生物活性

• 靶点	PTK IC50:12μM/19μM

• 描述Genistein is an isoflavone present in soy and is known to have multiple molecular effects, such as the inhibition of inflammation, promotion of apoptosis, and modulation of steroidal hormone receptors and metabolic pathways^[3]. Genistein is the natural isoflavone and a phytoestrogen with a broad range of pharmacological properties, such as tyrosine and topoisomerase inhibition. It also induces apoptosis and cell proliferation inhibition, differentiates cancer cells. Added health benefits include the reduction of osteoporosis by suppressing osteoclasts and lymphocyte functions, decreased the risk of cardiovascular attacks and relieved postmenopausal problems^[4]. Retardation of atherogenic activity and increasing the antioxidant defense of a cell has been attributed to genistein while as it has also been reported that genistein possesses suppressive effects on both the cell-mediated and humoral components of the adaptive immune system. In addition, genistein has its prominent role in preventing the DNA damage. Genistein confers a better protection to ischemic conditions thereby giving a significant cardioprotection^[5]. Gensitein possesses cancer related enzyme-inhibitory effect and substantially inhibits skin carcinogenesis and cutaneous aging induced by ultraviolet (UV) light in mice and photodamage in humans. The anticancer, anti-inflammatory, cardio-protective and enzyme-inhibitory effects of genistein might be related to their antioxidant activities^[6].
• 细胞研究
• Cell Data

  Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
  293T cells	-	Function assay	-	Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells, IC50=0.0013 μM	16219463
  3T3 cells	-	Cytotoxic assay	-	Cytotoxic effect on 3T3 cells, IC50=24 μM	8201603
  A431 cells	50 to 75 uM	Function assay	36 h	Cell cycle arrest in human A431 cells assessed as decrease in accumulation at G0/G1 phase at 50 to 75 uM after 36 hrs by propidium iodide staining-based flow cytometric analysis	24456004

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• 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
  NCT01036321	Prostate Cancer	Phase 2	Completed	-	United States, Florida ... more >> University of Florida & Shands Medical Center - Jacksonville Jacksonville, Florida, United States, 32209 H. Lee Moffitt Cancer Center and Research Institute Tampa, Florida, United States, 33612 James A. Haley VA Hospital Tampa, Florida, United States, 33612 Collapse <<
  NCT01036321	-	-	Completed	-	-
  NCT01232751	Postmenopause	Not Applicable	Completed	-	Netherlands ... more >> Wageningen University Wageningen, Gelderland, Netherlands, 6703 HD Collapse <<

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• 参考文献

• [1] Jalili C, Ahmadi S, et al. Effect of Genistein on reproductive parameter and serum nitric oxide levels in morphine-treated mice. Int J Reprod Biomed (Yazd). 2016 Feb;14(2):95-102.

  [2] Akiyama T, Ishida J, et al. Genistein, a specific inhibitor of tyrosine-specific protein kinases. J Biol Chem. 1987 Apr 25;262(12):5592-5.

  [3] Mukund V, Mukund D, Sharma V, Mannarapu M, Alam A. Genistein: Its role in metabolic diseases and cancer. Crit Rev Oncol Hematol. 2017 Nov;119:13-22

  [4] Jaiswal N, Akhtar J, Singh SP; Badruddeen, Ahsan F. An Overview on Genistein and its Various Formulations. Drug Res (Stuttg). 2019 Jun;69(6):305-313

  [5] Ganai AA, Farooqi H. Bioactivity of genistein: A review of in vitro and in vivo studies. Biomed Pharmacother. 2015 Dec;76:30-8

  [6] Rahman Mazumder MA, Hongsprabhas P. Genistein as antioxidant and antibrowning agents in in vivo and in vitro: A review. Biomed Pharmacother. 2016 Aug;82:379-92

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