Tocoflexol Derivatives for αTTP Binding and Bioavailability
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Solution Overview
Problem
Tocotrienols have lower bioavailability and do not bind efficiently to the αTTP receptor, limiting their effective delivery and biological activity compared to tocopherols.
Innovation Solution
Development of tocoflexol derivatives with a partially unsaturated hydrocarbon tail, allowing for enhanced flexibility and efficient binding to the αTTP receptor, thereby improving uptake and transport into the bloodstream.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If tocotrienols are used as dietary supplements, then beneficial health effects are achieved, but binding efficiency to αTTP receptor and bioavailability are reduced
Solution Approach 1:
The patent modifies the hydrocarbon tail parameters of tocotrienols by introducing specific double bond configurations (one to three double bonds at defined positions) and saturation patterns. These parameter changes in the molecular structure enable the derivatives to bind efficiently to the αTTP receptor while maintaining the beneficial health effects of tocotrienols, thereby resolving the contradiction between binding efficiency and bioavailability.
2Reliability
If tocopherols are used instead of tocotrienols, then efficient transport and longer half-life are achieved, but certain beneficial health effects are lost
Solution Approach 1:
The patent creates composite molecular structures that combine features of both tocopherols and tocotrienols. The tocoflexol derivatives incorporate the chroman head group common to both, with modified hydrocarbon tails that provide the flexibility and binding capability of tocotrienols while achieving the transport efficiency and stability characteristics of tocopherols through optimized saturation patterns and double bond configurations.
3Adaptability or versatility
If tocotrienols with unsaturated hydrocarbon tails are used, then certain health effects are achieved, but binding and uptake by αTTP receptor are less efficient
Solution Approach 1:
The patent applies local quality modifications to specific regions of the hydrocarbon tail. By introducing double bonds at particular positions (carbons 2-3, 4-5, or 6-7) and controlling saturation at other positions, the invention creates localized flexibility zones that enable receptor binding while maintaining overall structural integrity for efficient uptake. This localized modification approach allows the molecule to exhibit both the desired health effects and improved binding efficiency.
Data Source
AI summary
Tocol derivative compounds, compositions comprising these tocol derivatives and methods of using the tocol derivatives are provided herein. Specifically the tocol derivatives have a partially unsaturated hydrocarbon tail and are thus distinct from the tocopherols. The hydrocarbon tails do not have a trans carbon-carbon double bond in the second isoprene unit of the hydrocarbon tail and are distinct from the tocotrienols. The compounds are expected to allow improved interaction with the α-tocopherol transfer protein receptor than the tocotrienols and better bioactivity than the tocopherols.