Meroterpene and Linoleic Acid Composition for Endocannabinoid Regulation

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Solution Overview

Problem

Current therapeutic agents targeting the endocannabinoid system fail to effectively address stress and skin health issues due to undesirable side effects and limitations in modulating key enzymes like FAAH, MAGL, and FABP-5, while also lacking non-psychoactive alternatives to cannabis-derived products.

Innovation Solution

The combination of select meroterpenes, particularly bakuchiol, with linoleic acid esters, glycosides, or glycerides, which inhibit FAAH, MAGL, and FABP-5, maintaining anandamide levels and reducing stress markers like cortisol, thereby promoting skin health and barrier function.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If cannabis-derived products are used to target the endocannabinoid system, then stress and skin health issues are addressed, but psychoactive side effects occur

Engineering Contradiction:
Improveefficacy in addressing stress and skin healthVSAvoidpsychoactive side effects
Core Design Contradiction:
ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent extracts and isolates specific active components (meroterpenes and linoleic acid derivatives) from cannabis and other natural sources, separating the therapeutic effects from the psychoactive properties by using only the beneficial compounds that modulate FAAH, MAGL, and FABP-5 enzymes

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The patent uses meroterpenes and linoleic acid derivatives as intermediary substances that indirectly modulate the endocannabinoid system by inhibiting degradation enzymes (FAAH, MAGL) and binding proteins (FABP-5), rather than directly activating cannabinoid receptors, thereby avoiding psychoactive effects while maintaining therapeutic benefits

Inventive Principle:
Principle #24Intermediary (Mediator)

2Reliability

If single-component therapies are used to inhibit FAAH, MAGL, or FABP-5, then specific enzyme activity is reduced, but overall efficacy is limited

Engineering Contradiction:
Improveenzyme inhibition capabilityVSAvoidoverall therapeutic efficacy
Core Design Contradiction:
ReliabilityVSProductivity

Solution Approach 1:

The patent combines multiple active components (meroterpenes and linoleic acid derivatives) into a synergistic formulation where each component contributes to inhibiting different targets in the endocannabinoid system, creating a cumulative and enhanced therapeutic effect that exceeds the sum of individual components

Inventive Principle:
Principle #5Merging (Combining)

Solution Approach 2:

The patent employs a multi-functional formulation where meroterpenes and linoleic acid derivatives simultaneously perform multiple functions: inhibiting FAAH to increase anandamide levels, inhibiting MAGL to increase 2-AG levels, and inhibiting FABP-5 to prevent anandamide degradation, thereby comprehensively modulating the endocannabinoid system through a single therapeutic agent

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

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 combination provides a calming effect, enhances skin health, and mitigates skin damage by reducing oxidative and inflammatory stress, offering a non-psychoactive alternative to cannabis-derived products with improved efficacy over individual components.

Implementation Method 1

the combination of select meroterpenes, especially bakuchiol, and linoleic acid, ester, glycoside and/or glyceride... are found to modulate, particularly inhibit, Fatty Acid Amide Hydrolase (FAAH), Monoacylglycerol Lipase (MAGL) and Fatty Acid Binding Protein-5 (FABP-5)

Methodology Applied
Scientific EffectEnzyme inhibition: Enzyme

Data Source

PatentUS11759433B2Compositions and methods for regulating the endocannabinoid system
Publication Date: 2023.09.19 SYTHEON LTD
  • US11759433B2 patent drawing
  • US11759433B2 patent drawing
  • US11759433B2 patent drawing

AI summary

Compositions comprising select meroterpenes and a linoleic component and the use thereof in regulating the endocannabinoid system (ECS).