Perspectives Regarding the Role of Biochanin A in Humans

Abstract

Biochanin A (BCA) is an isoflavone mainly found in red clover with poor solubility and oral absorption that is known to have various effects, including anti-inflammatory, estrogen-like, and glucose and lipid metabolism modulatory activity, as well as cancer preventive, neuroprotective, and drug interaction effects. BCA is already commercially available and is among the main ingredients in many types of supplements used to alleviate postmenopausal symptoms in women. The activity of BCA has not been adequately evaluated in humans. However, the results of many in vitro and in vivo studies investigating the potential health benefits of BCA are available, and the complex mechanisms by which BCA modulates transcription, apoptosis, metabolism, and immune responses have been revealed. Many efforts have been exerted to improve the poor bioavailability of BCA, and very promising results have been reported. This review focuses on the major effects of BCA and its possible molecular targets, potential uses, and limitations in health maintenance and treatment.

The Effects of Trifolium pratense L. Sprouts’ Phenolic Compounds on Cell Growth and Migration of MDA-MB-231, MCF-7 and HUVEC Cells

“…Fermented sprouts' extracts contained aglycones, in contrast to extracts of sprouts prior to fermentation, in which there were also glycosides poorly absorbed in the body. Methoxy derivatives, such as biochanin A, even as aglycones, may be poorly absorbed; however, the administration of isoflavones in the mixture contributes to an increase in bioavailability, potentially through increased enterohepatic circulation [31]. The extracts influenced biological activities of human breast cancer cell lines MDA-MB-231 and MCF-7 and exerted cytotoxicity against both cells types, whereas in case of ERα-positive MCF-7 cells, dosages below IC 0 revealed little estrogenic activity of stimulating cell growth.…”

“…One of them is reduction of catalytic activity of enzymes involved in ROS generation; i.e., cyclooxygenase (COX) [30]. Biochanin A is known as strong scavenger of ROS, activator of SOD (superoxide dismutase) enzyme activity and reducer of COX-2 expression [31]. However, there is growing evidence of polyphenols' reactions with nonpolar compounds present in the hydrophobic inner membrane layer [18,32,33].…”

“…Data perceived with crystal violet staining revealed that the migration inhibition did not result from cellular detachment from the substrate, or the change of cellular shape; instead CUFH even slightly enhanced the number of cells or contacts between cells ( Figure 5D). The adhesiveness and attachment of the cells is reciprocally correlated with increased membrane fluidity; thus, agents able to reduce membrane fluidity are potent antimetastatic drugs [31,37,39,40]. Cellular membrane stiffness induced by isoflavones seems to be partially involved in migration and invasiveness limitation.…”

Evaluation of Isoflavones as Bone Resorption Inhibitors upon Interactions with Receptor Activator of Nuclear Factor-κB Ligand (RANKL)

“…The pair of methoxy isoflavones may be a good candidate to develop preparations for use as osteoporosis therapeutics, showing that plant extract containing a complex mixture of few isoflavones may act as a very effective therapeutic in contrast to one isolated substance. Intake of biochanin A in foods is additionally supported by the fact that biochanin A blood level has been shown to be higher when consumed in the presence of other isoflavones [24]. Intake of isoflavones may be particularly beneficial in preventing osteoporosis when they are additionally accompanied by proteins of both plant and animal origin [25].…”

Growth and Osteogenic Differentiation of Discarded Gingiva-Derived Mesenchymal Stem Cells on a Commercial Scaffold

“…However, it was demonstrated that pure collagen materials don't have enough osteoinductive activity to stimulate bone formation and many strategies, based on scaffold incorporation with bioactive molecules or hMSC treatment with bioactive molecules, have been developed (Otsuka et al, 2013). Biochanin A (5,7-dihydroxy-4 -methoxy-isoflavone), an isoflavone most commonly found in legumes as red clover (Trifolium pratense), which acts as a natural modulator of the estrogen receptor (ER) α and ERβ, is able to enhance the transcriptional pathways physiologically activated by estrogens and inhibited during human pathological conditions, as osteoporosis in postmenopausal women (Joannou et al, 1995;Brynin, 2002;Setchell et al, 2002;Somjen et al, 2005;Yu et al, 2019). In particular, Biochanin A has been showed to enhance the osteoblastic differentiation pathway and inhibit the osteoclastic differentiation pathway (Su et al, 2013a,b), contributing to the maintenance of bone health (Booth et al, 2006;Thompson Coon et al, 2007).…”