Therapeutic Potential of Genistein and its Derivatives as a Target for Anticancer Agents

Abstract

Genistein is a natural isoflavone and a phytoestrogen known to possess broad range of pharmacological properties specifically explored for anticancer effects. The compound is under clinical trials for different types of cancer treatment. Structural modification of genistein has been done to prepare analogs with improved anticancer potential and pharmaceutical properties. Also, novel formulations of genistein have been developed to further improve water solubility and bioavailability for better clinical effectiveness. In the present review, we have summarized the recent available literature on genistein anticancer effects along with mechanism of action and clinical trial studies, reported analogs and novel formulations developed for improving the anticancer efficacy of genistein during the period 2013–2022. Also, the structure activity relationship (SAR) study of reported genistein analogs is described. Further, articles published in this period showed that both genistein and its various derivatives exhibit promising potential for the development of effective chemotherapeutic agents against different types of cancer. Further, the present review will help the researchers in design and development of genistein formulation with desired drug profile.

A Comprehensive Review of Genistein’s Effects in Preclinical Models of Cervical Cancer

“…Genistein has a diphenol structure ( Figure 1 ) with the molecular formula C 15 H 10 O 5 and resembles human endogenous estrogen [ 14 , 16 ]. There is evidence that genistein has antioxidant [ 17 ], anti-inflammatory [ 18 ], antibacterial [ 19 ], antiviral [ 20 , 21 ], antidiabetic [ 22 , 23 ], neuroprotective [ 24 , 25 ], and anti-cancer [ 26 , 27 , 28 ] effects. Additionally, in male mice, genistein increased sperm motility and number, suggesting it has beneficial effects in the reproductive system [ 29 ].…”