L-Arginine BH4 Ascorbic Acid Composition Redox Balance

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Solution Overview

Problem

Current methods for managing oxidative stress are inadequate, as they often fail to effectively balance the redox state in cells and tissues, leading to limited success or even detrimental effects in reducing oxidative stress-related diseases.

Innovation Solution

A composition comprising L-Arginine, tetrahydrobiopterin (BH4), and ascorbic acid, administered in specific balanced ratios, is used to balance the redox state by providing a substrate for nitric oxide synthase, maintaining the enzyme in a coupled state, and acting as an antioxidant to reduce oxidative stress in cells and tissues.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If single-therapy approaches are used to reduce oxidative stress, then the treatment simplicity is maintained, but the effectiveness in balancing redox state is insufficient and may even have detrimental effects

Engineering Contradiction:
Improvetreatment simplicityVSAvoideffectiveness in balancing redox state
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent combines multiple agents (L-Arginine, BH4, and ascorbic acid) into a single composition that works synergistically to balance redox state. L-Arginine provides substrate for nitric oxide synthase, BH4 maintains the enzyme in a coupled state, and ascorbic acid acts as an antioxidant, together achieving effective oxidative stress reduction that single agents cannot accomplish alone.

Inventive Principle:
Principle #5Merging (Combining)

2Reliability

If multiple agents are combined to balance redox state, then the effectiveness in reducing oxidative stress is improved, but the composition complexity increases

Engineering Contradiction:
Improveeffectiveness in reducing oxidative stressVSAvoidcomposition complexity
Core Design Contradiction:
ReliabilityVSDevice complexity

Solution Approach 1:

Each agent in the composition serves multiple functions: L-Arginine serves as both substrate for nitric oxide production and precursor for polyamine synthesis; BH4 functions as both electron donor for nitric oxide synthase and antioxidant; ascorbic acid provides both direct antioxidant activity and regenerates other antioxidants. This multi-functionality reduces the need for additional separate agents.

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Reliability

If specific balanced ratios of agents are used, then the redox balancing effectiveness is optimized, but the manufacturing precision requirements increase

Engineering Contradiction:
Improveredox balancing effectivenessVSAvoidratio control precision
Core Design Contradiction:
ReliabilityVSManufacturing precision

Solution Approach 1:

The patent specifies optimal weight ratios (L-Arginine:BH4 = 2.5-50:1, BH4:ascorbic acid = 1:5-100) that maximize the synergistic effect of the agents. These parameter ranges provide flexibility in manufacturing while ensuring therapeutic effectiveness, allowing for practical formulation adjustments without compromising the redox balancing function.

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

This approach effectively reduces oxidative stress, promotes healthy function and differentiation of stem and progenitor cells, and improves clinical outcomes by normalizing the redox state, thereby addressing the limitations of single-therapy approaches.

Implementation Method 1

providing a substrate for nitric oxide synthase

Methodology Applied
Scientific EffectEnzyme catalysis: Enzyme

Implementation Method 2

maintaining the enzyme in a coupled state

Methodology Applied
Scientific EffectRedox reactions: Redox Reactions

Implementation Method 3

acting as an antioxidant to reduce oxidative stress

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Data Source

PatentEP2456432B1Compositions to reduce oxidative stress
Publication Date: 2024.02.28 UNIV OF MASSACHUSETTS
  • EP2456432B1 patent drawingFigure 1
  • EP2456432B1 patent drawingFigure 2A~2C
  • EP2456432B1 patent drawingFigure 3A~4B

AI summary

The invention relates to therapeutic applications for compositions that reduce the level of oxidative stress on cells in vivo or in vitro. The invention describes methods for improving the therapeutic properties of stem cells. The invention also provides combination therapies that are useful to balance the oxidative microenvironment of cells in vivo or in vitro.