Glucomoringin Isothiocyanate Modulation of Neuropathic Pain

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Solution Overview

Problem

Current treatments for chronic peripheral and neuropathic pain, particularly diabetic peripheral neuropathy and chemotherapy-induced neuropathy, are inadequate in providing effective relief, with existing pharmacological agents showing limited efficacy and potential toxicity, necessitating the exploration of novel natural and botanical derivatives.

Innovation Solution

Glucomoringin (GMG) and its isothiocyanate derivative GMG-ITC, isolated from Moringa oleifera seeds, are used to modulate peripheral neuropathic pain through oral or topical administration, either alone or in combination with other substances, formulated into various pharmaceutical forms, leveraging their bioactive properties to address pain induced by chemotherapy agents like taxanes and platinum complexes.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional pharmacological agents (amitriptyline, gabapentin, duloxetine, pregabalin) are used to treat chronic peripheral and neuropathic pain, then pain relief is achieved to some extent, but the treatments show limited efficacy and potential toxicity, and no real unique treatment has been found to date

Engineering Contradiction:

Improvepain relief efficacyVSAvoidtoxicity

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The patent employs natural products (glucomoringin and its isothiocyanate derivative) as alternative therapeutic agents that may offer effective pain relief with reduced toxicity compared to conventional pharmacological agents. These natural compounds represent a search for safer, more effective treatments that replace or complement current standard therapies.

Inventive Principle:

Principle #27Cheap short-living objects (Disposable)

Solution Approach 2:

The patent investigates the bioactivation of glucomoringin to its isothiocyanate derivative form, which may alter the pharmacological properties and enhance pain-modulating activity while reducing toxicity. This transformation represents a change in the chemical parameter of the active substance to achieve better therapeutic outcomes.

Inventive Principle:

Principle #35Parameter changes

2Reliability

If chemotherapy drugs (taxanes, cisplatin, oxaliplatin, epothilones, bortezomid, vincristine) are used to treat cancer, then cancer treatment is achieved, but neurotoxicity and peripheral neuropathy with pain generation occur

Engineering Contradiction:

Improvecancer treatment efficacyVSAvoidneurotoxicity

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent explores the use of glucomoringin and its isothiocyanate derivative as neuroprotective agents that may counteract the neurotoxic effects of chemotherapy drugs. These natural compounds could convert the harmful neurotoxicity induced by cancer treatment into a beneficial protective effect, reducing peripheral neuropathy and pain while maintaining cancer treatment efficacy.

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

3Reliability

If natural and botanical derivatives (plants containing phenolic compounds, cannabinoids, alkaloids, and vanilloids) are investigated for pain treatment, then promising results are obtained, but routine use is not recommended in current clinical practice

Engineering Contradiction:

Improvepain modulation activityVSAvoidclinical practice adoption

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent isolates and characterizes glucomoringin and its isothiocyanate derivative from Moringa oleifera seeds, extracting the active pain-modulating components from the natural plant material. This extraction process enables standardized preparation and potential clinical application of these natural derivatives, moving them from experimental investigation to potential routine use.

Inventive Principle:

Principle #2Taking out (Extraction)

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

GMG and GMG-ITC demonstrate significant pain-modulating activity in experimental models, comparable to standard treatments like pregabalin, offering a promising alternative for managing neuropathic pain with potential for reduced toxicity and improved patient outcomes.

Implementation Method 1

Its structure is depicted in Figure along with that of the corresponding des-thioglucoside isothiocyanate (4-(α-L-rhamnosyloxy)-benzyl isothiocyanate; glucomoringin-des-thioglucoside; GMG-ITC) which is formed by bioactivation of GMG with the enzyme myrosinase.

Methodology Applied

Scientific EffectBioactivation: Enzyme

Data Source

PatentEP3280407B1Use of isothiocyanate derivatives as modulators of peripheral and neuropathic pain

Publication Date: 2020.08.12 INDENA SPA

AI summary

The present invention relates to the use of glucomoringin (GMG) and of the corresponding isothiocyanate derivative glucomoringin des-thioglucoside (GMG-ITC) as modulators of peripheral pain with specific reference to that linked with diabetic peripheral neuropathy and chemotherapy-induced neuropathy.