Beta-endorphin Stabilization via Heparan Sulfate Synthesis

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Solution Overview

Problem

Current therapies for depression, particularly those using neurohormones like beta-endorphin, are limited by the short lifespan of these hormones due to rapid degradation, which reduces their effectiveness in maintaining mood enhancement and alleviating depressive states.

Innovation Solution

A therapeutic composition combining natural substances such as the oily extract of fleur de sel, Vanilla tahitensis, and Padina pavonica to enhance the expression and longevity of beta-endorphin, stabilizing it through the synthesis of heparan sulfate, thereby prolonging its biological activity and clinical effect.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If neurohormones such as beta-endorphin are used to treat depression, then mood enhancement and alleviation of depressive states are achieved, but the short lifespan and rapid degradation of these hormones reduce therapeutic effectiveness

Engineering Contradiction:
Improvetherapeutic effectivenessVSAvoidlifespan of beta-endorphin
Core Design Contradiction:
ReliabilityVSDuration of action of moving object

Solution Approach 1:

The patent uses heparan sulfate as an intermediary substance that binds to beta-endorphin, protecting it from degradation by proteases. This mediator extends the half-life of beta-endorphin from minutes to hours, maintaining therapeutic effectiveness while solving the rapid degradation problem

Inventive Principle:
Principle #24Intermediary (Mediator)

Solution Approach 2:

The invention creates a composite therapeutic system combining beta-endorphin with heparan sulfate or substances that stimulate its production (like padina pavonica extract). This composite approach allows the neurohormone to maintain stability and activity for extended periods, resolving the contradiction between effectiveness and duration

Inventive Principle:
Principle #40Composite materials

2Duration of action of moving object

If substances that inhibit degradation of neurotransmitters are used to increase their lifespan, then concentration of neurotransmitters in the synaptic cleft is increased, but the complexity of the treatment regimen increases

Engineering Contradiction:
Improvelifespan of neurotransmittersVSAvoidtreatment complexity
Core Design Contradiction:
Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent utilizes the body's own endogenous heparan sulfate system to protect beta-endorphin. By administering substances that stimulate the body's natural production of heparan sulfate (such as padina pavonica), the treatment leverages existing physiological mechanisms rather than requiring complex external intervention systems

Inventive Principle:
Principle #25Self-service

Solution Approach 2:

The invention combines multiple functions into a single therapeutic approach: the administered substance simultaneously stimulates heparan sulfate production and provides the neurohormone, creating a unified treatment that simplifies the regimen while achieving extended neurotransmitter lifespan

Inventive Principle:
Principle #5Merging (Combining)

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 combination significantly increases the half-life of beta-endorphin, maintaining its therapeutic benefits for longer periods, effectively addressing the limitations of existing treatments by enhancing mood and alleviating depressive symptoms.

Implementation Method 1

the release of beta-endorphin and its precursor pro-opiomelanocortin in cell culture was amplified when epithelial cells such as keratinocytes are cultured in the presence of the solubilized oily extract of fleur de sel

Methodology Applied
Scientific EffectStimulation of protein synthesis:

Implementation Method 2

The applicants have also shown that the extract of padine significantly enhanced the production of glycosaminoglycans such as heparan sulfate when added to a fibroblast culture

Methodology Applied
Scientific EffectProtease inhibition:

Implementation Method 3

one or more natural substances aimed at increasing the lifespan of beta-endorphin, by inhibiting the degradation of neurohormones

Methodology Applied
Scientific EffectEnzymatic degradation inhibition:

Data Source

PatentEP2198874B1Therapeutic compositions designed for treating depression
Publication Date: 2017.08.23 PATRINOVE SOCIETE CIVILE
  • EP2198874B1 patent drawingFigure 1
  • EP2198874B1 patent drawingFigure 2
  • EP2198874B1 patent drawingFigure 3

AI summary

Dietary and/or pharmaceutical composition (I) for oral administration, comprises an extract of Vanilla, an extract of Padina, and an extract of flower of salt ( Flos salis) in a mixture or in combination with one or more excipients, diluents or vehicles for oral. ACTIVITY : Anabolic; Antidepressant. MECHANISM OF ACTION : Beta-endorphin degradation inhibitor. The ability of (I) (comprising extract of Vanillaand Cyclotella) to inhibit beta-endorphin degradation was tested. The result showed that (I) exhibited the beta-endorphin expression of 0.22.