Receptor binding and transactivation activities of red clover isoflavones and their metabolites

Trifolium species-derived substances and extracts—Biological activity and prospects for medicinal applications

“…Forage plant; wound healing T. pratense L. (Red clover) Forage plant; expectorant, antiseptic, analgesic herb; treatment of sore throat, fever, pneumonia and meningitis; skin problems, lung illnesses as well as some disorders of nervous and reproductive system Estrogenic effect (Booth et al, 2006, Pfitscher et al, 2008, Nissan et al, 2007, Coon (2007 (Rev. ), Yatkin and Daglioglu, 2011, Adaikan et al, 2009, Lipovac et al (2010, Del Giorno et al, 2010;…”

“…It has been also found that all of these isoflavones (except formononetin) bind to one or both of estrogen receptors (a and b). Since isoflavones undergo various metabolic transformations after the dietary intake, the phytoestrogenic actions of their metabolites were also investigated (Pfitscher et al, 2008). The binding and transactivating properties of red clover isoflavones and their metabolites may be assessed by the analysis of estrogen receptors a and b, as well as androgen and progesterone receptors.…”

Soybean isoflavone exposure does not have feminizing effects on men: a critical examination of the clinical evidence

“…Isoflavones have a chemical structure similar to the hormone estrogen, bind to and transactivate estrogen receptors (ER) (53)(54)(55), and exert estrogen-like effects under certain experimental conditions in vitro and in vivo (56). Isoflavones have been classified by some as selective estrogen receptor modulators (mixed estrogen agonists/antagonists) (57)(58)(59), in part because of their preferential binding to and transactivation of ER-b compared with ER-a (54,60).…”

Trifolium pratense

“…Red clover extracts were reported to contain a variety of isofl avones, with affi nity towards oestrogen receptor alpha (ERalpha), oestrogen receptor beta (ERbeta), androgen receptor (AR) and progesterone receptor (PR) (Pfi tscher et al 2008 Mueller and Jungbauer ( 2008 ) found that red clover extracts and its major components, genistein and biochanin A, and especially several main metabolites exerted signifi cant PPAR-γ ligand binding and transactivational activity. 6-Hydroxydaidzein exerted a more than 100-fold higher binding affi nity than its precursor daidzein.…”