(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively[1]. (R)-Equol induces a dose-dependent inhibitory effect on the invasive capacity of MDA-MB-231 cells that is significant at the highest concentration tested (50 μM). Following 48-h exposure to (R)-Equol, invasion is reduced by 62% (p=0.009, versus untreated cells) with 50 μM (R)-Equol. Matrix metalloproteinase-2 (MMP-2) expression is significantly down-regulated following treatment with 50 μM (R)-Equol (p=0.035)[2].
Animals fed (R)-Equol have a significantly reduced number of palpable tumors over time when compare with Controls (P=0.002). Furthermore, the number of palpable tumors formed per rat in the (R)-Equol-fed group is significantly lower than that of rats treated with S-(-)equol (P=0.008). (R)-Equol-fed animals have 43% fewer tumors than the control group and this difference is highly statistically significant (P=0.004). The number of tumors/tumor-bearing animal is significantly lower in the animals fed (R)-Equol compare with Controls (3.3±0.4 versus 5.5±0.5, P=0.004). At necropsy, the mean (±SEM) tumor weight per animal for (R)-Equol fed rats (5.3±1.1 mg) is significantly reduced (P=0.04) when compare with Controls (9.9±1.4 mg). Feeding the (R)-Equol diet results in significantly increased tumor latency (P=0.003)[3].
References:
[1]. Setchell KD, et al. S-equol, a potent ligand for estrogen receptor beta, is the exclusive enantiomeric form of the soy isoflavone metabolite produced by human intestinal bacterial flora. Am J Clin Nutr. 2005 May;81(5):1072-9.
[2]. Magee PJ, et al. Daidzein, R-(+)equol and S-(-)equol inhibit the invasion of MDA-MB-231 breast cancer cells potentially via the down-regulation of matrix metalloproteinase-2. Eur J Nutr. 2014 Feb;53(1):345-50.
[3]. Brown NM, et al. The chemopreventive action of equol enantiomers in a chemically induced animal model of breast cancer. Carcinogenesis. 2010 May;31(5):886-93.