Tryptophol and 4-Ethyl-Phenol Derivatives for Quorum Sensing Inhibition

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Solution Overview

Problem

There is a pressing need for novel antibacterial agents that can effectively target bacterial communication pathways, particularly quorum sensing, to combat antibiotic resistance and modulate bacterial virulence, with a focus on reducing biofilm production and addressing inflammatory and amyloid-related diseases.

Innovation Solution

A composition comprising derivatives of Tryptophol and 4-Ethyl-Phenol, along with a microorganism mixture including Kluyveromyces marxianus and probiotic microorganisms, is used to inhibit biofilm production and treat inflammatory and amyloid-related diseases by disrupting quorum sensing pathways.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibiotics are used to treat bacterial infections, then bacterial growth is inhibited, but bacterial resistance develops

Engineering Contradiction:

Improveeffectiveness of antibacterial treatmentVSAvoidbacterial resistance

Core Design Contradiction:

ReliabilityVSAdaptability or versatility

Solution Approach 1:

The patent employs quorum sensing inhibitors (QSIs) as intermediary molecules that disrupt bacterial communication pathways rather than directly killing bacteria. These QSIs act as mediators that interfere with the production or detection of autoinducers, preventing bacteria from coordinating virulence and biofilm formation without exerting direct selective pressure for resistance development

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention replaces the mechanical/chemical direct killing mechanism of conventional antibiotics with a signaling interference mechanism. Instead of using antibiotics that directly target bacterial cell processes (mechanical disruption of cell walls, protein synthesis inhibition), the patent uses molecules that substitute the natural quorum sensing signaling pathway with inhibitory signals, fundamentally changing the mode of action from direct attack to communication disruption

Inventive Principle:

Principle #28Mechanics substitution (Replace mechanical system)

2Object-affected harmful factors

If quorum sensing pathways are targeted to reduce biofilm production, then bacterial virulence is modulated, but novel antibacterial agents are required

Engineering Contradiction:

Improvebiofilm productionVSAvoidavailability of novel agents

Core Design Contradiction:

Object-affected harmful factorsVSEase of manufacture

Solution Approach 1:

The patent utilizes parameter changes in molecular structure and concentration to achieve quorum sensing inhibition. By modifying the chemical parameters of autoinducer molecules (such as changing the acyl chain length, adding functional groups, or altering the core structure), the invention creates a series of QSIs with different potencies and specificities, allowing for optimized therapeutic agents that can be manufactured using established organic synthesis methods

Inventive Principle:

Principle #35Parameter changes

3Stability of the object's composition

If autoinducers are used for population modulation, then bacterial communication is regulated, but substances that interfere with quorum sensing must be identified

Engineering Contradiction:

Improvebacterial population modulationVSAvoididentification of interfering substances

Core Design Contradiction:

Stability of the object's compositionVSDifficulty of detecting and measuring

Solution Approach 1:

The patent employs feedback mechanisms through reporter gene systems and bioassays to identify and characterize quorum sensing interfering substances. By incorporating reporter genes that respond to quorum sensing activation (such as luciferase or fluorescent proteins), the invention creates a feedback loop that allows high-throughput screening of compound libraries, making the detection and measurement of QSIs systematic and efficient rather than relying on random identification

Inventive Principle:

Principle #23Feedback

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 solution effectively reduces biofilm formation, modulates inflammatory responses, and addresses amyloid aggregation, providing a potential alternative to conventional antibiotics by targeting bacterial communication mechanisms.

Implementation Method 1

Identification and use of substances that interfere and/or disrupt in quorum sensing pathways of pathogenic bacteria and thus block their virulence

Methodology Applied

Scientific EffectQuorum sensing interference:

Implementation Method 2

a method of treating an inflammatory disease, wherein said inflammatory disease comprises inflammatory disease in the lungs, inflammatory disease in the liver, inflammatory diseases in the gastrointestinal tract

Methodology Applied

Scientific EffectAnti-inflammatory effect:

Implementation Method 3

a method for treating a disease selected from the group consisting of: an inflammatory disease, an infectious disease, and an amyloid aggregates-related disease

Methodology Applied

Scientific EffectAmyloid aggregation reduction:

Data Source

PatentUS20220160680A1Microorganism mixtures, molecules derived therefrom, and methods of use thereof

Publication Date: 2022.05.26 BG NEGEV TECHNOLOGIES & APPLICATIONS LTD

AI summary

The present invention is directed to a composition comprising a Tryptophol derivative and a 4-Ethyl-Phenol derivative, and at least one acceptable carrier. Further provided are methods for reducing the formation of load of organic-based contaminant.