Enteric Bitter Oligopeptides for Endogenous GLP-1 Release
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Solution Overview
Problem
Current treatments for type 2 diabetes mellitus, such as GLP-1 analogs and inhibitors, have adverse effects and do not effectively mimic the metabolic responses seen after bariatric surgery, which significantly improve glucose control and weight loss.
Innovation Solution
Administration of bitter oligopeptides, such as BPx1, BPx2, BPx3, and BPx4, derived from milk-whey proteins, that interact with bitter taste receptors like TAS2R38 on L-cells in the gastrointestinal tract to stimulate the release of GLP-1 and PYY, thereby enhancing metabolic responses similar to those observed post-bariatric surgery.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If GLP-1 analogs and inhibitors are used to treat type 2 diabetes, then glucose control is improved, but adverse effects occur and the treatment does not effectively mimic the metabolic responses seen after bariatric surgery
Solution Approach 1:
The patent uses bitter taste receptors (TAS2R) as intermediary targets instead of directly acting on GLP-1 pathways. Bitter peptides act as mediators that trigger endogenous GLP-1 release from L-cells through TAS2R activation, creating an indirect pathway that mimics physiological responses and avoids adverse effects associated with direct GLP-1 analogs
Solution Approach 2:
The treatment activates the body's own GLP-1 production system rather than introducing external analogs. By stimulating TAS2R receptors, the body's L-cells naturally release GLP-1, allowing the physiological system to serve itself and produce the therapeutic effect without external interference that causes adverse reactions
2Reliability
If bitter peptides are administered to stimulate GLP-1 release, then metabolic responses similar to post-bariatric surgery are achieved, but the peptides must survive gastrointestinal conditions to reach target receptors
Solution Approach 1:
The patent applies enteric coating technology before administration to protect bitter peptides from degradation. The coating is pre-applied to create a protective barrier that prevents gastrointestinal enzymes and acidic conditions from degrading the peptides before they reach the small intestine where TAS2R receptors are located
Solution Approach 2:
The enteric coating acts as an intermediary protective layer between the fragile bitter peptides and the harsh gastrointestinal environment. This mediator allows the peptides to pass through the stomach and upper intestine intact, releasing them only in the lower small intestine where they can effectively stimulate L-cells
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 bitter oligopeptides increase gut hormone release, leading to improved glucose control and weight management by mimicking the metabolic benefits of bariatric surgery without adverse effects, offering a potential therapeutic approach for type 2 diabetes.
Implementation Method 1
bitter oligopeptides, such as BPx1, BPx2, BPx3, and BPx4, derived from milk-whey proteins, that interact with bitter taste receptors like TAS2R38 on L-cells in the gastrointestinal tract
Data Source
AI summary
Described herein are methods and compositions for treatment of diabetes and/or obesity. Bitter oligopeptide molecules formulated for enteric delivery modulate signals involving receptors facing the lumen of the gastrointestinal tract, said signaling related hormones such as glucagon-like peptide-1 (GLP-1) and peptide tyrosine-tyrosine (PYY) that involve inhibition of gastric emptying and appetite. As a novel way to treat diabetes with limited adverse effects the described invention uses body's own endocrine system to treat diabetes, which is an advantage over current therapies that may simply provide disease management without cure or require more radical approaches such as surgical intervention.