Genistein (DB01645): A Comprehensive Pharmacological and Therapeutic Monograph

Executive Summary

Genistein is a prominent, naturally occurring isoflavone, a class of organic compounds characterized by a distinctive chemical structure that allows them to interact with a wide array of biological systems.[1] Primarily derived from soybeans and soy-based food products, it has been the subject of extensive scientific investigation for its diverse and pleiotropic pharmacological properties.[3] At the core of its biological activity is a dual pharmacological identity. On one hand, Genistein functions as a Selective Estrogen Receptor Modulator (SERM), exhibiting a structural similarity to endogenous estrogen that allows it to bind to estrogen receptors, with a notable preference for the beta subtype (ERβ).[1] On the other hand, it acts as a broad-spectrum inhibitor of critical cellular enzymes, most notably protein tyrosine kinases (PTKs) and DNA topoisomerase II, which are fundamental to cell signaling, proliferation, and survival.[1]

This multifaceted mechanism of action underpins its investigation across a broad therapeutic landscape. Preclinical and clinical research has focused heavily on its potential role in the prevention and treatment of hormone-dependent cancers, particularly those of the breast and prostate, as well as in the management of postmenopausal conditions, including vasomotor symptoms and osteoporosis.[5] Emerging evidence also points to potential applications in improving cardiovascular health and offering neuroprotection against degenerative diseases.[6]