Quinone Methide Compounds Modulate Von Willebrand Factor Levels
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Solution Overview
Problem
Current treatments for blood disorders related to von Willebrand factor (vWF) levels are inadequate, as specific compounds from the quinone methides class have not been identified to modulate vWF activity effectively.
Innovation Solution
Development of triterpene and diterpene compounds, particularly quinone methides, that target endothelial cells to regulate vWF levels, with celastrol being a specific compound shown to reduce vWF protein expression in human endothelial cells.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If existing treatments are used for blood disorders related to vWF levels, then current standard care is provided, but treatment effectiveness is inadequate
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of quinone methide compounds to optimize their ability to modulate vWF levels. Specifically, the invention identifies compounds with particular substituent patterns (R1, R4, R9, R13, R14, R17, R20a groups) that enhance the compounds' effectiveness in lowering vWF expression in endothelial cells, thereby improving treatment reliability for blood disorders
Solution Approach 2:
The patent uses quinone methide compounds as intermediary substances that mediate between the administration route and the target endothelial cells. These compounds serve as chemical messengers that specifically interact with cellular pathways to downregulate vWF expression, providing a versatile mechanism for treating various blood disorders with different underlying causes
2Reliability
If vWF levels are elevated, then blood clotting function is maintained, but cardiovascular disease risk increases
Solution Approach 1:
The patent applies partial action by selectively lowering vWF levels rather than completely eliminating them. The quinone methide compounds achieve a therapeutic window where vWF expression is reduced from pathological levels to physiological levels, maintaining sufficient clotting function while eliminating excessive cardiovascular risk associated with chronically elevated vWF
Solution Approach 2:
The invention changes the parameter of vWF concentration from pathological (elevated) to therapeutic (optimized) levels. Through dose-dependent modulation by quinone methide compounds, the patent achieves precise control over vWF expression, transforming the harmful high-vWF state into a beneficial optimized state that balances clotting function with cardiovascular protection
3Adaptability or versatility
If new compound classes are developed, then novel intervention mechanisms are provided, but compound identification complexity increases
Solution Approach 1:
The patent segments the complex task of identifying effective vWF-modulating compounds into manageable components by establishing systematic structure-activity relationships. The invention divides the quinone methide compound class into specific subcategories based on substituent patterns, allowing researchers to methodically evaluate different structural variations and their effects on vWF modulation without being overwhelmed by the full complexity of compound discovery
Data Source
AI summary
The present invention relates to a compound having the structure of Formula (I) for use in the prevention or treatment of a blood disorder, in particular by the modulation of von Willebrand factor levels. A nutraceutical product or food product comprising the compound of the invention 5 are also provided.