Genistein: An Integrative Overview of Its Mode of Action, Pharmacological Properties, and Health Benefits

Abstract

Genistein is an isoflavone first isolated from the brooming plant Dyer’s Genista tinctoria L. and is widely distributed in the Fabaceae family. As an isoflavone, mammalian genistein exerts estrogen-like functions. Several biological effects of genistein have been reported in preclinical studies, such as the antioxidant, anti-inflammatory, antibacterial, and antiviral activities, the effects of angiogenesis and estrogen, and the pharmacological activities on diabetes and lipid metabolism. The purpose of this review is to provide up-to-date evidence of preclinical pharmacological activities with mechanisms of action, bioavailability, and clinical evidence of genistein. The literature was researched using the most important keyword “genistein” from the PubMed, Science, and Google Scholar databases, and the taxonomy was validated using The Plant List. Data were also collected from specialized books and other online resources. The main positive effects of genistein refer to the protection against cardiovascular diseases and to the decrease of the incidence of some types of cancer, especially breast cancer. Although the mechanism of protection against cancer involves several aspects of genistein metabolism, the researchers attribute this effect to the similarity between the structure of soy genistein and that of estrogen. This structural similarity allows genistein to displace estrogen from cellular receptors, thus blocking their hormonal activity. The pharmacological activities resulting from the experimental studies of this review support the traditional uses of genistein, but in the future, further investigations are needed on the efficacy, safety, and use of nanotechnologies to increase bioavailability and therapeutic efficacy.

Effect of Dietary Polyphenols on Osteoarthritis—Molecular Mechanisms

“…Genistein, an isoflavone belonging to the sub-class of flavonoids, is one of the most studied isoflavones. This is due to its potent therapeutic properties in alleviating diseases such as diabetes, lipid metabolism, depression, neurodegeneration, bone health, and cardiovascular disease and is associated with its antioxidant, anti-inflammatory, anticancer, and cytotoxic activities [ 86 ].…”

Genistein: A Potent Anti-Breast Cancer Agent

“…In plants, the synthesis of genistein starts from a flavanone, naringenin, by the isoflavone synthase enzyme due to ring migration [1,3]. The structure of genistein (chemically, 4′,5,7-trihydroxyisoflavone (C15H10O5)) and estradiol have been observed to be similar [5]; hence, genistein has estrogenic activity and is a good example of a phyto-estrogenic substance.…”

“…Several in vitro and in vivo studies have attempted to understand and gain a better insight into the mechanisms underlying the biomedical properties of genistein [2][3][4]. The isoflavonoid has been analyzed and previously reviewed for its neoplastic potentials.…”

Hyssopus Essential Oil: An Update of Its Phytochemistry, Biological Activities, and Safety Profile

“…Natural products are a rich source of compounds with many applications in cancer chemotherapy [ 65 – 67 ]. Moreover, the broad spectrum of natural compounds provides important compounds for therapeutic refinement through molecular modifications [ 68 , 69 ].…”