Burdock Fruit Extract Arctigenin Production Enzymatic Conversion
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Solution Overview
Problem
Current methods struggle to produce a burdock fruit extract with high arctigenin content and controlled arctigenin to arctiin ratio, making it difficult to develop an effective anticancer agent for pancreatic cancer, especially for patients refractory to gemcitabine treatment.
Innovation Solution
A method involving enzymatic conversion of arctiin to arctigenin using beta-glucosidase from burdock fruit, adjusting enzyme activity, particle size, and extraction temperature to achieve a weight ratio of arctigenin to arctiin between 0.7 to 1.3, resulting in a burdock fruit extract with enhanced anticancer properties.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Manufacturing precision
If conventional hot water extraction method is used, then extraction process is simple, but arctigenin content in extract is low and arctigenin to arctiin ratio cannot be controlled
Solution Approach 1:
The patent applies preliminary action by performing enzymatic conversion of arctiin to arctigenin using beta-glucosidase before the extraction process. This pre-treatment step increases the arctigenin content in the raw material, which then allows the subsequent extraction to produce an extract with high and controllable arctigenin content and a controlled arctigenin to arctiin ratio (0.7 to 1.3).
Solution Approach 2:
The patent employs parameter changes by optimizing several extraction parameters including particle size (0.5 to 5.0 mm), extraction temperature (20 to 80°C), extraction time (1 to 24 hours), and solvent-to-material ratio (5 to 20 mL/g). By adjusting these parameters, the method achieves high arctigenin content (0.3 to 3.0%) and controlled arctigenin to arctiin ratio in the extract.
2Quantity of substance
If arctigenin content is increased, then anticancer effect is enhanced, but solubility in water decreases
Solution Approach 1:
The patent uses parameter changes by optimizing extraction temperature (20 to 80°C) and particle size (0.5 to 5.0 mm) to achieve high arctigenin content while maintaining adequate water solubility. The controlled extraction process ensures that arctigenin is extracted along with other soluble components, creating a formulation that balances concentration with solubility.
3Productivity
If enzymatic conversion is used to increase arctigenin content, then arctigenin yield is improved, but production time and process complexity increase
Solution Approach 1:
The patent optimizes enzymatic conversion parameters including incubation temperature (30 to 50°C), pH (4.0 to 6.0), and time (1 to 24 hours) to achieve efficient arctiin to arctigenin conversion. By finding the optimal parameter range, the method achieves high arctigenin yield while minimizing the additional time required compared to conventional 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
The method produces a burdock fruit extract with a high arctigenin content and controlled ratio, demonstrating significant anticancer effects, including tumor reduction and low toxicity, effectively treating pancreatic cancer refractory to gemcitabine.
Implementation Method 1
enzymatic conversion of arctiin to arctigenin using beta-glucosidase from burdock fruit
Implementation Method 2
enzymatic conversion of arctiin to arctigenin
Implementation Method 3
extraction temperature to achieve a weight ratio of arctigenin to arctiin between 0.7 to 1.3
Data Source
AI summary
The present invention is intended to provide a novel anticancer agent which is effective to a cancer. After administering an agent prepared using burdock fruit extract to a pancreas cancer patient so that a dose of arctigenin was 100 mg or more per day, the tumor reducing effect was observed, and, in addition, lowering of tumor markers was confirmed. The present invention provides an anticancer agent containing arctigenin, wherein a dose of the arctigenin is 100 mg or more per day. In addition, the present invention provides the anticancer agent containing arctigenin and arctiin at a weight ratio of arctigenin/arctiin=0.7 to 1.3.