Endocrine Treatment Compositions Using GPCR-Mediated GLP-1 Secretion
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Solution Overview
Problem
Existing GLP-1 and dual GLP-1/GIP analogs for treating obesity and diabetes mellitus are associated with high risks of adverse events, side effects, and high costs, particularly due to subcutaneous injections and immune responses.
Innovation Solution
Compositions comprising natural compounds that activate olfactory receptors (OR51E1, OR2C1, FFAR1, FFAR4, TRPA1) and free fatty acids (lauric acid, cinnamaldehyde) to induce GLP-1 and GIP secretion, reducing body mass and appetite without injections or significant side effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If subcutaneous injections of GLP-1 and dual GLP-1/GIP analogs are used to treat obesity and diabetes mellitus, then insulin secretion and appetite suppression are improved, but the risk of adverse events, side effects, and immune responses increases
Solution Approach 1:
The patent uses natural compounds (orphan olfactory agonists and free fatty acids) as intermediary substances that indirectly activate GLP-1 and GIP secretion through olfactory receptors and free fatty acid receptors, rather than directly administering GLP-1/GIP analogs via injection. This intermediary approach activates endogenous secretion pathways, reducing immune response risks while maintaining therapeutic efficacy
Solution Approach 2:
The patent replaces the mechanical injection system with an oral or non-invasive administration system using natural compounds. Instead of using needles and subcutaneous delivery mechanisms, the invention uses ingestible or inhalable compositions that activate receptors naturally, eliminating injection-related adverse events and improving patient compliance
2Reliability
If traditional GLP-1 and dual GLP-1/GIP analogs are administered, then treatment effectiveness for obesity and diabetes is improved, but treatment cost increases significantly
Solution Approach 1:
The patent employs natural compounds such as orphan olfactory agonists and free fatty acids that are inexpensive to produce and can be administered orally or non-invasively. These short-acting natural substances are metabolized and eliminated naturally, requiring no expensive delivery systems or specialized storage, thereby significantly reducing treatment costs while maintaining effectiveness
Solution Approach 2:
The patent changes the administration route from expensive subcutaneous injection to affordable oral or inhalation delivery. By transforming the delivery parameters and using naturally occurring compounds instead of synthetic analogs, the treatment achieves cost-effectiveness without sacrificing therapeutic outcomes
3Reliability
If subcutaneous injections are used for GLP-1 analog administration, then insulin secretion is effectively induced, but patient compliance and ease of operation deteriorate
Solution Approach 1:
The patent replaces the complex injection mechanism with simple oral or inhalation administration of natural compounds. This substitution eliminates the need for needles, syringes, and injection training, making the treatment as easy to administer as a pill or breath, thereby dramatically improving patient compliance and ease of operation
Solution Approach 2:
The patent enables patients to self-administer treatment through oral ingestion or inhalation without requiring healthcare professional intervention for injections. The natural compounds are designed for direct patient use, empowering patients to manage their own treatment and improving accessibility and compliance
4Weight of moving object
If GLP-1 analogs are administered to suppress appetite and reduce body mass, then weight loss is achieved, but the risk of hypoglycemia and other adverse pathological events increases
Solution Approach 1:
The patent uses natural compounds as intermediaries that activate endogenous GLP-1 and GIP secretion through olfactory and free fatty acid receptors. This indirect activation pathway produces more physiological and balanced hormone release, avoiding the excessive and unregulated insulin secretion that causes hypoglycemia with direct GLP-1 analog administration, while still achieving effective appetite suppression and weight loss
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 compositions effectively modulate insulin secretion and appetite suppression with minimal side effects, offering a safer and potentially cost-effective alternative to traditional GLP-1 and dual GLP-1/GIP analogs.
Implementation Method 1
compositions comprising natural compounds that activate olfactory receptors (OR51E1, OR2C1, FFAR1, FFAR4, TRPA1) and free fatty acids (lauric acid, cinnamaldehyde) to induce GLP-1 and GIP secretion
Implementation Method 2
insulin secretion is induced by pancreatic β-cells when glucagon-like peptide-1 (GLP-1) binds to and activates GLP-1 receptor proteins on endogenous gastrointestinal (GI) cells
Implementation Method 3
GLP-1 also decreases the rate of gastric emptying and acid secretion, resulting in reduced appetite and, thereby, weight loss
Data Source
AI summary
Disclosed herein are compounds and ligands, and compositions formed therewith, which modulate insulin secretion, suppress appetite, and reduce body mass by activating G-protein coupled receptors (GPCRs), such as ectopic olfactory receptors, and transient receptor potential (TRP) ion channels. Also disclosed herein are methods for using the compositions to treat endocrine diseases, such as type-2 diabetes and obesity.