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Please use this identifier to cite or link to this item: http://repository.li.mahidol.ac.th/dspace/handle/123456789/43320
Title: Licorice root components in dietary supplements are selective estrogen receptor modulators with a spectrum of estrogenic and anti-estrogenic activities
Authors: Nittaya Boonmuen
Ping Gong
Zulfiqar Ali
Amar G. Chittiboyina
Ikhlas Khan
Daniel R. Doerge
William G. Helferich
Kathryn E. Carlson
Teresa Martin
Pawinee Piyachaturawat
John A. Katzenellenbogen
Benita S. Katzenellenbogen
University of Illinois at Urbana-Champaign
Mahidol University
University of Mississippi School of Pharmacy
National Center for Toxicological Research
Keywords: Biochemistry, Genetics and Molecular Biology;Chemistry
Issue Date: 1-Jan-2016
Citation: Steroids. Vol.105, (2016), 42-49
Abstract: © 2015 Published by Elsevier Inc. Licorice root extracts are often consumed as botanical dietary supplements by menopausal women as a natural alternative to pharmaceutical hormone replacement therapy. In addition to their components liquiritigenin (Liq) and isoliquiritigenin (Iso-Liq), known to have estrogenic activity, licorice root extracts also contain a number of other flavonoids, isoflavonoids, and chalcones. We have investigated the estrogenic activity of 7 of these components, obtained from an extract of Glycyrrhiza glabra powder, namely Glabridin (L1), Calycosin (L2), Methoxychalcone (L3), Vestitol (L4), Glyasperin C (L5), Glycycoumarin (L6), and Glicoricone (L7), and compared them with Liq, Iso-Liq, and estradiol (E2). All components, including Liq and Iso-Liq, have low binding affinity for estrogen receptors (ERs). Their potency and efficacy in stimulating the expression of estrogen-regulated genes reveal that Liq and Iso-Liq and L2, L3, L4, and L6 are estrogen agonists. Interestingly, L3 and L4 have an efficacy nearly equivalent to E2 but with a potency ca. 10,000-fold less. The other components, L1, L5 and L7, acted as partial estrogen antagonists. All agonist activities were reversed by the antiestrogen, ICI 182,780, or by knockdown of ERα with siRNA, indicating that they are ER dependent. In HepG2 hepatoma cells stably expressing ERα, only Liq, Iso-Liq, and L3 stimulated estrogen-regulated gene expression, and in all cases gene stimulation did not occur in HepG2 cells lacking ERα. Collectively, these findings classify the components of licorice root extracts as low potency, mixed ER agonists and antagonists, having a character akin to that of selective estrogen receptor modulators or SERMs.
URI: https://www.scopus.com/inward/record.uri?partnerID=HzOxMe3b&scp=84949818228&origin=inward
http://repository.li.mahidol.ac.th/dspace/handle/123456789/43320
ISSN: 18785867
0039128X
Appears in Collections:Scopus 2016-2017

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