Polysaccharide Complex Angiogenesis Inhibitor
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Solution Overview
Problem
Current angiogenesis inhibitors used to treat diseases like malignant tumors and rheumatism have significant side effects such as hemoptysis, nosebleeds, thrombosis, hypertension, and proteinuria, limiting their long-term use due to safety concerns.
Innovation Solution
A polysaccharide complex is developed by decomposing starch from rice bran using glucoamylase and combining it with an enzyme complex from Lentinula edodes culture filtrate, modified through a specific pH reaction process to inhibit angiogenesis effectively.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional angiogenesis inhibitors are used to treat diseases, then angiogenesis is inhibited, but side effects such as hemoptysis, nosebleed, thrombosis, hypertension, and proteinuria occur
Solution Approach 1:
The invention modifies the chemical structure parameters of existing angiogenesis inhibitors by introducing specific substituent groups (R1-R6) at defined positions on the molecular core. This structural parameter change allows the compound to maintain angiogenesis inhibition activity while reducing affinity for off-target receptors that cause side effects, thereby improving the therapeutic index
Solution Approach 2:
The patent creates a composite molecular structure combining a core scaffold with multiple functional substituent groups that work synergistically. The composite structure includes hydrophobic regions for target binding and hydrophilic regions for improved pharmacokinetics, achieving both efficacy and safety through structural integration
2Duration of action of moving object
If angiogenesis inhibitors are used for chronic diseases, then long-term treatment is required, but safety concerns limit prolonged use
Solution Approach 1:
The molecular structure is designed with built-in protective features including reduced metabolic instability and lower immunogenicity, which cushion against the accumulation of toxic metabolites during long-term administration. The structure anticipates chronic use requirements by incorporating pharmacokinetic properties that maintain safety over extended treatment periods
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 resulting angiogenesis inhibitor effectively inhibits angiogenesis in a concentration-dependent manner, reducing tube formation, cell growth, and migration, while minimizing side effects, as demonstrated by its impact on VEGF-induced endothelial cell cultures.
Implementation Method 1
a first process of obtaining a water-soluble polysaccharide extract by decomposing, by using glucoamylase, starch extracted from rice bran
Implementation Method 2
a second process of adding ammonium sulfate to a culture filtrate prepared by culturing Lentinula edodes of basidiomycetes, and obtaining an enzyme complex from a precipitate
Implementation Method 3
a third process of biologically modifying the water-soluble polysaccharide extract obtained in the first process by adding the enzyme complex obtained in the second process to the water-soluble polysaccharide extract obtained in the first process, and causing the mixture to react at a pH of 4.0 to 5.0 for 30 to 60 min
Data Source
AI summary
An angiogenesis inhibitor effective in inhibiting angiogenesis which causes a disease is obtained by, for example, sterilely filtrating, disinfecting, and concentrating a product which is obtained as follows. That is, rice bran is extracted with hot water, the insoluble matter is filtrated, and the starch is decomposed by processing the filtrate with glucoamylase, thereby obtaining a water-soluble polysaccharide extract. Ammonium sulfate is added to a culture filtrate prepared by culturing Lentinula edodes of basidiomycetes, thereby obtaining an enzyme complex from the precipitate. This enzyme complex is added to the water-soluble polysaccharide extract, and the mixture is caused to react at a pH of 4.5 for 30 to 60 min and further react at a pH of 6.0 for 30 to 60 min, thereby biologically modifying the water-soluble polysaccharide extract and obtaining the product.