MF101: a multi-component botanical selective estrogen receptor beta modulator for the treatment of menopausal vasomotor symptoms

Leitman, Dale C.; Christians, Uwe

doi:10.1517/13543784.2012.685652

Cited by 10 publications

(9 citation statements)

References 72 publications

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“…MF101 is an oral, botanically derived extract that selectively regulates ERβ, and is demonstrated by both preclinical and clinical data for its therapeutic promise for treating postmenopausal vasomotor symptoms without increasing cancer risks (Grady et al, 2009; Leitman and Christians, 2012). Our own research has provided further support for the therapeutic potential of an ERβ-based therapy for the improvement of both physical and neurological health during menopause (Zhao et al, 2009; Zhao et al, 2011a).…”

Section: Erβ-targeted Therapeutics For Ad and Beyondmentioning

confidence: 99%

Estrogen receptor β in Alzheimer’s disease: From mechanisms to therapeutics

Zhao

Woody

Chhibber

2015

Ageing Research Reviews

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Alzheimer's disease (AD) disproportionally affects women and men. The female susceptibility for AD has been largely associated with the loss of ovarian sex hormones during menopause. This review examines current understanding of the role of estrogen receptor β (ERβ) in the regulation of neurological health and its implication in the development and intervention of AD. Since its discovery in 1996, research conducted over the last 15-20 years has documented a great deal of evidence indicating that ERβ plays a pivotal role in a broad spectrum of brain activities from development to aging. ERβ genetic polymorphisms have been associated with cognitive impairment and increased risk for AD predominantly in women. The role of ERβ in the intervention of AD has been demonstrated by the alteration of AD pathology in response to treatment with ERβ-selective modulators in transgenic models that display pronounced plaque and tangle histopathological presentations as well as learning and memory deficits. Future studies that explore the potential interactions between ERβ signaling and the genetic isoforms of human apolipoprotein E (APOE) in brain aging and development of AD-risk phenotype are critically needed. The current trend of lost-in-translation in AD drug development that has primarily been based on early-onset familial AD (FAD) models underscores the urgent need for novel models that recapitulate the etiology of late-onset sporadic AD (SAD), the most common form of AD representing more than 95% of the current human AD population. Combining the use of FAD-related models that generally have excellent face validity with SAD-related models that hold more reliable construct validity would together increase the predictive validity of preclinical findings for successful translation into humans.

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Section: Erβ-targeted Therapeutics For Ad and Beyondmentioning

confidence: 99%

Estrogen receptor β in Alzheimer’s disease: From mechanisms to therapeutics

Zhao

Woody

Chhibber

2015

Ageing Research Reviews

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“…Our results showing that CC7 potentiates E2 transcriptional activation of ERβ might be a useful property to further prevent the proliferative effects of estrogens. We previously showed that the ERβ-selective plant extract 28 , MF101, reduced hot flashes in postmenopausal women, 29,30 suggesting another possible indication for CC7. Our findings suggest that an ERα coligand/estrogen combination could potentially provide superior safety to the estrogen only and estrogen/progestin regimens, and might make the current estrogens in MHT safe for long-term therapy to prevent chronic diseases associated with menopause.…”

Section: Discussionmentioning

confidence: 95%

2’, 3’, 4’-trihydroxychalcone is an Estrogen Receptor Ligand Which Modulates the Activity of 17β-estradiol

Herber

Quirit

Firestone

et al. 2019

Preprint

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Menopausal hormone therapy (MHT) reduces the risk of osteoporosis, fractures, obesity and diabetes, but longterm MHT increases risk of other diseases. Safe long-term MHT that exploits its benefits and abrogates its adverse effects requires a new approach. Here we demonstrate that 2', 3', 4'-trihydroxychalcone (CC7) acts as an estrogen receptor alpha (ERα) ligand that may improve the safety profile of MHT. CC7 reprograms the actions of estradiol (E2) to regulate unique genes in bone-derived U2OS cells, with 824/1358 genes not regulated by E2. The proliferative action of E2 on human MCF-7 breast cancer cells and mouse uterus is blocked when combined with CC7. Thermostability and molecular dynamics simulation studies suggest that CC7 binds concurrently with E2 in the ERα ligand binding pocket to produce a unique coliganded conformation to modulate ERα. Compounds such as CC7 that act as coligands represent a new class of ERα reprograming drugs that potentially can be combined with existing estrogens to produce a safer MHT regimen for long-term therapy. RESULTS CC7 acts as an ER coagonist in U2OS cellsPreviously, we isolated the flavanone liquiritigenin from

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“…To assess liquiritigenin content, a previously validated HPLC method was adapted for LC/MS use (15). The analytical column used was a Chiralpak ® AD-RH (150mm  4.6mm i.d., 5 To quantify pinostrobin, a second LC/MS method was developed from a previously validated HPLC method (17). Separation was achieved using a Chiralpak ® AD-RH (150mm  4.6mm i.d., 5-µm particle size, Chiral Technologies Inc. West Chester, PA, USA).…”

Section: Analysis Methodsmentioning

confidence: 99%

“…Liquiritigenin (Figure 1) has recently been shown to be a highly selective estrogen receptor ß agonist (4). It is present in licorice species (Glycyrrhizae uralensis and Glycyrrhizae glabra) and has been identified as one of multiple active components in a proprietary botanical mixture called MF101 currently being tested in clinical trials for activity against menopausal vasomotor symptoms (5). Pinocembrin ( Figure 2) is present in the traditional medicinial plant Alpinia galangal and is notably recognized as the flavonoid of highest concentration in propolis, the resinous glue collected from plants by bees for use in hive building, and also a traditional medicine (6,7).…”

Section: Introductionmentioning

confidence: 99%

Quantification of Three Chiral Flavonoids with Reported Bioactivity in Selected Licensed Canadian Natural Health Products and US Marketed Dietary Supplements

Sayre

Davies

2013

J Pharm Pharm Sci

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Purpose. Research indicating potentially beneficial bioactivity of flavonoids has produced a market and demand for natural health products and dietary supplements containing flavonoids. Implementation of the Canadian natural health product (NHP) regulations in January of 2004 increased regulation and oversight of NHP manufacture and marketing leading many consumers and clinicians to assume a similar pathway of development and approval to over-the-counter or prescription drugs. Methods. Three stereospecific liquid chromatograph/mass spectrometry (LC/MS) methods were used to assess the flavonoids, liquiritigenin, pinocembrin, and pinostrobin, in selected Canadian licensed NHP’s and US marketed dietary supplements. Results. The present study quantifies bioactive flavonoids in these products and notes variability in flavonoid content. Conclusions. Efficacy and safety of NHP’s and dietary supplements should not be assumed due to differences in criteria for NHP licensure by Health Canada as well as variation of flavonoid content between manufacturers and products with similar indications for use. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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MF101: a multi-component botanical selective estrogen receptor beta modulator for the treatment of menopausal vasomotor symptoms

Abstract: Preclinical and clinical studies indicate that MF101, a selective estrogen receptor beta agonist, represents a new class of drugs that is safe and effective for treating HF and nighttime awakenings.

Cited by 10 publications

References 72 publications

Estrogen receptor β in Alzheimer’s disease: From mechanisms to therapeutics

Estrogen receptor β in Alzheimer’s disease: From mechanisms to therapeutics

2’, 3’, 4’-trihydroxychalcone is an Estrogen Receptor Ligand Which Modulates the Activity of 17β-estradiol

Quantification of Three Chiral Flavonoids with Reported Bioactivity in Selected Licensed Canadian Natural Health Products and US Marketed Dietary Supplements

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