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

Citation
S. Tamir et al., Estrogen-like activity of glabrene and other constituents isolated from licorice root, J STEROID B, 78(3), 2001, pp. 291-298
Citations number
24
Categorie Soggetti
Biochemistry & Biophysics
Journal title
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
ISSN journal
09600760 → ACNP
Volume
78
Issue
3
Year of publication
2001
Pages
291 - 298
Database
ISI
SICI code
0960-0760(200109)78:3<291:EAOGAO>2.0.ZU;2-B
Abstract
Licorice root extract and its major isoflavan, glabridin, exhibited varying degrees of estrogen receptor (ER) agonism in different tissues in vitro an d in vivo. Animals fed with licorice extract, compared with estradiol and g labridin, showed an increase in creatine kinase (CK) activity, a known mark er for estrogen responsive genes, which was higher than expected from the l evels of glabridin in the extract. This led us to test for other components that may contribute to this strong estrogen agonist activity. Results indi cated that glabrene and isoliquiritigenin, (2 ' ,4 ' ,4-three hydroxy chalc one) (ILC) in the licorice extract can bind to the human ER with higher aff inity (IC50, 1 and 0.5 muM) than glabridin (IC50, 5 muM). The stimulatory e ffects of glabrene in vivo were tissue specific and similar to those of est radiol, The effect of increasing concentrations of glabrene and ILC on the growth of breast tumor cell were biphasic. Both showed an ER-dependent grow th-promoting effect at low concentrations (10 nM-10 muM), and ER-independen t antiproliferative activity at concentrations > 15 muM. This is the first study to indicate that glabrene, an isoflavene exerted varying degrees of E R agonism in different tissues. (C) 2001 Elsevier Science Ltd. All rights r eserved.