Phe-Pro Peptide Oral Brain Function Enhancement

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Solution Overview

Problem

Current therapeutic drugs for Alzheimer's disease and other brain function deterioration symptoms, such as acetylcholinesterase inhibitors and peptides, face issues like hepatotoxicity, strong side effects, high costs, and require large doses for efficacy, while existing peptides' actions in improving brain function are unknown.

Innovation Solution

A composition comprising Phe-Pro or its salt, administered orally, which improves brain function by potentially increasing acetylcholine release, demonstrated through behavioral pharmacological tests, offering a prophylactic and curative effect against brain dysfunction.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If acetylcholinesterase inhibitors are administered to improve brain function, then the concentration of acetylcholine increases, but hepatotoxicity and strong side effects occur

Engineering Contradiction:
Improveconcentration of acetylcholineVSAvoidhepatotoxicity and side effects
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses Phe-Pro peptide as an intermediary substance that indirectly increases acetylcholine concentration through a different mechanism than acetylcholinesterase inhibitors. Instead of blocking acetylcholinesterase directly, Phe-Pro activates C3a receptors on cholinergic neurons, which triggers intracellular signaling cascades that enhance acetylcholine release. This intermediary approach achieves the desired increase in acetylcholine while avoiding the direct toxic effects of acetylcholinesterase inhibitors on the liver and other organs.

Inventive Principle:
Principle #24Intermediary (Mediator)

2Quantity of substance

If peptides are administered in large doses to demonstrate anti-amnesic effect, then the effect against scopolamine-induced amnesia is achieved, but oral ingestibility and sufficient effect level are compromised

Engineering Contradiction:
Improvedose of peptideVSAvoidoral ingestibility and sufficient effect
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent changes the key parameter of peptide structure from random sequences or longer peptides to the specific dipeptide Phe-Pro (amino acid sequence: phenylalanine-proline). This structural parameter change dramatically improves oral bioavailability and reduces the required dose. The patent demonstrates that Phe-Pro at 30 mg/kg body weight (a very low dose) administered orally produces significant protective effects against scopolamine-induced amnesia, making it both orally ingestible and sufficiently effective.

Inventive Principle:
Principle #35Parameter changes

3Reliability

If existing peptides are used for brain function improvement, then some anti-amnesic effect is observed, but the actions involved in improvement are unknown

Engineering Contradiction:
Improveanti-amnesic effectVSAvoidunknown mechanism of action
Core Design Contradiction:
ReliabilityVSLoss of information

Solution Approach 1:

The patent establishes a feedback mechanism by investigating and elucidating the mechanism of action of Phe-Pro. Through behavioral pharmacological tests and molecular biological studies, the patent identifies that Phe-Pro activates C3a receptors on cholinergic neurons, which triggers intracellular signaling pathways that enhance acetylcholine release. This feedback loop of investigation and understanding transforms the unknown mechanism into known, verifiable biological processes, allowing for rational optimization of the treatment approach.

Inventive Principle:
Principle #23Feedback

4Reliability

If therapeutic drugs are administered to treat brain function deterioration, then symptoms are addressed, but high costs are incurred

Engineering Contradiction:
Improvetreatment effectivenessVSAvoidcost of treatment
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent employs a cheap, simple dipeptide Phe-Pro that can be easily synthesized and administered. Unlike expensive acetylcholinesterase inhibitors requiring complex chemical structures and synthesis procedures, Phe-Pro consists of only two common amino acids that can be produced cost-effectively. The patent demonstrates that this inexpensive peptide provides significant protective effects against brain function deterioration, making treatment more accessible and affordable while maintaining therapeutic effectiveness.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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

Phe-Pro or its salt effectively prevents amnesia and strengthens memory, as shown in Y-shaped maze tests, with potential applications in treating depression, schizophrenia, and dementia, providing a safer and more cost-effective option for improving brain function.

Implementation Method 1

a release of acetylcholine from the intracerebral C3a receptor has been suggested as one of the mechanisms involved in this effect

Methodology Applied
Scientific EffectAcetylcholine release:

Data Source

PatentEP2617432B1Brain function enhancement composition and method for enhancing brain function
Publication Date: 2015.09.02 CALPIS
  • EP2617432B1 patent drawingFigure 1
  • EP2617432B1 patent drawing

AI summary

The present invention provides a composition which may be ingested orally in a small dose for the purpose of improving brain function, and a method for improving brain function. The present invention is a composition for improving brain function, comprising, as an active ingredient, Phe-Pro.