生物活性

• 描述ER (Estrogen Receptor) is the receptor of estrogens. ER is a nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription factors to mediate ERE-independent signaling^[3]. Equol is a metabolite produced in vivo from the soy phytoestrogen daidzein. Equol is a ligand for ER. According to a report, equol had 13 fold higher binding affinity preferential for ERβ than ERα, with Ki of 16 nM as detected by binding assays^[4]. Other data suggested that equol stimulated the growth of ER positive MCF-7 cells in a concentration-dependent manner when used between 10 nM to 10 μM^[5]. However, equol inhibited the growth of human prostate cancer LnCaP, DU145 and PC3 cells, with IC50s of 169 μM, 140 μM and 119 μM, as detected at 72h time point by MTT method. In PC3 cells, equol caused cell cycle arrest in the G2/M phase at the concentration of 150 μM and induced apoptosis at the concentration of 100 μM when incubated for 48h^[6]. In a PC3 xenograft model established in Balb/c nude mice, equol intragastricly administrated at the dose of 10 mg/kg daily for 33 days inhibited tumor growth by 43.2% as compared to control group^[7].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT02309801	Healthy	Phase 1	Completed	-	Spain ... more >> Parc de Salut Mar. Barcelona, Spain, 08003 Collapse <<
  NCT00765479	Prostate Cancer	Phase 2 Phase 3	Completed	-	United States, Illinois ... more >> University of Illinois Cancer Center Chicago, Illinois, United States, 60612-7243 Collapse <<
  NCT01116310	Postmenopausal Women With Mode... more >>rate Vasomotor Symptoms Collapse <<	Phase 4	Unknown	July 2012	Spain ... more >> Hospital Central de Asturias Withdrawn Asturias, Spain, H. Central de Asturias Hospital del Cruces Recruiting Barakaldo, Spain, 48903 Principal Investigator: José L. Neyro, Dr.          Assir CAP Sant Martí Withdrawn Barcelona, Spain, 08020 Hospital de la Santa Creu i Sant Pau Recruiting Barcelona, Spain, 08025 Principal Investigator: Misericordia Guinot, Dr.          USP Instituto Universitario Dexeus Active, not recruiting Barcelona, Spain, 08028 ASSIR CAP San Andreu Active, not recruiting Barcelona, Spain, 08030 Hospital Universitari Vall d'Hebrón Recruiting Barcelona, Spain, 08035 Principal Investigator: Francesc Baró, Dr.          Hospital Monteprincipe Recruiting Boadilla del Monte, Madrid, Spain, 28660 Principal Investigator: Manuel Marcos, Dr.          Hospital General de Ciudad Real Active, not recruiting Ciudad Real, Spain, 13005 Centro Diatros Recruiting Gavá (Barcelona), Spain, 08850 Principal Investigator: Rafael Sánchez Borrego, Dr.          Hospital Universitario de Guadalajara Recruiting Guadalajara, Spain, 19002 Principal Investigator: María J. Cancelo, Dr.          Consorci Sanitari d l´Anoia-H. de Igualada Recruiting Igualada, Barcelona, Spain, 08700 Principal Investigator: Ana R Pérez Aguado, Dr.          Centro de Estudios de Obstetricia y Ginecología Asociado Lugo Recruiting Lugo, Spain, 27002 Principal Investigator: Francisco Vázquez, Dr.          Gabinete Médico Velázquez Recruiting Madrid, Spain, 28001 Principal Investigator: Silvia González, Dr.          Instituto Palacios Recruiting Madrid, Spain, 28009 Principal Investigator: Santiago Palacios, Dr.          Hospital Mateu Orfila Withdrawn Mao, Spain, 07701 H. San Joan d'Alacant Recruiting San Juan, Alicante, Spain, 03550 Principal Investigator: Francisco Quereda, Dr.          Hospital Universitario La Fe Recruiting Valencia, Spain, 46009 Principal Investigator: Dolores Juliá, Dr.          Hospital Doctor Pesset Recruiting Valencia, Spain, 46017 Principal Investigator: Antonio Cano, Dr.          Hospital Miguel Servet Withdrawn Zaragoza, Spain, 50009 Collapse <<

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• 参考文献

• [1] Muthyala RS, Ju YH, et al. Equol, a natural estrogenic metabolite from soy isoflavones: convenient preparation and resolution of R- and S-equols and their differing binding and biological activity through estrogen receptors alpha and beta. Bioorg Med Chem. 2004 Mar 15;12(6):1559-67.

  [2] Setchell KD, Brown NM, et al. The clinical importance of the metabolite equol-a clue to the effectiveness of soy and its isoflavones. J Nutr. 2002 Dec;132(12):3577-84.

  [3] Saville B, Wormke M, Wang F, Nguyen T, Enmark E, Kuiper G, Gustafsson JA, Safe S. Ligand-, cell-, and estrogen receptor subtype (alpha/beta)-dependent activation at GC-rich (Sp1) promoter elements. J Biol Chem. 2000 Feb 25;275(8):5379-87.

  [4] Muthyala RS, Ju YH, Sheng S, Williams LD, Doerge DR, Katzenellenbogen BS, Helferich WG, Katzenellenbogen JA. Equol, a natural estrogenic metabolite from soy isoflavones: convenient preparation and resolution of R- and S-equols and their differing binding and biological activity through estrogen receptors alpha and beta. Bioorg Med Chem. 2004 Mar 15;12(6):1559-67.

  [5] Sathyamoorthy N, Wang TT. Differential effects of dietary phyto-oestrogens daidzein and equol on human breast cancer MCF-7 cells. Eur J Cancer. 1997 Dec;33(14):2384-9.

  [6] Lu Z, Zhou R, Kong Y, Wang J, Xia W, Guo J, Liu J, Sun H, Liu K, Yang J, Mi M, Xu H. 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.

  [7] Lu Z, Zhou R, Kong Y, Wang J, Xia W, Guo J, Liu J, Sun H, Liu K, Yang J, Mi M, Xu H. 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.

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