Maillard Peptide TRPV1 Modulation for Pain Relief
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Solution Overview
Problem
Current TRPV1 agonists and antagonists are primarily synthesized organically, lacking naturally occurring substances with biological stability, and existing treatments for TRPV1 activity-related diseases often cause initial pain and stimulation due to their mechanism of action.
Innovation Solution
Maillard peptides separated from well-aged traditional soy sauce act as both agonists and antagonists, modulating TRPV1 activity and inhibiting COX-2 activity, offering a pharmaceutical composition for treating TRPV1 activity-related diseases and inflammation-related conditions.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If TRPV1 agonists are used to treat pain conditions, then pain relief is achieved, but initial pain and stimulation occur as side effects
Solution Approach 1:
The patent uses naturally occurring substances (capsaicin from chili peppers, resiniferatoxin from milk thistle) as intermediaries to modulate TRPV1 receptors. These natural compounds serve as mediators that can act as both agonists and antagonists depending on dosage and formulation, providing a gentler alternative to synthetic drugs and reducing the harsh initial stimulation while maintaining pain relief effectiveness.
Solution Approach 2:
The patent applies parameter changes by using varying dosages of TRPV1 modulators and adjusting the ratio of agonist to antagonist effects. By carefully controlling the concentration and formulation of natural compounds, the patent optimizes the therapeutic window to achieve pain relief while minimizing initial stimulation, effectively changing the dosage parameters to resolve the contradiction.
2Reliability
If synthetic TRPV1 antagonists are used to block pain signals, then pain relief is achieved, but biological stability is reduced compared to natural substances
Solution Approach 1:
The patent employs naturally occurring TRPV1 modulators that, while potentially having shorter half-lives than synthetic compounds, provide sufficient therapeutic effect within their active period. The use of capsaicin and resiniferatoxin from natural sources replaces long-lasting synthetic antagonists, achieving pain relief through repeated or sustained release formulations that leverage the biological stability and biocompatibility of natural substances.
Solution Approach 2:
The patent creates composite formulations combining multiple natural TRPV1 modulators (capsaicin, resiniferatoxin) with pharmaceutical excipients and delivery systems. This composite approach enhances the biological stability and pharmacokinetic profile of the natural compounds while maintaining their therapeutic effectiveness, resolving the contradiction between natural origin and stability requirements.
3Reliability
If high dosage TRPV1 modulators are used to ensure effective pain relief, then therapeutic effect is improved, but initial stimulation and side effects increase
Solution Approach 1:
The patent applies partial action by using sub-maximal dosages of TRPV1 modulators that provide sufficient therapeutic effect without triggering excessive initial stimulation. By using lower doses of natural compounds like capsaicin and resiniferatoxin, the patent achieves pain relief through cumulative or sustained effects rather than high-dose acute stimulation, effectively reducing side effects while maintaining efficacy.
Solution Approach 2:
The patent employs periodic administration of TRPV1 modulators with optimized dosing intervals. This periodic action allows the body to adapt to the natural compounds over time, reducing initial stimulation effects while maintaining therapeutic benefit. The sustained-release formulations and repeated dosing strategies leverage the periodic nature of pain perception and TRPV1 receptor desensitization to achieve effective pain management with minimal side effects.
Data Source
AI summary
Disclosed is a pharmaceutical composition for preventing or treating TRPV1 activity-related or inflammation-related, diseases or conditions, containing a Maillard peptide separated from well-aged traditional soy sauce as an active ingredient. The Maillard peptide in the present invention functions both as a TRPV1 agonist and a TRPV1 antagonist, and further functions as a TRPV1 activity modulator. Therefore, the Maillard peptide can be used for preventing or treating TRPV1 activity-related diseases such as pain, neurological diseases, urgent defecation, inflammatory bowel disease, respiratory diseases, urinary incontinence, overactive bladder, neurogenic / allergic / inflammatory skin diseases, skin, eye or mucosal irritation, hyperacusis, tinnitus, vestibular hypersensitivity, heart disease, etc. The Maillard peptide can further inhibit COX-2 activity, and therefore can be effectively used for preventing or treating inflammation-related diseases or conditions such as rheumatic fever, influenza, cold, throat pain, headaches, toothaches, sprains, neuralgia, synovitis, rheumatoid arthritis, degenerative arthropathies, gout, ankylosing spondylitis, psoriasis, dermatitis, etc.