Burdock Fruit Extract Arctigenin Arctiin Ratio Control

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Solution Overview

Problem

Current methods struggle to produce burdock fruit extracts with a high content of arctigenin and arctiin at a controlled weight ratio, particularly 1:1, due to arctigenin's low content and poor water solubility, making it difficult to achieve effective anticancer agents for pancreatic cancer treatment.

Innovation Solution

A method involving selecting burdock fruits with high beta-glucosidase activity, cutting them to specific particle sizes, enzymatically converting arctiin to arctigenin at controlled temperatures, and extracting with ethanol at elevated temperatures to achieve a burdock fruit extract with a weight ratio of arctigenin/arctiin between 0.7 to 1.3.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of manufacture

If conventional hot water extraction method is used, then extraction process is simple, but arctigenin content remains low and water solubility is poor

Engineering Contradiction:
Improveextraction process simplicityVSAvoidarctigenin content
Core Design Contradiction:
Ease of manufactureVSQuantity of substance

Solution Approach 1:

The patent changes the extraction parameters by using organic solvents (ethanol, methanol, or acetone) instead of water, and controls the extraction temperature between 20-80°C. This parameter change enables effective extraction of arctigenin while overcoming its poor water solubility, achieving both high arctigenin content (0.1-10%) and improved manufacturability

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent creates a composite extract containing multiple components (arctigenin, arctiin, and other burdock fruit constituents) in specific ratios. By controlling the arctigenin/arctiin weight ratio to be 0.1 to 10, the composite extract achieves enhanced anticancer activity while maintaining good solubility in organic solvents

Inventive Principle:
Principle #40Composite materials

2Quantity of substance

If enzymatic conversion is used to increase arctigenin content, then arctigenin content increases, but control of arctigenin/arctiin ratio becomes difficult

Engineering Contradiction:
Improvearctigenin contentVSAvoidarctigenin/arctiin ratio control
Core Design Contradiction:
Quantity of substanceVSManufacturing precision

Solution Approach 1:

The patent performs preliminary action by selecting burdock fruit raw materials with specific characteristics (high beta-glucosidase activity, appropriate moisture content of 5-20%) before extraction. This preliminary selection ensures that the enzymatic conversion during extraction produces the desired arctigenin/arctiin ratio (0.1 to 10) without requiring additional conversion steps, thereby achieving both high arctigenin content and precise ratio control

Inventive Principle:
Principle #10Preliminary action

Solution Approach 2:

The patent controls the extraction temperature parameter (20-80°C) to optimize the enzymatic conversion of arctiin to arctigenin by beta-glucosidase. By adjusting this temperature parameter, the patent achieves precise control over the arctigenin/arctiin ratio while maximizing arctigenin extraction efficiency

Inventive Principle:
Principle #35Parameter changes

3Reliability

If arctigenin content is increased for anticancer effect, then anticancer activity improves, but water solubility decreases making extraction difficult

Engineering Contradiction:
Improveanticancer effectVSAvoidextraction difficulty
Core Design Contradiction:
ReliabilityVSEase of manufacture

Solution Approach 1:

The patent uses organic solvents (ethanol, methanol, or acetone) as intermediaries to extract arctigenin from burdock fruit. These intermediary solvents bridge the gap between the hydrophobic arctigenin and the aqueous environment, enabling effective extraction of high arctigenin content while maintaining ease of manufacture through standard extraction procedures

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

This method enables the production of burdock fruit extracts with a stable antitumor effect, improving growth inhibition and antitumor activity for pancreatic cancer treatment while enhancing productivity.

Implementation Method 1

converting arctiin which is inherent in the burdock fruit into arctigenin by enzymatic conversion by beta-glucosidase which is inherent in the burdock fruit

Methodology Applied
Scientific EffectEnzymatic conversion: Enzyme

Implementation Method 2

enzymatically converting arctiin into arctigenin with beta-glucosidase

Methodology Applied
Scientific EffectHydrolysis: Hydrolysis

Implementation Method 3

extracting an extract containing arctigenin and arctiin of a temperature of 80°C or more by adding an organic solvent after the step of enzymatic conversion

Methodology Applied
Scientific EffectExtraction: Solvation

Data Source

PatentEP2623107B1Arctigenin-containing bardanae fructus extract and method for producing same
Publication Date: 2019.03.06 KRACIE HLDG

AI summary

PROBLEM TO BE SOLVED The present invention is intended to provide a burdock fruit extract containing arctigenin and arctiin at a definite ratio and a method for producing the same. More particularly, the present invention is intended to provide a method for producing a burdock fruit extract containing arctigenin and arctiin at a weight ratio of approximately 1:1. SOLUTION A method for producing a burdock fruit extract containing arctigenin and arctiin at a weight ratio of arctigenin/arctiin = 0.7 to 1.3 is provided, including the steps of: cutting a burdock fruit and converting arctiin which is inherent in the burdock fruit into arctigenin by enzymatic conversion by beta-glucosidase which is inherent in the burdock fruit, wherein the enzymatic conversion includes reaction at a temperature from 20°C to 50°C. Also provided is the method further including a step of extracting an extract containing arctigenin and arctiin by adding an organic solvent and heating to reflux.