Equol is a non-steroidal estrogen produced from the metabolism of the isoflavonoid phytoestrogen daidzen by human intestinal microflora.The estrogen receptor (ER) agonist activity of the naturally occurring (S)-enantiomer (EC50 = 85 and 65 nM for human ERα and ERβ, respectively) is similar to that of genistein but exceeds that of daidzein.(S)-Equol preferentially binds ERβ (Ki = 0.73 nM) and demonstrates approximately 9-fold lower affinity for ERα (Ki = 6.41 nM).(S)-equol is also a potent antagonist of dihydrotestosterone, which has important implications for prostate cancer and other androgen-mediated pathologies.
产品描述: (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
靶点: Human Endogenous Metabolite;EstrogenReceptor/ERR; Estrogen/progestogenReceptor; EndogenousMetabolite
体内研究:
(-)-(S)-Equol inhibits the tumor growth by 43.2% and 28.4% compared to the control on day 33, suggesting that the compound is not overtly toxic
参考文献:
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. Lu Z, et al. S-equol, a Secondary Metabolite of Natural Anticancer Isoflavone Daidzein, Inhibits Prostate Cancer Growth In Vitro and In Vivo, Though Activating the Akt/FOXO3a Pathway. Curr Cancer Drug Targets. 2016;16(5):455-65. 3. Horiuchi H, et al. S-equol nantioselectively activates cAMP-protein kinase A signaling and reduces alloxan-induced cell death in INS-1 pancreatic β-cells. J Nutr Sci Vitaminol (Tokyo). 2014;60(4):291-6.
溶解性: DMSO : 100 mg/mL (412.76 mM; Need ultrasonic and warming)