Fraxinus excelsior Seed Extract for Diabetes Management

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Solution Overview

Problem

Type 2 diabetes mellitus (DM-2) and obesity-related diseases pose significant health challenges due to insulin deficiency, insulin insensitivity, and increasing prevalence of obesity, with current treatments having limitations in effectively managing blood glucose and weight.

Innovation Solution

Isolation and extraction of novel secoiridoids from Fraxinus excelsior seeds, specifically excelside A and B, which are oleoside-type secoiridoids, using a unique extraction and chromatographic process, and their use in activating PPAR-alpha to inhibit adipogenesis and improve insulin sensitivity.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If conventional extraction methods are used to obtain bioactive compounds from plant material, then the extraction process is simple and quick, but the extraction efficiency and yield of active compounds are low

Engineering Contradiction:
Improveextraction efficiencyVSAvoidextraction process complexity
Core Design Contradiction:
ProductivityVSDevice complexity

Solution Approach 1:

The extraction process is divided into multiple sequential steps: initial extraction with organic solvent, filtration, concentration, and sequential elution with solvents of increasing polarity (water, ethanol, methanol, acetone). This segmentation allows each step to optimize for specific compound classes, dramatically improving overall extraction efficiency and yield of bioactive compounds compared to single-step methods.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The patent performs preliminary actions by first extracting with non-polar solvents to remove lipids and chlorophylls, then progressively using polar solvents to extract phenolic compounds, flavonoids, and other polar bioactives. This preliminary separation prevents interference between compound classes and maximizes the yield of target compounds in each fraction.

Inventive Principle:
Principle #10Preliminary action

2Adaptability or versatility

If a broad spectrum of therapeutic agents is used to treat type 2 diabetes, then more treatment options are available, but the complexity of treatment regimens increases

Engineering Contradiction:
Improvetreatment versatilityVSAvoidtreatment regimen complexity
Core Design Contradiction:
Adaptability or versatilityVSDevice complexity

Solution Approach 1:

The Fraxinus excelsior seed extract demonstrates multi-functionality by simultaneously exhibiting hypoglycemic activity (blood glucose lowering), antioxidant properties, anti-inflammatory effects, and potential lipid-lowering capabilities. This single extract can address multiple pathogenic mechanisms of type 2 diabetes concurrently, providing versatile treatment without requiring multiple separate medications or complex regimens.

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

Solution Approach 2:

The patent utilizes a composite phytochemical mixture from F. excelsior seeds containing diverse compounds including phenolic acids, flavonoids, secoiridoids, and triterpenoids. This composite formulation leverages synergistic interactions between different compound classes to achieve enhanced therapeutic effects for diabetes management, combining multiple mechanisms of action in a single treatment.

Inventive Principle:
Principle #40Composite materials

3Ease of operation

If traditional medicines are used to treat type 2 diabetes, then cultural relevance and accessibility are improved, but the standardization and quality control become difficult

Engineering Contradiction:
ImproveaccessibilityVSAvoidquality standardization
Core Design Contradiction:
Ease of operationVSManufacturing precision

Solution Approach 1:

The patent establishes specific quantitative parameters for the extract including concentration ranges of key bioactive compounds (phenolic acids, flavonoids, secoiridoids), extraction conditions (solvent ratios, temperatures, durations), and yield specifications. By defining these critical parameters, the traditional remedy can be standardized for consistent quality, potency, and safety while maintaining accessibility through natural product formulation.

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 secoiridoids from Fraxinus excelsior seeds demonstrate significant hypoglycemic activity, reduce body weight, and improve insulin sensitivity by inhibiting adipogenesis and activating PPAR-alpha, effectively managing DM-2 and obesity-related conditions.

Implementation Method 1

The seeds are ground into granules with a particle size in a range from 0.1 mm to 30 mm to increase the surface area for the solvent to contact and to increase extraction efficiency

Methodology Applied
Scientific EffectExtraction: Solvation

Implementation Method 2

The secoiridoids can be isolated from the FE extract by a chromatographic process

Methodology Applied
Scientific EffectChromatography: Chromatography

Data Source

PatentEP2664361B1Extract of fraxinus excelsior seeds and therapeutic applications therefor
Publication Date: 2015.07.29 NATUREX SA
  • EP2664361B1 patent drawingFigure 1-1~1-2
  • EP2664361B1 patent drawingFigure 1-3~1-4
  • EP2664361B1 patent drawingFigure 1-5~1-6

AI summary

A Fraxinus excelsior seed extract that can be administered for therapeutic treatment of a subject, including a human, by blocking fat synthesis, activating PPAR-alpha, increasing hypoglycemic activity, reducing bodyweight, controlling fasting plasma insulin levels against hyperinsulinemia, and promoting insulin sensitivity and causing a beneficial acute insulinotropic effect. The Fraxinus excelsior seed extract includes, inter alia, an isolated compound (2S, 3E, 4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl) oxy]-3,4-dihydro-5-(methoxycarbonyl) methyl ester, commonly called excelside A, an isolated compound (2S, 3E, 4S) 2H-Pyran-4-acetic acid-3-ethylidene-2-[(6-O-β-D-glucopyranosyl-β-D-glucopyranosyl)oxy]-3,4-dihydro-5-(methoxycarbonyl)2-(4- hydroxyphenyl) ethyl ester, commonly called excelside B, and the compounds GI5, GI3, nuzhenide, and oleoside dimethyl ester.