Morus alba Extract Estrogen Receptor Modulation
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Solution Overview
Problem
Current estrogen replacement therapies, such as HRT with estradiol, have undesirable effects like increased breast cancer risk, and selective estrogen receptor modulators like tamoxifen and raloxifene have side effects like hot flushes and uterine cancer risks, necessitating the development of natural estrogenic compositions.
Innovation Solution
A plant extract composition from Morus alba L. is developed, which elicits an estrogenic effect by interacting with estrogen receptors, activating or repressing specific gene responses, providing an alternative to traditional hormone therapies.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If hormone replacement therapy with estradiol is used to treat osteoporosis and cardiovascular disease, then therapeutic effects are achieved, but breast cancer risk increases by 35%
Solution Approach 1:
The patent uses phytoestrogens from Morus alba as an intermediary substance that can bind to estrogen receptors and modulate estrogenic activity. These plant-derived compounds act as natural mediators between the need for estrogenic therapy and the risk of breast cancer, providing therapeutic benefits while potentially reducing harmful effects through selective receptor modulation.
Solution Approach 2:
The invention changes the chemical parameters of estrogenic compounds by using plant-derived phytoestrogens instead of synthetic estradiol. This parameter change involves using compounds with different molecular structures and binding affinities that may provide selective estrogenic activity in target tissues while reducing overall carcinogenic risk.
2Object-affected harmful factors
If selective estrogen receptor modulators like tamoxifen are used to reduce breast cancer risk, then breast cancer protection is achieved, but uterine cancer risk and hot flushes increase
Solution Approach 1:
The patent applies the local quality principle by using phytoestrogens that may exhibit tissue-selective estrogenic activity. Different plant compounds can bind to estrogen receptors in various tissues with different affinities and effects, potentially providing protection in breast tissue while having minimal or beneficial effects on uterine tissue, thus avoiding the harmful side effects of conventional SERMs.
3Productivity
If conventional extraction methods are used to obtain plant extracts, then extraction is achieved, but extraction efficiency and purity are insufficient
Solution Approach 1:
The patent employs composite extraction systems combining multiple solvents and advanced extraction technologies. By using combinations of solvents with different polarities and applying techniques like supercritical fluid extraction or ultrasonic assistance, the method achieves both high extraction efficiency and superior purity, overcoming the limitations of conventional single-solvent extraction methods.
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 Morus alba L. extract composition effectively activates estrogen response elements, represses tumor necrosis factor expression, and offers a natural, potentially safer alternative for treating conditions like breast cancer and osteoporosis, reducing the risk of side effects associated with traditional therapies.
Implementation Method 1
The invention also provides a method of eliciting an estrogenic effect in a subject. The method includes administering to a subject an estrogenically effective amount of the estrogenic Morus alba L. extract composition.
Implementation Method 2
The invention further provides a method of activating estrogen response element (ERE). The method includes contacting a cell, which has both a gene under control of an estrogen response element and an estrogen receptor, with an amount of the inventive Morus alba L. extract composition that is effective to activate the gene through interaction of the ER with the estrogen response element.
Data Source
AI summary
Extracts of various species of the Moraceae family have estrogenic properties. For example, aqueous and ethanolic extracts of Morus alba L. species possess estrogenic properties in both ERα+ and ERβ+ cells. These estrogenic effect include estrogen response element (ERE) stimulation as well as tumor necrosis factor (TNF) repression. Methods are provided for treating climacteric symptoms, breast and/or uterine cancer, and osteoporosis.