Tectoridin from Maackia amurensis modulates both estrogen and thyroid receptors

• Published in: Phytomedicine (Stuttgart) 2014-04, Vol.21 (5), p.602-606
• Main Authors: Shim, Myeongkuk, Bae, Ji-Yeong, Lee, Young Joo, Ahn, Mi-Jeong
• Format: Article
• Language: English
• Subjects: Animals; Cell Proliferation - drug effects; Drug Evaluation, Preclinical; Estrogen; Estrogen receptor; Estrogen Receptor alpha - metabolism; Estrogen Receptor Modulators - isolation & purification; Health aspects; Humans; Isoflavones - isolation & purification; Isoflavones - pharmacology; Maackia - chemistry; Maackia amurensis; Materia medica, Vegetable; MCF-7 Cells; Medicinal plants; Pharmacology, Experimental; Physiological aspects; Plant Bark - chemistry; Plant extracts; Plant Extracts - chemistry; Plant Extracts - pharmacology; Plants, Medicinal; Rats; Receptors, Thyroid Hormone - agonists; Tectoridin; Thyroid hormones; Thyroid receptor; Transcriptional Activation - drug effects
• ISSN: 0944-7113; 1618-095X
• DOI: 10.1016/j.phymed.2013.10.022

The stem bark of Maackia amurensis has been used as folk medicine for the treatment of cancer, cholecystitis, arthritis, and hyperthyroidism in females. In this study we examined the effects of the ethyl acetate fraction obtained from the 70% ethanol extract of M. amurensis and tectoridin, an active constituent isolated from the ethyl acetate fraction on thyroid and estrogen hormone activity. The effect of the ethanolic extract of M. amurensis stem bark on thyroid hormone activity was evaluated using thyroid hormone responsive-luciferase assay. We isolated tectoridin from the ethyl acetate fraction using a recrystallization method. T-screen assays were used to confirm thyroid hormone activity. The estrogenic activity of the ethyl acetate fraction of M. amurensis and tectoridin was evaluated by estrogen responsive-luciferase assay and estrogen receptor alpha regulation as compared to 17β-estradiol. Both the ethyl acetate fraction and tectoridin activated thyroid-responsive reporters and increased thyroid hormone-dependent proliferation of rat pituitary GH3 cells, indicating modulation of thyroid hormone receptors. In parallel, the estrogenic activity of the fraction and tectoridin were characterized in a transient transfection system using estrogen-responsive luciferase plasmids in MCF-7 cells. The ethyl acetate fraction and tectoridin activated reporter gene expression and decreased the estrogen receptor protein level. These data indicate that tectoridin acts as a weak phytoestrogen as well as a thyroid hormone-like agent by activating both estrogen and thyroid hormone receptors.