Liquiritigenin is a plant-derived highly selective estrogen receptor β agonist

Oxidative In Vitro Metabolism of Liquiritigenin, a Bioactive Compound Isolated from the Chinese Herbal Selective Estrogen β-Receptor Agonist MF101

Antidiabetic Actions of an Estrogen Receptor β Selective Agonist

The estrogen receptor β (ERβ) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERβ selective agonist WAY200070 as an insulinotropic molecule. We demonstrate that WAY200070 enhances glucose-stimulated insulin secretion both in mouse and human islets. In vivo experiments showed that a single administration of WAY...

Oxidative in vitro metabolism of liquiritigenin, a bioactive compound isolated from the Chinese herbal selective estrogen beta-receptor agonist MF101.

Liquiritigenin [2,3-dihydro-7-hydroxy-2-(4-hydroxyphenyl)-(S)-4H-1-benzopyran-4-one] is one of the major active compounds of MF101, an herbal extract currently in clinical trials for the treatment of hot flashes and night sweats in postmenopausal women. MF101 is a selective estrogen receptor beta agonist but does not activate the estrogen receptor alpha. Incubation with pooled human liver micro...

The effect of intrahippocampal injection of diarylpropionitrile, a selective estrogen receptor-beta agonist, on passive avoidance learning

Introduction: Neurohormones like testosterone and estradiol have an important role in learning and memory. The hippocampus is essentially involved in learning and memory, and is known to be a target for estradiol actions. Estrogen receptors (ERs) are highly expressed in CA1 of rat hippocampus, and mediate the effects of estrogen on learning and memory. Estradiol receptor belong to a family ...

Selective Estrogen Receptor β Agonist LY500307 as a Novel Therapeutic Agent for Glioblastoma

Glioblastomas (GBM), deadly brain tumors, have greater incidence in males than females. Epidemiological evidence supports a tumor suppressive role of estrogen; however, estrogen as a potential therapy for GBM is limited due to safety concerns. Since GBM express ERβ, a second receptor for estrogen, targeting ERβ with a selective agonist may be a potential novel GBM therapy. In the present study,...