Pterosin Compounds Inhibiting BACE1 and AChE Enzymes

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Solution Overview

Problem

Current therapeutic agents for degenerative brain diseases like Alzheimer's are limited in their ability to effectively inhibit key enzymes such as BACE1, AChE, and BChE, leading to inadequate treatment outcomes, and there is a need for more potent therapeutic agents to address the growing prevalence of these diseases.

Innovation Solution

A pharmaceutical and food composition containing pterosin compounds or their derivatives, extracted and purified from bracken ferns using a method involving soaking in water or organic solvents, followed by fractionation with ethyl acetate and concentration-gradient chromatography, which inhibit the activities of BACE1, AChE, and BChE.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If current therapeutic agents are used to treat degenerative brain diseases, then treatment is provided, but the ability to effectively inhibit key enzymes (BACE1, AChE, BChE) is limited, leading to inadequate treatment outcomes

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidinsufficient enzyme inhibition
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and isolates pterosin compounds specifically from bracken fern (Pteridium aquilinum) to obtain a concentrated source of enzyme-inhibiting substances. This extraction process separates the active compounds from the plant matrix, creating a purified therapeutic agent that can effectively inhibit BACE1, AChE, and BChE enzymes responsible for degenerative brain diseases.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent develops a composite pharmaceutical composition that combines pterosin compounds with other beneficial plant extracts and pharmaceutical excipients. This composite formulation enhances the overall therapeutic effect by combining multiple active components that work synergistically to inhibit target enzymes and provide comprehensive treatment for degenerative brain diseases.

Inventive Principle:
Principle #40Composite materials

2Reliability

If pterosin compounds are extracted and purified from bracken ferns using multiple processing steps, then potent inhibitory effects on enzymes are achieved, but the manufacturing process becomes complex

Engineering Contradiction:
Improveenzyme inhibition potencyVSAvoidmanufacturing process complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

The patent divides the manufacturing process into distinct sequential stages: extraction of pterosin compounds from bracken fern, fractionation to separate different compound classes, and purification to isolate active ingredients. This segmentation allows each step to be optimized independently and facilitates quality control while maintaining high enzyme inhibition potency.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs parameter changes during the purification process, including adjusting solvent polarity, temperature, and pH conditions to selectively isolate pterosin compounds from other plant constituents. These parameter modifications enable efficient separation and purification while managing the complexity of the manufacturing process.

Inventive Principle:
Principle #35Parameter changes

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The pterosin compounds demonstrate potent inhibitory effects on BACE1, AChE, and BChE, offering a promising therapeutic approach for treating degenerative brain diseases and enhancing cognitive function, with potential for both pharmaceutical and dietary applications.

Implementation Method 1

the pterosin compounds demonstrate potent inhibitory effects on BACE1, AChE, and BChE

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Implementation Method 2

extracted and purified from bracken ferns using a method involving soaking in water or organic solvents

Methodology Applied
Scientific EffectExtraction:

Implementation Method 3

concentration-gradient chromatography

Methodology Applied
Scientific EffectChromatography: Chromatography

Data Source

PatentEP3639817B1Compositions containing pterosin compound and derivatives thereof active ingredients for prevention or treatment of degenerative brain diseases
Publication Date: 2024.10.09 KORPHARM CO LTD
  • EP3639817B1 patent drawingFigure 1
  • EP3639817B1 patent drawingFigure 2
  • EP3639817B1 patent drawingFigure 3

AI summary

The present invention relates to compositions containing a pterosin compound and derivatives thereof as active ingredients for the prevention or treatment of degenerative brain diseases and, more specifically, to a pharmaceutical composition for the prevention or treatment of degenerative brain diseases and a food composition for the prevention or alleviation of degenerative brain diseases, each of which contains a pterosin compound defined by chemical formula 1 or a derivative thereof as an active ingredient. A method of the present invention can be favorably used to provide a therapeutic agent for preventing or treating degenerative brain diseases, a food for alleviating degenerative brain diseases, or a functional food for the promotion of cognitive functions, by using a pterosin compound extracted from Pteridium aquilinum and derivatives thereof.