Phospholipid Ester Conjugated Linoleic Acid Neuroinflammation

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Solution Overview

Problem

Current treatments for psychiatric disorders with neuroinflammatory and neurodegenerative bases, such as depression and schizophrenia, are inadequate in addressing the underlying neuroinflammatory mechanisms, leading to suboptimal clinical outcomes and unmet clinical needs.

Innovation Solution

The development of a phospholipid ester conjugated with conjugated linoleic acid (CLA), specifically the c9,t11 isomer, which is readily incorporated into the central nervous system, activates PPAR alpha, increasing levels of PEA and OEA, thereby exerting anti-inflammatory effects and promoting neurogenesis, reducing TNF-alpha levels, and improving dopaminergic function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional therapies are used for psychiatric disorders, then treatment is provided, but the underlying neuroinflammatory mechanisms are not adequately addressed, leading to suboptimal clinical outcomes

Engineering Contradiction:
Improveclinical outcomesVSAvoidneuroinflammatory mechanisms
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent introduces PPAR alpha as an intermediary target that mediates between the administered compound and the neuroinflammatory pathways. By activating PPAR alpha, the treatment indirectly addresses neuroinflammatory mechanisms through this molecular mediator, thereby improving clinical outcomes while specifically targeting the harmful inflammatory pathways in psychiatric disorders

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The patent employs parameter changes by modifying the metabolic state through PPAR alpha activation, which alters the expression of genes involved in inflammation and metabolism. This changes the biochemical parameters of neuroinflammatory pathways, shifting them from a pro-inflammatory state to an anti-inflammatory state, thus addressing the underlying mechanisms while improving treatment reliability

Inventive Principle:
Principle #35Parameter changes

2Object-affected harmful factors

If anti-inflammatory treatments are applied, then neuroinflammatory activation is reduced, but the complexity of treating multiple psychiatric symptoms simultaneously increases

Engineering Contradiction:
Improveneuroinflammatory activationVSAvoidtreatment complexity
Core Design Contradiction:
Object-affected harmful factorsVSDevice complexity

Solution Approach 1:

The patent applies universality by using a single compound that simultaneously addresses multiple aspects of psychiatric disorders through PPAR alpha activation. This multi-functional approach tackles neuroinflammatory activation, metabolic abnormalities, and neuronal protection in one treatment, reducing overall treatment complexity while effectively reducing neuroinflammatory activation across different psychiatric conditions

Inventive Principle:
Principle #6Universality (Multi-functionality)

3Ease of operation

If current antidepressant therapies are used, then depressive symptoms are treated, but neurogenesis and neuronal plasticity effects are insufficient

Engineering Contradiction:
Improvedepressive symptom treatmentVSAvoidneurogenesis and neuronal plasticity
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent uses parameter changes by activating PPAR alpha to alter the biochemical environment in a way that promotes neurogenesis and neuronal plasticity. This changes key parameters such as brain-derived neurotrophic factor expression and synaptic plasticity markers, thereby improving the reliability of neurogenic effects while maintaining ease of operation for treating depressive symptoms

Inventive Principle:
Principle #35Parameter changes

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 phospholipid ester with CLA enhances anti-inflammatory responses, improves neuronal function, and shows potential in treating psychiatric disorders by reducing inflammatory mediators and promoting synaptic and neuronal growth, offering a novel therapeutic approach for neuroinflammatory and neurodegenerative conditions.

Implementation Method 1

activates PPAR alpha, increasing levels of PEA and OEA, thereby exerting anti-inflammatory effects

Methodology Applied
Scientific EffectPPAR alpha activation:

Implementation Method 2

reducing TNF-alpha levels, and improving dopaminergic function

Methodology Applied
Scientific EffectAnti-inflammatory effect:

Data Source

PatentEP3174544B1Ester of a phospholipid with conjugated linoleic acid for the treatment of psychiatric disorders with neuroinflammatory and neurodegenerative basis
Publication Date: 2020.12.09 UNIV DEGLI STUDI DI CAGLIARI
  • EP3174544B1 patent drawingFigure 1A~1B
  • EP3174544B1 patent drawingFigure 2~3

AI summary

The present invention relates to an ester of a phospholipid with conjugated linoleic acid for use in the therapeutic treatment of or as a food supplement for psychiatric disorders with neuroinflammatory and neurodegenerative basis, such as depression and schizophrenia.