Non-covalent Dimer Cation Antioxidant for NAFLD

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Solution Overview

Problem

Current treatments for non-alcoholic fatty liver disease (NAFLD) are limited in effectively addressing oxidative stress and repairing damaged liver cells, with existing drugs either having limited efficacy or posing health risks due to their impact on essential fatty substances.

Innovation Solution

A non-covalent dimer cation, specifically a compound with a formula comprising a moiety with a non-covalent bond, is developed, which acts as an antioxidant, capable of scavenging reactive oxygen species and reducing oxidative stress in liver cells, potentially treating NAFLD by forming a stable salt with various anions.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If vitamin E is used to improve antioxidant capacity, then total antioxidant capacity and glutathione peroxidase activity are improved, but the effect is limited and safety of long-term administration cannot be ensured

Engineering Contradiction:
Improveantioxidant capacityVSAvoidlong-term safety
Core Design Contradiction:
ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent changes the chemical structure parameters by introducing a non-covalent dimer cation structure with specific functional groups (imidazole, pyridine, or triazole rings) and substituent patterns (R1-R7 groups). This structural modification transforms vitamin E from a monomer to a dimeric cation, fundamentally altering its antioxidant mechanism and pharmacokinetic properties to achieve both enhanced efficacy and improved safety profile for long-term use

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite molecular structure by combining two vitamin E moieties through a non-covalent bond to form a dimer cation. This composite structure integrates the antioxidant properties of individual vitamin E units while adding new functional characteristics through the cationic charge and non-covalent linkage, resulting in a molecule with superior and more stable antioxidant activity compared to monomeric vitamin E

Inventive Principle:
Principle #40Composite materials

2Object-affected harmful factors

If lipid-regulating drugs are used to block fat digestion and absorption, then fatty liver disease progression is delayed, but other health risks are introduced due to blocking essential fatty substances

Engineering Contradiction:
Improvefatty liver progressionVSAvoidhealth risks from blocking essential fats
Core Design Contradiction:
Object-affected harmful factorsVSObject-generated harmful factors

Solution Approach 1:

The patent converts the harmful effect of oxidative stress into a beneficial therapeutic mechanism. The non-covalent dimer cation specifically targets and neutralizes reactive oxygen species through its antioxidant activity, transforming the oxidative damage that drives fatty liver progression into a controlled therapeutic action that protects liver cells without interfering with normal fat metabolism or essential fatty acid utilization

Inventive Principle:
Principle #22Blessing in disguise (Convert harm into benefit)

3Duration of action of stationary object

If existing drugs are used to treat fatty liver disease, then disease progression is delayed, but damaged liver cells cannot be repaired

Engineering Contradiction:
Improvedisease progression delayVSAvoidliver cell repair capability
Core Design Contradiction:
Duration of action of stationary objectVSEase of repair

Solution Approach 1:

The patent enables liver cells to repair themselves by providing them with a potent antioxidant agent that directly neutralizes reactive oxygen species within the cells. The non-covalent dimer cation acts as a self-service therapeutic that empowers liver cells to counteract oxidative damage independently, restoring their natural repair capabilities rather than merely slowing disease progression through external intervention

Inventive Principle:
Principle #25Self-service

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 non-covalent dimer cation effectively reduces oxidative stress and improves cell viability in NAFLD models, demonstrating potential as a safer and more effective treatment option compared to existing therapies.

Implementation Method 1

the non-covalent dimer cation effectively reduces oxidative stress and improves cell viability in NAFLD models, demonstrating potential as a safer and more effective treatment option compared to existing therapies

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Data Source

PatentUS20240140935A1Non-covalent dimer cation, salt thereof, preparation method thereof, and use thereof as antioxidant
Publication Date: 2024.05.02 SUZHOU PROTONATION CHAIN BIOTECHNOLOGY CO LTD
  • US20240140935A1 patent drawing
  • US20240140935A1 patent drawing
  • US20240140935A1 patent drawing

AI summary

Herein provides a non-covalent dimer cation of formula (A), a tautomer thereof, or a stereoisomer thereof. Herein provides a salt, which includes the cation of the present application and a first anion. Herein provides use of the cation of the present application or the salt of the present application in antioxidation, preparation of an antioxidant, preparation of a drug for inhibiting, reducing or reversing oxidative stress in human or animal cells, or preparation of a drug for treating an oxidative stress-associated disease or symptom, such as, use in preparation of a drug for treating non-alcoholic fatty liver disease.