Isoflavone-rich food and food supplements have gained increasing popularity also in the Western world. Their weak estrogenic effect has been considered as a potential risk, although all epidemiological studies and clinical trials show a significant cancer protection and decreased risk of cardiovascular diseases. In vitro data suggest that the concerted action of the isoflavones and their metabolites show antiproliferative behaviour, reduce angiogenesis, reduce tumor progression and exert antiinflammatory effects. For the evaluation of the biological effects, special emphasis has to be put on the concerted action between the isoflavones and their metabolites. For instance, while isolated genistein shows some growth promoting effect at low concentrations, the metabolite equol or soy extract show growth retardation as well as higher concentrations of genistein do. The isoflavones have multiple affinities to other members of the steroid hormone receptor superfamily. The beneficial effect on metabolic diseases and weight reduction by isoflavone consumption can be partly explained by its affinity for the PPAR family. In light of the in vitro experiments, together with the epidemiological observations and the clinical experience, isoflavones can be considered as safe compounds and their consumption as food and food supplements has to be promoted.