More than 130 different compounds have been identified from over 16 species of the Epimedium genus of the Berberidaceae family. Eight of these species have been used in the Traditional Chinese Medicines (TCM) over centuries to treate a wide range of diseases. From in vitro and in vivo experimental data, and preliminary structure-activity relationship (SAR) analysis of the androgenic/anti-estrogenic and anti-oxidant activities of the icariin series of flavonoids and glycosides, the results appear to be consistent with those of known anti-estrogenic flavonoids, such as luteolin. Further QSAR analysis of the different active ingredients is now in progress and will be reported elsewhere. Our survey suggests the possibility of multiple targets and multiple mechanisms of action by Epimedium preparations and their purified compounds. These may serve as leads for further new drug development.