Liquiritigenin is a plant-derived highly selective estrogen receptor beta agonist.

Abstract

After the Women's Health Initiative found that the risks of hormone therapy outweighed the benefits, a need for alternative drugs to treat menopausal symptoms has emerged. We explored the possibility that botanical agents used in Traditional Chinese Medicine for menopausal symptoms contain ERbeta-selective estrogens. We previously reported that an extract containing 22 herbs, MF101 has ERbeta-selective properties. In this study we isolated liquiritigenin, the most active estrogenic compound from the root of Glycyrrhizae uralensis Fisch, which is one of the plants found in MF101. Liquiritigenin activated multiple ER regulatory elements and native target genes with ERbeta but not ERalpha. The ERbeta-selectivity of liquiritigenin was due to the selective recruitment of the coactivator steroid receptor coactivator-2 to target genes. In a mouse xenograph model, liquiritigenin did not stimulate uterine size or tumorigenesis of MCF-7 breast cancer cells. Our results demonstrate that some plants contain highly selective estrogens for ERbeta.

• Authors: Jennifer E Mersereau, Nitzan Levy, Richard E Staub, Scott Baggett, Tatjana Zogovic, Tetjana Zogric, Sylvia Chow, William A Ricke, Mary Tagliaferri, Isaac Cohen, Leonard F Bjeldanes, Dale C Leitman
• Journal: Molecular and cellular endocrinology (Mol Cell Endocrinol) Vol. 283 Issue 1-2 Pg. 49-57 (Feb 13 2008) ISSN: 0303-7207 [Print] Ireland
• PMID: 18177995 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)

Chemical References

• Estrogen Receptor alpha
• Estrogen Receptor beta
• Flavanones
• Nuclear Receptor Coactivator 2
• Selective Estrogen Receptor Modulators
• liquiritigenin

Topics

• Animals
• Breast Neoplasms (pathology)
• Cell Line, Tumor
• Cell Proliferation (drug effects)
• Estrogen Receptor alpha (metabolism)
• Estrogen Receptor beta (agonists)
• Female
• Flavanones (chemistry, pharmacology)
• Glycyrrhiza (metabolism)
• Humans
• Mice
• Mice, Nude
• Nuclear Receptor Coactivator 2 (metabolism)
• Selective Estrogen Receptor Modulators (pharmacology)
• Transcription, Genetic (drug effects)
• Transfection
• Uterus (cytology, drug effects)
• Xenograft Model Antitumor Assays