Drug intelligence / Profile preview

Biochanin A

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Biochanin A is a naturally occurring O-methylated isoflavone found in red clover (Trifolium pratense), chickpea, soybean, alfalfa sprouts, and other legumes. It is classified as a phytoestrogen and has been studied for its anti-inflammatory, antioxidant, anti-cancer, neuroprotective, and metabolic modulatory properties[1][3][4][7]. Mechanistically, Biochanin A acts as a selective agonist at estrogen receptor beta (ER-β) with low activity at ER-α[5], modulates peroxisome proliferator-activated receptors (PPARα/γ)[1], inhibits inflammatory mediators via the ERK-MAPK/MSK1 cascade and TLR/TIRAP/MyD88 pathway[1], antagonizes the HER2/neu receptor tyrosine kinase and MAPK/ERK signaling in cancer cells[6][8], inhibits aromatase enzyme activity to decrease estrogen levels[6], binds to aryl hydrocarbon receptor (AhR)[5], and can inhibit topoisomerase II as well as DNA replication in cancer cells[8]. It also exhibits weak inhibition of fatty acid amide hydrolase. Biochanin A is under investigation for potential use in postmenopausal osteopenia (clinical trial NCT02174666)[2] and has shown preclinical efficacy against various cancers including breast, lung, colon, prostate, and pancreatic cancers[4][6].

Other names
BCA4'-methoxy-5,7-dihydroxyisoflavone
02

Targets

PPARG (Peroxisome proliferator-activated receptor gamma)NF-κBBACE1 (Beta-site APP-cleaving enzyme 1)CYP19A1 (Aromatase)PPARA (Peroxisome proliferator-activated receptor alpha)ESR2 (ERβ)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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