Genistein: Natural Source and Pharmacological Effect

Genistein is a natural compound found in soy foods such as soybeans and beans. It is used to treat a variety of diseases and has anti-inflammatory, antioxidant and anticancer effects. Genistein can activate the Nrf2 cell signaling pathway and protect cells from oxidative stress and cytotoxicity. Genistein can stimulate telomere activity in prostate cancer cells and protect vascular smooth muscle cells at low concentrations (1-10μM).

Figure 1. Genistein

Physicochemical properties

Genistein is a heterocyclic diphenol containing three hydroxyl groups, with the chemical name 4′,5,7-trihydroxyisoflavone or 5,7-dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one. It has low solubility in water but high solubility in methanol. The nonlinear pharmacokinetic behavior of genistein may be related to its poor solubility in water.

Anticancer effects

Genistein can upregulate the expression of multiple tumor suppressor genes, such as p16, p21 and p53, which are responsible for senescence response and cell cycle arrest. Genistein terminates telomerase function in breast, ovarian, brain, and prostate cancer cells at 50 μM concentration.

Effects on neurodegenerative diseases

Genistein affects tumorigenesis/carcinogenesis through epigenetic regulation. It reduces the risk of breast cancer and enhances DNA demethylation of the SF1 promoter in the endometrium. Genistein also reduces the hypermethylation level of the tumor suppressor gene CHD5 and promotes the expression of CHD5 and p53, thereby preventing neuroblastoma (NB) growth and tumor microangiogenesis.

Effects on Alzheimer's disease (AD)

Genistein has potent antioxidant properties, relieves oxidative stress, and rescues mitochondria by increasing glutathione reduction rate and reducing 8-oxo-20-deoxyguanine, an indicator of mitochondrial DNA damage.

Fighting aging and age-related diseases

Genistein has a multimodal mechanism of action with anticancer protective, antioxidant, anti-inflammatory, anti-amyloid β, and pro-autophagic properties. It could be a therapeutic approach to treat age-related diseases.

Neuroprotection against stroke

Genistein is a polyphenolic compound that belongs to the class of flavonoid compounds found in many plants, including legumes. In the human diet, genistein is found primarily in soybeans and soy products, such as tofu and soy milk. It exists as an aglycone, or more commonly bound to a sugar group. Genistein bound to glucose is called "genistein" and is the predominant form found in soy foods.

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