Epigenetic Modifiers Induce Host Defense Peptides

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Solution Overview

Problem

Current alternatives to antibiotics in animal feed, such as direct-fed microbials and botanical extracts, lack the cost-effectiveness, convenience, and performance of conventional antibiotics, and often induce unwanted inflammation and antimicrobial resistance.

Innovation Solution

The use of combinations of histone deacetylase inhibitors (HDACi) and DNA/histone methyltransferase inhibitors (DNMTi/HMTi) to synergistically induce the expression of antimicrobial host defense peptides (HDPs) in animals, thereby enhancing their innate immune response without triggering inflammation or inducing resistance.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibiotics are used in animal feed, then infection control is effective, but antimicrobial resistance develops and public health is compromised

Engineering Contradiction:

Improveinfection control effectivenessVSAvoidantimicrobial resistance

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent converts the harmful overuse of antibiotics into a beneficial alternative approach by using epigenetic modifiers (HDACi and DNMTi/HMTi) to stimulate the animal's own host defense peptide production. This transforms the problem of antibiotic resistance into a solution that leverages the immune system's natural defenses, thereby maintaining infection control effectiveness without contributing to antimicrobial resistance.

Inventive Principle:

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

Solution Approach 2:

The invention enables the animal's immune system to serve itself by upregulating endogenous host defense peptides through epigenetic modulation. Instead of relying on external antibiotics, the animal's cells are stimulated to produce their own antimicrobial peptides (such as defensins and cathelicidins), creating a self-sustaining immune response that does not contribute to resistance development.

Inventive Principle:

Principle #25Self-service

2Reliability

If immunomodulators are used to stimulate immune responses, then infection resistance is improved, but inflammation and adverse effects on animal growth occur

Engineering Contradiction:

Improveinfection resistanceVSAvoidinflammation and adverse growth effects

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent applies local quality by specifically targeting the upregulation of host defense peptides through epigenetic mechanisms rather than nonspecific immune stimulation. The HDACi and DNMTi/HMTi compounds act on specific gene expression pathways to enhance antimicrobial peptide production without triggering broad-spectrum inflammatory responses, thereby achieving infection resistance without the harmful side effects of general immunomodulation.

Inventive Principle:

Principle #3Local quality

3Object-affected harmful factors

If alternatives to antibiotics are explored, then antimicrobial resistance is reduced, but cost-effectiveness and performance are compromised

Engineering Contradiction:

Improveantimicrobial resistance reductionVSAvoidcost-effectiveness and animal performance

Core Design Contradiction:

Object-affected harmful factorsVSProductivity

Solution Approach 1:

The patent employs a composite approach by combining two different classes of epigenetic modifiers (HDACi and DNMTi/HMTi) that work synergistically to upregulate host defense peptides. This composite strategy enhances the effectiveness of the alternative treatment, potentially improving animal performance and making the approach more cost-effective compared to single-agent therapies, while still avoiding antibiotic resistance.

Inventive Principle:

Principle #40Composite materials

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 the occurrence of infections in animals by enhancing the expression of HDPs, thereby maintaining optimal animal health and performance while avoiding the drawbacks of conventional antibiotics.

Implementation Method 1

Acetylation of histones occurs through histone acetyltransferases (HAT) and deacetylation through histone deacetylases (HDAC). HDAC inhibitors (HDACi) are classified into hydroximates, cyclic peptides, aliphatic acids, and benzamides based on their structural differences

Methodology Applied

Scientific EffectHistone deacetylation:

Implementation Method 2

DNA is modified by methylation and demethylation. DNA is methylated by DNA methyltransferases (DNMT) and demethylated actively by various enzymes or passively during DNA replication

Methodology Applied

Scientific EffectDNA methylation:

Implementation Method 3

Histones are also methylated by a group of histone methyltransferases (HMT) and demethylated by histone demethylases

Methodology Applied

Scientific EffectHistone methylation:

Data Source

PatentUS20250144056A1Antimicrobial host defense peptide-inducing compositions and methods of production and use thereof

Publication Date: 2025.05.08 BOARD OF REGENTS FOR THE OKLAHOMA AGRI & MECHANICAL COLLEGE ACTING FOR & ON BEHALF OF OKLAHOMA STATE UNIV

AI summary

Compositions are disclosed that include a combination of at least one histone deacetylase inhibitor with at least one DNA or histone methyltransferase inhibitor. The combination of the histone deacetylase inhibitor with the methyltransferase inhibitor synergistically induces antimicrobial host defense peptide gene expression.