Liquiritigenin is a plant-derived highly selective estrogen receptor @b agonist
Mol Cell Endocrinol 283(1-2):9 (2008) PMID 18177995 PMCID 2277338
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 ER@b-selective estrogens. We previously reported that an extract containing 22 herbs, MF101 has ER@b-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 ER@b but not ER@a. The ER@b-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 ER@b.
DOI: 10.1016/j.mce.2007.11.020Version: za2963e q8za4 q8zb4 q8zc2 q8zdd q8ze2 q8zf2 q8zg1
