Polysubstituted Hexaric Acids for Neuroprotection
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Solution Overview
Problem
Current treatments for neurodegenerative diseases, particularly Alzheimer's, lack effective neuroprotective agents that can significantly reduce the neurotoxicity of beta-amyloid peptides and promote neuronal survival and neurite network integrity.
Innovation Solution
Polysubstituted hexaric acids, specifically polycafeoylhexaric acids and their ester derivatives, such as leontopodic acid B and its esters, are developed for use in pharmaceutical and nutraceutical compositions to provide neuroprotection by reducing oxidative stress and promoting neuronal survival and astrocyte protection.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If current treatments for neurodegenerative diseases are used, then existing therapeutic options are available, but they lack effective neuroprotective capabilities to reduce beta-amyloid toxicity and promote neuronal survival
Solution Approach 1:
The patent applies parameter changes by modifying the chemical structure of hexaric acid derivatives through polysubstitution with caffeoyl groups and esterification with various alcohols. These structural parameter changes enhance the compounds' neuroprotective properties, enabling them to effectively reduce beta-amyloid toxicity and promote neuronal survival, thereby resolving the contradiction between reliability of neuroprotection and adaptability to specific neurodegenerative disease mechanisms
2Reliability
If polysubstituted hexaric acids and their ester derivatives are used, then neuroprotective effects are enhanced, but the complexity of compound structure increases
Solution Approach 1:
The patent employs composite material principles by creating polysubstituted hexaric acid derivatives where multiple caffeoyl groups are attached to a central glucaric acid core, and further esterified with various alcohol groups. This composite molecular architecture combines multiple functional moieties (phenolic hydroxyl groups from caffeoyl, carboxyl groups from glucaric acid, and ester linkages) into a single molecule, achieving enhanced neuroprotective effects through the synergistic interaction of these components while managing the inherent structural complexity
3Reliability
If leontopodic acid and its ester derivatives are developed for pharmaceutical use, then neuroprotective capabilities are improved, but the difficulty of extraction and purification from plant sources increases
Solution Approach 1:
The patent applies preliminary action by performing esterification reactions on leontopodic acid and its derivatives with various alcohols to create esterified products. This preliminary chemical modification serves multiple purposes: it enhances the neuroprotective and astrocyte-protective capabilities of the compounds, and simultaneously improves their pharmacokinetic properties and potential for pharmaceutical formulation, thereby addressing both the reliability of neuroprotection and the ease of manufacture by creating more stable and bioavailable derivatives
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
These compounds demonstrate significant neuroprotective effects by enhancing neuronal survival, maintaining neurite network integrity, and protecting astrocytes, offering potential therapeutic benefits for neurodegenerative diseases like Alzheimer's.
Implementation Method 1
it exhibits a pronounced antioxidant power, comparable to that of caffeic acid
Data Source
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AI summary
The invention relates to polysubstituted hexaric acids and the ester derivatives thereof, of general formula (I), wherein R1 and R2 are a hydrogen atom or an optionally substituted C1-C18 alkyl group, and Q1, Q2, Q3 and Q4 are a caffeoyl group, a CH3-CH(OH)-CH2-CO- group or a hydrogen atom, provided that at least one of these radicals is a caffeoyl group, for use in preventing and/or treating a neurodegenerative disease, in particular Alzheimer's disease. The invention also relates to compounds of formula (I) as such, such compounds to be used as a medicament, in particular for preventing and/or treating a neurodegenerative disease such as Alzheimer's disease, and a pharmaceutical or nutraceutical composition comprising at least one of these compounds.