Nitroxyl Polyphenol Derivatives for Low-Dose Antiaging Antioxidants

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Solution Overview

Problem

Current polyphenol compounds used for antiaging have limited bioavailability and require high concentrations for effective action, and there is a lack of information on the antioxidant/antiaging activity of existing derivatives.

Innovation Solution

Development of nitroxyl polyphenol derivatives through specific ester linking groups and nitroxyl radicals, synthesized using controlled reactions in organic solvents, to enhance bioavailability and antioxidant properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If polyphenol compounds are used for antiaging, then antioxidant activity is achieved, but bioavailability is limited and high concentrations are required

Engineering Contradiction:
Improveantioxidant activityVSAvoidconcentration required
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The patent modifies the chemical structure of polyphenols by introducing nitroxyl radicals and ester linking groups, changing molecular parameters to enhance bioavailability and reduce the concentration required for effective antiaging action

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention creates composite molecular structures combining polyphenols with nitroxyl radicals and ester groups, resulting in derivatives that exhibit improved pharmacokinetic properties and lower effective concentrations

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If polyphenol derivatives are synthesized, then bioavailability is improved, but manufacturing complexity increases

Engineering Contradiction:
ImprovebioavailabilityVSAvoidsynthesis process complexity
Core Design Contradiction:
Quantity of substanceVSDevice complexity

Solution Approach 1:

The synthesis process is divided into discrete steps: introducing nitroxyl radicals, forming ester linking groups, and modifying specific polyphenol positions, allowing controlled complexity management

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent employs intermediate compounds and reagents (such as carbodiimide activators and heterocyclic compounds) to facilitate the synthesis of nitroxyl polyphenol derivatives, simplifying the overall manufacturing process

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

The nitroxyl polyphenol derivatives exhibit improved antioxidant activity, delaying cellular aging by reducing oxidative stress and showing bioactive effects on various molecular targets, with modified properties based on parent molecule and hydroxy group presence.

Implementation Method 1

The nitroxyl polyphenol derivatives exhibit improved antioxidant activity, delaying cellular aging by reducing oxidative stress

Methodology Applied
Scientific EffectAntioxidant activity: Oxidation

Data Source

PatentUS20260008751A1Nitroxyl polyphenol derivative, methods for the preparation thereof and use thereof
Publication Date: 2026.01.08 UNIWERSYTET WARSZAWSKI
  • US20260008751A1 patent drawing
  • US20260008751A1 patent drawing
  • US20260008751A1 patent drawing

AI summary

The object of the invention is a nitroxyl polyphenol derivative of formula:wherein Q is a group derived from a polyphenol;L is an ester linking group containing 1 to 3 carbon atoms;A is a 5- or 6-membered heterocyclic group containing one nitrogen atom which is in the form of nitroxyl radical (NO·), in which both carbon atoms adjacent to the nitroxyl radical are substituted independently of each other with one or two C1-C3 alkyl groups; andn is an integer of 1 to 5.The object of the invention is also methods for the preparation of the above-defined derivative and a use thereof as an antioxidant agent, in particular an antiaging agent.