactor AChE-ICER.

[0083] As shown in Figure 3(A)...

Embodiment 3

[0085] Example 3 Ligand Fishing Method

[0086] (1) Preparation of extract

[0087] Accurately weigh 2.0g of gonglao wood powder, place it in a stoppered conical flask, add 50mL of hydrochloric acid-methanol (1:100, v / v) mixed solution, seal the weight and then cold soak for 30min, ultrasonic treatment (power 300W, frequency 40kHz) 60min, vacuum rotary steaming until dry extract is obtained;

[0088] Accurately weigh 15 mg of Gonglao Mugan extract, place it in a 5 mL volumetric flask, add ammonium acetate buffer (10 mM, pH=7.4) to dissolve to the scale, and make the concentration 3 mg / mL, and carry out ligand fishing analysis;

[0089] (2) Elution method of functional AChE-ICER monolithic column:

[0090] The first step: use the mobile phase ammonium acetate buffer (10mM, pH=7.4) to provide it through a peristaltic pump, the flow rate is 5 μL / min, the sample injection volume is 100 μL, and last for 40 minutes to collect fractions;

[0091] Step 2: Change the mobile phase fr...

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
The inside diameter ofaaaaaaaaaa
Login to View More

Abstract

The invention provides an anti-acetylcholinesterase active composition in Chinese mahonia stem, and a screening method and application of the anti-acetylcholinesterase active composition. The composition is prepared from columbamine, jateorhizine, palmatine and berberine. According to the anti-acetylcholinesterase active composition, the traditional Chinese medicine Chinese mahonia stem is taken as a study object, based on an affinity chromatography principle, an immobilized enzyme technology is combined, an acetylcholinesterase reactor is prepared, an active compound fishing platform is constructed, four active components for anti-acetylcholinesterase are successfully screened and identified, an effective screening method for discovery of extracting anti-acetylcholinesterase active substances from the Chinese mahonia stem, when the compounds columbamine and jateorhizine are fixed, other compounds are correspondingly added to be mixed with the columbamine and the jateorhizine, when theconcentration of the columbamine or the jateorhizine is below IC60 or IC70, the obvious synthesis or summation effect occurs, according to the research, the compound components developing the anti-AChE activity in the Chinese mahonia stem extraction are discovered and identified for the first time, the combination with synthesis or summation is obtained, and the combination can be assuredly developed to a potential anti-AChE inhibitor.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a composition with anti-acetylcholinesterase activity in gonglaomu and its screening method and application. Background technique [0002] Alzheimer's disease (AD) is a primary degenerative brain disease of unknown etiology, which has brought a huge burden to society and families and has become a global health problem. Acetylcholinesterase inhibitors, as the only AD drug approved by the US FDA, have a certain therapeutic effect, but the action time is short and often accompanied by side effects. In recent years, traditional Chinese medicine has shown good prospects in the prevention and treatment of AD. It has many potential advantages such as low toxicity and side effects, and overall effect. treatment is particularly important. [0003] Gonggongmu is recorded as its name, and its source is the dried stems of Mahonia bealei (Fort.) Carr. and Mahoniafortunei (Lindl.) Fedde., whi...

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): A61K31/4375A61P25/28G01N30/02
CPCA61K31/4375A61P25/28G01N30/02A61K2300/00G01N2030/8813A61K36/29A61K31/4704A61K31/4745C12Q1/46C12Y301/01007G01N33/6896G01N2800/2821G01N2560/00G01N33/573
Inventor 王铁杰王珏殷果江坤江正瑾
Owner SHENZHEN INST FOR DRUG CONTROL SHENZHEN TESTING CENT OF MEDICAL DEVICES
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