Polyhydroxy Fullerenes Catalyze Endogenous H2S Production

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Solution Overview

Problem

Current methods for boosting endogenous hydrogen sulfide (H2S) levels for therapeutic benefits are challenging due to acute toxicity risks and poor translatability from rodent models to humans, especially in conditions with impaired enzymatic activity or genetic mutations affecting H2S production enzymes.

Innovation Solution

Administration of polyhydroxy fullerenes (PHFs) that catalytically generate H2S from sulfur-containing amino acids, enhancing endogenous production and reducing symptoms associated with inflammation and low H2S levels, with PHFs being used in various formulations such as food products and delivery systems.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If exogenous H2S supplementation is used to treat diseases, then H2S levels are increased, but acute toxicity occurs due to high reactivity

Engineering Contradiction:
ImproveH2S levelsVSAvoidacute toxicity
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses carbon-based nanomaterials as intermediaries that catalyze the conversion of sulfur-containing amino acids to H2S in vivo. This mediator approach allows controlled endogenous production of H2S rather than direct administration, reducing acute toxicity while maintaining therapeutic H2S levels. The nanomaterial catalyst enables the body to produce its own H2S from dietary amino acids.

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention enables the body to serve itself by producing H2S endogenously through catalysis of sulfur-containing amino acids by carbon-based nanomaterials. Instead of relying on external H2S supplementation, the system uses the body's own amino acid metabolism to generate H2S where and when it is needed, reducing toxicity while maintaining therapeutic efficacy.

Inventive Principle:
Principle #25Self-service

2Quantity of substance

If dietary restriction or hormone lowering is used to boost endogenous H2S production, then H2S levels increase, but patient compliance and safety issues prevent widespread implementation

Engineering Contradiction:
Improveendogenous H2S productionVSAvoidpatient compliance
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent employs carbon-based nanomaterials that act as reusable catalysts to convert inexpensive sulfur-containing amino acids (from normal diet) into therapeutic H2S. This approach replaces complex lifestyle interventions with a simple supplement containing the catalyst and amino acids, dramatically improving ease of operation and patient compliance while maintaining effective H2S production.

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

3Quantity of substance

If dietary restriction or hormone lowering is used to boost endogenous H2S production, then H2S levels increase, but translatability from rodent models to humans is poor

Engineering Contradiction:
Improveendogenous H2S productionVSAvoidtranslatability
Core Design Contradiction:
Quantity of substanceVSAdaptability or versatility

Solution Approach 1:

The carbon-based nanomaterial catalyst serves as a universal intermediary that works across species barriers. Unlike physiological interventions (dietary restriction, hormone manipulation) that have different effects in rodents versus humans, the catalytic conversion of amino acids to H2S by carbon nanomaterials represents a fundamental chemical process that is conserved across species, improving translatability from preclinical to clinical settings.

Inventive Principle:
Principle #24Intermediary (Mediator)

4Quantity of substance

If H2S is administered to treat conditions with impaired enzymatic activity, then H2S levels increase, but mutations or epigenetic gene-silencing negate the therapeutic effect

Engineering Contradiction:
ImproveH2S levelsVSAvoidtherapeutic effect
Core Design Contradiction:
Quantity of substanceVSReliability

Solution Approach 1:

The carbon-based nanomaterial acts as an artificial enzyme or catalyst that bypasses defective endogenous H2S-producing enzymes. By providing an alternative catalytic pathway that does not depend on CBS or CGL enzyme activity, the system reliably produces H2S even in patients with genetic mutations or epigenetic silencing of these enzymes, ensuring consistent therapeutic effect across diverse patient populations.

Inventive Principle:
Principle #24Intermediary (Mediator)

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

PHFs effectively catalyze H2S production in human liver cells and in vivo, demonstrating potential therapeutic benefits for conditions like cardiovascular and metabolic disorders, with sustained activity and reduced toxicity, improving symptoms and survival rates in animal models.

Implementation Method 1

PHFs effectively catalyze H2S production in human liver cells and in vivo

Methodology Applied
Scientific EffectCatalysis: Catalysis

Data Source

PatentUS20240139121A1Fullerenes to treat diseases and conditions
Publication Date: 2024.05.02 THE CLEVELAND CLINIC FOUND
  • US20240139121A1 patent drawing
  • US20240139121A1 patent drawing
  • US20240139121A1 patent drawing

AI summary

Provided herein are compositions, systems, kits, and methods for treating a subject with a disease or condition by administering a composition comprising fullerenes to the subject such that H2S is generated in said subject. In certain embodiments, the disease or condition is associated with inflammation and/or below normal H2S levels. In certain embodiments, the fullerenes are polyhydroxy fullerenes (PHFs).