HMOs Activating GPR35 to Reduce Nociception

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Solution Overview

Problem

Current treatments for nociception and nociceptive sensitivity, such as analgesics, have limited efficacy and often result in side effects, necessitating the development of safe and well-tolerated interventions that can be taken chronically to manage chronic pain conditions like fibromyalgia, irritable bowel syndrome, and neuropathic pain.

Innovation Solution

The use of human milk oligosaccharides, specifically 6′-sialyllactose (6′-SL) and lacto-N-tetraose (LNT), either alone or in combination, to activate the GPR35 receptor, reducing nociception and nociceptive sensitivity through a synthetic composition or dietary management, particularly for non-infant humans.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If analgesics are used to treat nociception and nociceptive sensitivity, then pain relief is achieved, but side effects occur and efficacy is limited

Engineering Contradiction:
Improveefficacy of pain reliefVSAvoidside effects of medication
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent uses GPR35 receptor as an intermediary target. Instead of directly blocking pain signals or using traditional analgesics that cause side effects, the invention employs 6'-SL and LNT to activate the GPR35 receptor, which then mediates the reduction of nociception and nociceptive sensitivity through natural physiological pathways, thereby achieving pain relief without the harmful side effects of conventional medications

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent changes the therapeutic parameter from using traditional analgesic drugs to using human milk oligosaccharides (6'-SL and LNT). This parameter change shifts the mechanism of action to receptor activation rather than direct analgesic effect, resulting in a treatment that maintains efficacy while eliminating the side effects associated with conventional pain medications

Inventive Principle:
Principle #35Parameter changes

2Duration of action of stationary object

If traditional analgesic treatments are used chronically to manage chronic pain, then pain symptoms are suppressed, but medication side effects increase and tolerance develops

Engineering Contradiction:
Improveduration of pain managementVSAvoidchronic medication side effects
Core Design Contradiction:
Duration of action of stationary objectVSObject-affected harmful factors

Solution Approach 1:

The GPR35 receptor serves as a safe intermediary that can be activated chronically without the accumulation of side effects. The patent demonstrates that long-term activation of GPR35 by 6'-SL and LNT provides sustained pain management while avoiding the tolerance and side effects that occur with chronic analgesic use, as the receptor activation follows natural physiological pathways

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs a natural, biologically-derived compound (human milk oligosaccharides) that can be administered chronically without accumulation. These compounds are metabolized and eliminated naturally, preventing the buildup of toxic metabolites that occurs with chronic analgesic use, thereby enabling long-term pain management without chronic side effects

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

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 activation of GPR35 receptors by 6′-SL and LNT provides a safe and effective means to prevent or reduce nociception and nociceptive sensitivity, as demonstrated by their synergistic action and safety profile, offering a potential solution for chronic pain management without the side effects of traditional medications.

Implementation Method 1

The activation of GPR35 receptors by 6'-SL and LNT provides a safe and effective means to prevent or reduce nociception and nociceptive sensitivity

Methodology Applied
Scientific EffectReceptor activation:

Data Source

PatentUS11304966B2Composition comprising HMOs for preventing or reducing nociception
Publication Date: 2022.04.19 GLYCOM AS
  • US11304966B2 patent drawing

AI summary

The application relates to synthetic compositions and methods for preventing or reducing nociception and/or nociceptive sensitivity in a non-infant human. The human is administered a composition comprising 6′-sialyllactose (6′-SL) and/or lacto-N-tetraose (LNT).