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
Engineering 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
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.
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
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.
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
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.
4Reliability
If therapeutic drugs are administered to treat brain function deterioration, then symptoms are addressed, but high costs are incurred
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.
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
Data Source
Figure 1
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.