Sirtuin Activator Composition for Metabolic Pathway Modulation

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Solution Overview

Problem

Current treatments for metabolic disorders, such as obesity and diabetes, are limited in effectiveness due to issues like low bioavailability of SIRT1 activators like resveratrol, which require high dosages and pose safety concerns, and fail to safely regulate metabolic pathways effectively.

Innovation Solution

A composition combining synergistic amounts of a sirtuin pathway activator, such as resveratrol, with branched chain amino acids like leucine and their metabolites, which synergistically activate SIRT1 and SIRT3, enhancing mitochondrial biogenesis, fatty acid oxidation, and insulin sensitivity, thereby addressing metabolic disorders.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Quantity of substance

If high dosages of SIRT1 activators like resveratrol are used to overcome low bioavailability, then the activator can reach effective concentrations, but safety concerns increase

Engineering Contradiction:
Improvedosage of SIRT1 activatorVSAvoidsafety concerns
Core Design Contradiction:
Quantity of substanceVSObject-affected harmful factors

Solution Approach 1:

The patent uses amino acid metabolites (beta-hydroxy-beta-methylbutyrate from leucine metabolism) as intermediary compounds that enhance the activity and efficacy of SIRT1 activators. This mediation allows lower dosages of resveratrol to achieve therapeutic effects, thereby reducing safety concerns associated with high dosages while maintaining bioavailability

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention combines SIRT1 activators (like resveratrol) with amino acid metabolites (HMB, KIC, leucine) to create a composite therapeutic composition. This composite approach synergistically enhances the metabolic effects, allowing reduced dosages of the SIRT1 activator while achieving the desired therapeutic outcome, thus resolving the contradiction between dosage and safety

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional treatments target specific energy metabolism pathways, then they attempt to address metabolic disorders, but they fail to safely regulate metabolic pathways effectively

Engineering Contradiction:
Improveeffectiveness of metabolic pathway regulationVSAvoidsafety issues
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent merges the action of SIRT1 activators with amino acid metabolites that activate related metabolic pathways (including AMPK and PGC-1α). This combined approach creates a synergistic effect that more effectively and safely regulates multiple metabolic pathways simultaneously, addressing the limitation of conventional single-pathway treatments

Inventive Principle:
Principle #5Merging (Combining)

3Productivity

If high dosages of resveratrol are administered to achieve therapeutic effects, then metabolic pathway activation is enhanced, but the treatment becomes less safe

Engineering Contradiction:
Improvesirtuin pathway outputVSAvoidsafety concerns
Core Design Contradiction:
ProductivityVSObject-affected harmful factors

Solution Approach 1:

Amino acid metabolites serve as intermediaries that amplify the signaling through the sirtuin pathway. By using these intermediary compounds, the patent achieves high sirtuin pathway output with lower dosages of resveratrol, thereby maintaining productivity while reducing the harmful effects associated with high dosages

Inventive Principle:
Principle #24Intermediary (Mediator)

Data Source

PatentUS10383837B2Compositions and methods for modulating metabolic pathways
Publication Date: 2019.08.20 NUSIRT SCIENCES INC
  • US10383837B2 patent drawing
  • US10383837B2 patent drawing
  • US10383837B2 patent drawing

AI summary

Compositions and methods useful for inducing an increase in fatty acid oxidation or mitochondrial biogenesis, reducing weight gain, inducing weight loss, or increasing Sirt1, Sirt3, or AMPK activity are provided herein. Such compositions can contain synergizing amounts of a sirtuin-pathway activators, including but not limited to resveratrol, in combination with beta-hydroxymethylbutyrate (HMB), keto isocaproic acid (KIC), leucine, or combinations of HMB, KIC and leucine.