Endomorphin-1 Peptide Modulation of CGRP for Neurogenic Inflammation

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Solution Overview

Problem

Current therapies for neurogenic inflammation, particularly those involving steroids and non-steroidal anti-inflammatory compositions, suffer from high toxicity and poor efficacy, and existing treatments do not effectively address the role of endomorphin-1 peptides in inflammatory processes.

Innovation Solution

Administration of endomorphin-1 peptide or its analogs with a specific formula, such as Tyr-X1—X2—X3, where X1 is Pro, D-Lys, or D-Orn, X2 is Trp, Phe, or N-alkyl-Phe, and X3 is Phe, Phe-NH2, D-Phe, or p-Y-Phe, to inhibit neurogenic inflammation by modulating immune responses and reducing the over-production of calcitonin gene-related peptide (CGRP) and substance P.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If steroids and non-steroidal anti-inflammatory compositions are used to treat neurogenic inflammation, then anti-inflammatory effect is achieved, but toxicity increases and efficacy decreases

Engineering Contradiction:
ImproveefficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention changes the chemical parameter from conventional steroids and non-steroidal anti-inflammatory drugs to endomorphin-1 peptide and its analogs, which bind to mu-opiate receptors. This parameter change resolves the contradiction by providing anti-inflammatory effects through a different mechanism that does not carry the same toxicity profile as traditional anti-inflammatory compositions

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The invention uses endomorphin-1 peptide, a composite structure involving specific amino acid sequences (Tyr-X1-X2-X3) with particular properties, to achieve both efficacy and reduced toxicity. The specific composition of the peptide with defined molecular characteristics provides the desired therapeutic effect without the harmful side effects of conventional anti-inflammatory agents

Inventive Principle:
Principle #40Composite materials

2Reliability

If conventional anti-inflammatory compositions are used, then inflammation is suppressed, but treatment effectiveness is poor

Engineering Contradiction:
ImproveefficacyVSAvoidtreatment effectiveness
Core Design Contradiction:
ReliabilityVSQuantity of substance

Solution Approach 1:

The invention changes the therapeutic agent from conventional anti-inflammatory compositions to endomorphin-1 peptide analogs with specific molecular structures. This parameter change enables better treatment effectiveness by targeting mu-opiate receptors, which play a role in inflammatory processes, thereby resolving the contradiction between suppression of inflammation and treatment effectiveness

Inventive Principle:
Principle #35Parameter changes

3Reliability

If endomorphin-1 peptide and analogs are administered to treat neurogenic inflammation, then anti-inflammatory efficacy is improved, but toxicity is reduced compared to conventional treatments

Engineering Contradiction:
ImproveefficacyVSAvoidtoxicity
Core Design Contradiction:
ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The invention administers endomorphin-1 peptide and analogs with specific molecular parameters (amino acid sequences Tyr-X1-X2-X3) to achieve improved efficacy. The parameter change from conventional anti-inflammatory drugs to opioid peptides resolves the contradiction by providing a new mechanism of action that is both effective and less toxic

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The endomorphin-1 peptide acts as an intermediary substance that binds to mu-opiate receptors to mediate the anti-inflammatory effect. This intermediary mechanism resolves the contradiction by providing a bridge between the administered substance and the therapeutic effect, achieving both efficacy and reduced toxicity through receptor-mediated action

Inventive Principle:
Principle #24Intermediary (Mediator)

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 peptides effectively suppress neurogenic inflammatory reactions, providing a novel and potent treatment for conditions like neurogenic inflammation, osteoarthritis, asthma, and other inflammatory disorders with reduced side effects compared to existing treatments.

Implementation Method 1

Endomorphin-1 peptide (EM-1) and analogs have been found to exhibit opiate-like activity by binding to the mu (morphine) opiate receptor

Methodology Applied
Scientific EffectReceptor binding: Absorption (physical)

Data Source

PatentUS11324798B2Materials and methods for treatment of inflammation
Publication Date: 2022.05.10 CYTOGEL PHARMA LLC
  • US11324798B2 patent drawing
  • US11324798B2 patent drawing
  • US11324798B2 patent drawing

AI summary

The subject invention pertains to peptides and salts thereof that are useful as anti-inflammatory agents and to compositions containing such peptides and salts as active ingredients. Specifically exemplified herein are endomorphin-1 peptide (EM-1), analogs and salts thereof, and uses for modulation of calcitonin gene-related peptide (CGRP) production and/or substance P (SP) and for treatment of inflammation, particularly neurogenic inflammation.