Oleacein Extraction in PEG for Pure Bioavailable Secoiridoids
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Solution Overview
Problem
Existing methods fail to produce pure and bioavailable forms of S-(E)-oleacein and S-(E)-oleomissional, and their active forms S-(E)-oleaceinediol and S-(E)-oleomissionadiol, which exhibit increased activity and solubility, in significant yields without chromatographic purification, and there is a lack of understanding of their therapeutic actions due to different functional groups reacting with water under varying conditions.
Innovation Solution
A method involving the use of polymeric hydrophilic alcohols like PEG200 or PEG400 to solubilize oleacein and oleomissional, converting them into their active forms oleaceinediol and oleomissionadiol, using specific enzymatic reactions and solvent extractions at controlled temperatures and pH, followed by filtration and evaporation to achieve high purity without chromatography.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Productivity
If conventional extraction methods are used to obtain oleacein and oleomissional, then the substances can be isolated from olive fruits or leaves, but the yields are low and chromatographic purification is required
Solution Approach 1:
The patent changes the chemical parameters of the extraction process by using specific solvent systems (aqueous alcohol solutions with controlled pH and temperature) to selectively extract the target compounds. By adjusting these parameters, the method achieves high yields without requiring chromatographic purification, as the extraction process itself becomes selective enough to provide pure compounds directly.
Solution Approach 2:
The patent employs selective extraction techniques where specific solvent systems are used to extract oleacein and oleomissional directly in pure form from olive fruits or leaves. The extraction process is designed to separate these compounds from other matrix components, eliminating the need for subsequent chromatographic purification steps while maintaining high yields.
2Reliability
If oleacein and oleomissional are used directly, then the substances are obtained from natural sources, but they require activation in the human body and have low water solubility
Solution Approach 1:
The patent performs preliminary chemical modification by converting oleacein and oleomissional into their corresponding diol forms (oleaceinediol and oleomissionadiol) during the extraction process itself. This preliminary action transforms the compounds into their bioavailable active forms with enhanced water solubility, eliminating the need for subsequent activation in the human body and improving bioavailability directly at the source.
3Reliability
If existing methods are used to produce active forms oleaceinediol and oleomissionadiol, then the bioavailable forms can be obtained, but the yields are very low and mixtures with non-utilizable substances are produced
Solution Approach 1:
The patent optimizes the extraction parameters (solvent composition, pH, temperature, time) to selectively produce the active diol forms of oleacein and oleomissional in high yields. By carefully controlling these parameters, the method achieves both high bioavailability and high productivity, obtaining pure active forms without mixtures of non-utilizable substances.
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 method produces pure and stable solutions of oleaceinediol and oleomissionadiol, enabling effective therapeutic applications such as cancer treatment, inflammation reduction, and antioxidant properties, with yields up to 2% and 95% purity, suitable for pharmaceutical preparations and nutritional supplements.
Implementation Method 1
substances (1), (2), when they come into contact with human biological fluids, they react chemically with water at a relatively slow rate, different for each substance, and are gradually converted to the active forms of 5S-(E)-oleaceinediol (3), 5S-(E)-oleomissionadiol (4)
Implementation Method 2
followed by filtration and evaporation to achieve high purity without chromatography
Implementation Method 3
followed by filtration and evaporation to achieve high purity without chromatography
Data Source
AI summary
The present invention relates to a method for obtaining in pure form or in a mixture the oleacein and oleomissional substances from olive fruits and leaves and certain derivatives thereof, the bioactive diol forms, by selective extraction of specially selected leaves or fruits with water or organic solvents. It also relates to pharmaceutical preparations containing the above substances in various combinations and the therapeutic properties of these preparations for the treatment of cancer, degenerative diseases of the central nervous system, diabetes, hyperlipidemia, inflammatory diseases and the prevention of creation of atherosclerotic plaques and thrombi.