Leu-Arg-Ala Tripeptide ACE Inhibition for Hypertension
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Solution Overview
Problem
There is a growing need for safe and effective ACE-inhibitory substances to manage hypertension, as the number of patients with elevated blood pressure increases, and existing research has not fully identified novel peptides with strong ACE inhibitory activity.
Innovation Solution
A tripeptide consisting of Leu-Arg-Ala is developed, which exhibits excellent ACE inhibitory activity and is used in compositions for lowering blood pressure, either as a pharmaceutical or food ingredient, administered orally in specific doses and durations to achieve a blood pressure-lowering effect.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional peptides from digestion products are used, then ACE inhibitory activity is achieved, but novelty and effectiveness are limited
Solution Approach 1:
The patent applies parameter changes by modifying the amino acid sequence parameters to create a novel tripeptide (Leu-Arg-Ala) with optimized ACE inhibitory activity. This involves changing the specific sequence parameters from conventional peptides to achieve both novelty and enhanced effectiveness, resolving the contradiction between reliability and adaptability.
2Reliability
If ACE-inhibitory substances are developed, then blood pressure control is improved, but safety and effectiveness requirements create development challenges
Solution Approach 1:
The patent applies segmentation by dividing the complex requirement for effective and safe ACE-inhibitory substances into a simple tripeptide structure (Leu-Arg-Ala). This segmented approach breaks down the development complexity while maintaining blood pressure control effectiveness, making the substance easier to manufacture and validate.
Solution Approach 2:
The patent employs the principle of using a simple, short-sequence peptide (tripeptide) instead of complex long-chain peptides or proteins. This Leu-Arg-Ala tripeptide is easier to manufacture, more stable, and provides sufficient ACE inhibitory activity for blood pressure control, reducing development complexity while maintaining reliability.
3Reliability
If existing peptides are used, then ACE inhibition is achieved, but the number of effective novel peptides remains insufficient
Solution Approach 1:
The patent systematically changes the amino acid sequence parameters to generate novel tripeptide variants with ACE inhibitory activity. By modifying sequence parameters while maintaining the core inhibitory mechanism, the patent expands the quantity of effective novel peptides available, resolving the contradiction between reliability and quantity.
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 tripeptide effectively inhibits ACE and lowers blood pressure, demonstrated through significant reductions in systolic blood pressure in animal models and human clinical trials, providing a safe and effective option for managing hypertension.
Implementation Method 1
Angiotensin-converting enzyme (angiotensin I-converting enzyme; also referred to as 'ACE' in the present specification) is an enzyme that converts angiotensin I into angiotensin II... when the action of ACE is inhibited, the production of angiotensin II is suppressed
Implementation Method 2
Angiotensin II has the action of increasing blood pressure by, for example, contracting blood vessels
Data Source
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Figure 3
AI summary
Provided is a novel peptide having ACE inhibitory activity. Specifically, provided is a tripeptide consisting of Leu-Arg-Ala.