Estrogen-like activity of glabrene and other constituents isolated from licorice root.

Abstract	Licorice root extract and its major isoflavan, glabridin, exhibited varying degrees of estrogen receptor (ER) agonism in different tissues in vitro and in vivo. Animals fed with licorice extract, compared with estradiol and glabridin, showed an increase in creatine kinase (CK) activity, a known marker for estrogen responsive genes, which was higher than expected from the levels of glabridin in the extract. This led us to test for other components that may contribute to this strong estrogen agonist activity. Results indicated that glabrene and isoliquiritigenin, (2',4',4-three hydroxy chalcone) (ILC) in the licorice extract can bind to the human ER with higher affinity (IC50, 1 and 0.5 microM) than glabridin (IC50, 5 microM). The stimulatory effects of glabrene in vivo were tissue specific and similar to those of estradiol. The effect of increasing concentrations of glabrene and ILC on the growth of breast tumor cell were biphasic. Both showed an ER-dependent growth-promoting effect at low concentrations (10 nM-10 microM), and ER-independent antiproliferative activity at concentrations >15 microM. This is the first study to indicate that glabrene, an isoflavene exerted varying degrees of ER agonism in different tissues.
Authors	S Tamir, M Eizenberg, D Somjen, S Izrael, J Vaya
Journal	The Journal of steroid biochemistry and molecular biology (J Steroid Biochem Mol Biol) Vol. 78 Issue 3 Pg. 291-8 (Sep 2001) ISSN: 0960-0760 [Print] England
PMID	11595510 (Publication Type: Journal Article)
Chemical References	Estrogen Receptor Modulators Estrogens, Non-Steroidal Isoflavones Phenols Phytoestrogens Plant Preparations Receptors, Estrogen Tamoxifen Estradiol glabrene glabridin
Topics	Animals Breast Neoplasms (drug therapy, metabolism) Cell Division (drug effects) Estradiol (pharmacology) Estrogen Receptor Modulators (pharmacology) Estrogens, Non-Steroidal Female Glycyrrhiza (chemistry) HeLa Cells Humans Isoflavones Organ Specificity Phenols (isolation & purification, pharmacology) Phytoestrogens Phytotherapy Plant Preparations Rats Rats, Wistar Receptors, Estrogen (agonists) Tamoxifen (pharmacology) Transcription, Genetic (drug effects) Tumor Cells, Cultured

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