"目录号: HY-14596
Protein Tyrosine Kinase/RTKJAK/STAT SignalingAutophagy-
Genistein 是一种有效的蛋白酪氨酸激酶 (PTK) 抑制剂，抑制EGFR，IC50为 0.7 μg/mL (0.6 μM)。
EGFRAutophagy
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生物活性
Description
Genistein is a potent inhibitor of the protein tyrosine kinase (PTK) activity of theEGFRin vitro with anIC50of 0.7 μg/mL (0.6 μM).
IC50& Target
IC50: 0.7 μg/mL (0.6 μM) (EGFR)[1]
In Vitro
Genistein inhibits serum-stimulated growth of MCF-7 and T47D ER+cells with IC50values of 7.6 and 8.7 μg/mL by dye exclusion, respectively, and 8.7 and 10.6 μg/mL by [3H]thymidmne incorporation, respectively. These values are similar to the IC50values of 9.4 and 7 μg/mL for MCF-7 and T47D ER+cells, respectively, obtained with the MTT assay. Additionally, Genistein at concentrations up to 20 μg/mL does not alter MTT mitochondrial reduction when compared to control cells in an 8 h incubation period. Furthermore, neither biochanin A or daidzein are found to interfere with the MTT assay at IC50concentrations. Therefore, the MTT assay is valid for determining growth inhibition by Genistein at concentrations under 20 μg/mL in the systems studied[1].
In Vivo
In the present study, the effective dose of morphine caused a significant decrease in testis weight of mice compared to Saline group (p=0.00). Moreover, testis weight are significantly increase in treated animals with Genistein and Genistein plus morphine in all doses in comparison with morphine group (p=0.028). Morphine caused a significant decrease in the testosterone, LH and FSH hormones compared to saline group (p=0.00). In addition, the testosterone, LH and FSH hormones increased significantly in Genistein (p<0.05) and Genistein plus morphine in all groups administration compared to morphine group (p=0.024)[2]. Bisphenol A (BPA) treatment alone and combined with Genistein had no significant effect on the protein expression of LC3II and PPARα in liver of STD- or HFD-fed rats (P>0.05; P>0.05). Significant decreasing of the protein expression of PPARγ in liver is observed when Genistein is added to rats, compared to either HFD group or HFD-BPA group[3].
Clinical Trial
NCT01985763
Sofya Pintova-DSM Nutritional Products, Inc.-Icahn School of Medicine at Mount Sinai
Colon Cancer-Rectal Cancer-Colorectal Cancer
November 2013
Phase 1-Phase 2
NCT02499861
St. Justine's Hospital
Cancer
July 2015
Phase 1-Phase 2
NCT00882765
Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Pancreatic Cancer
May 2009
Phase 2
NCT02796794
TC Erciyes University
Sepsis
June 2015
Phase 4
NCT00769990
Masonic Cancer Center, University of Minnesota
Breast Cancer-Kidney Cancer-Lung Cancer-Melanoma-Metastatic Cancer-Pain-Prostate Cancer
September 2008
Phase 1-Phase 2
NCT01982578
Fundación para la Investigación del Hospital Clínico de Valencia-University of Valencia
Alzheimer's Disease
November 2013
NCT01126879
Northwestern University-National Cancer Institute (NCI)
Adenocarcinoma of the Prostate-Recurrent Prostate Cancer-Stage I Prostate Cancer-Stage II Prostate Cancer-Stage III Prostate Cancer
May 2010
Phase 2
NCT00541710
University of Messina-Ministry of Education, Universities and Research, Italy
Metabolic Syndrome
October 2007
Phase 2-Phase 3
NCT02766478
Emory University
Prostate Cancer
August 1, 2017
Phase 2
NCT01489813
Emory University
Bladder Cancer
May 19, 2017
Phase 2
NCT02624388
University of Virginia
Lymphoma-Childhood Lymphoma-Solid Tumor-Childhood Solid Tumor-Neuroblastoma-Ewing Sarcoma-Hodgkin Lymphoma-Non-Hodgkin Lymphoma-Rhabdomyosarcoma-Soft Tissue Sarcoma-Medulloblastoma-Germ Cell Tumor-Wilms Tumor-Brain Neoplasms-Medulloblastoma, Childhood-Neuroectodermal Tumors, Primitive
August 2016
Phase 2
NCT01325311
National Cancer Institute (NCI)
Prostate Adenocarcinoma-Stage I Prostate Cancer-Stage IIA Prostate Cancer-Stage IIB Prostate Cancer
December 2011
Phase 2
NCT00626769
University of Messina-Primus Pharmaceuticals
Menopause-Osteopenia
July 2005
Phase 2-Phase 3
NCT00276835
Northwestern University-National Cancer Institute (NCI)
Kidney Cancer-Melanoma (Skin)
November 2005
Early Phase 1
NCT00590538
Children's Hospital of Philadelphia-Cystic Fibrosis Foundation Therapeutics
Cystic Fibrosis
February 2003
Phase 1-Phase 2
NCT01628471
Uman Pharma-DSM Nutritional Products, Inc.-MDEIE Ministry, Québec Government-INRS-Institut Armand Frappier , Université du Québec
Non Small Cell Lung Cancer
November 2012
Phase 1-Phase 2
NCT00016744
Children's Hospital of Philadelphia-Cystic Fibrosis Foundation Therapeutics-National Center for Research Resources (NCRR)
Cystic Fibrosis
September 2001
Phase 1-Phase 2
NCT01664650
University of Messina-Ministry of Education, Universities and Research, Italy
Metabolic Syndrome
September 2008
Phase 2-Phase 3
NCT03040531
University of Messina-Ministry of Health, Italy
Osteoporosis, Steroid Induced
January 19, 2017
Phase 2-Phase 3
NCT00244933
Barbara Ann Karmanos Cancer Institute-National Cancer Institute (NCI)
Breast Cancer
February 2004
Phase 2
NCT01538316
University of Hohenheim-University Hospital Tuebingen-Quercegen Pharmaceuticals
Primary Prevention of Prostate Cancer
March 2012
NCT00099008
UNC Lineberger Comprehensive Cancer Center-National Cancer Institute (NCI)
Breast Cancer-Endometrial Cancer
March 2004
Phase 1
NCT00058266
Northwestern University-National Cancer Institute (NCI)
Prostate Cancer
December 2002
Phase 2
NCT00001696
National Cancer Institute (NCI)-National Institutes of Health Clinical Center (CC)
Cancer
April 1998
Phase 1
NCT00118040
National Cancer Institute (NCI)
Recurrent Bladder Cancer-Stage I Bladder Cancer-Stage II Bladder Cancer-Stage III Bladder Cancer
June 2005
Phase 2
NCT00005827
UNC Lineberger Comprehensive Cancer Center-National Cancer Institute (NCI)
Prostate Cancer
December 1999
Phase 1
NCT00546039
University Hospital, Aker
Prostatic Neoplasms
April 2007
Phase 2
NCT00290758
National Cancer Institute (NCI)
Breast Cancer
January 2006
Phase 2
NCT00584532
University of California, Davis
Prostate Cancer
November 2003
Phase 2-Phase 3
NCT00287690
Imperial College London
Coronary Artery Disease
October 1999
Phase 2-Phase 3
NCT00355953
University of Messina
Menopause-Osteopenia
January 2003
Phase 2-Phase 3
NCT00269555
University of California, Davis
Prostate Cancer
May 2004
NCT00951912
Sun Yat-sen University-Chinese Nutrition Society-Danone Institute International-Department of Health of Guangdong Province
Type 2 Diabetes Mellitus
August 2009
NCT00376948
Barbara Ann Karmanos Cancer Institute-National Cancer Institute (NCI)
Pancreatic Cancer
May 2005
Phase 2
NCT00244907
Purdue University-National Center for Complementary and Integrative Health (NCCIH)-Office of Dietary Supplements (ODS)
Osteoporosis-Osteopenia
January 2006
Phase 1
NCT00004858
Parker Hughes Cancer Center-National Cancer Institute (NCI)
Leukemia-Lymphoma
March 2000
Phase 1
NCT00000613
National Heart, Lung, and Blood Institute (NHLBI)
Bone Diseases-Cardiovascular Diseases-Coronary Disease-Depression-Heart Diseases-Myocardial Ischemia-Osteoporosis-Postmenopause
April 1997
Phase 2
NCT01556737
Wageningen University
Postmenopause
November 2011
NCT00499408
Wake Forest University Health Sciences-National Cancer Institute (NCI)
Prostate Cancer
April 2007
Phase 2
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References
[1].Peterson G, et al. Genistein inhibits both estrogen and growth factor-stimulated proliferation of human breast cancer cells. Cell Growth Differ. 1996 Oct;7(10):1345-51.
[2].Jalili C, 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.
[3].Ding S, et al. Environmentally Relevant Dose of Bisphenol A Does Not Affect Lipid Metabolism and Has No Synergetic or Antagonistic Effects on Genistein's Beneficial Roles on Lipid Metabolism. PLoS One. 2016 May 12;11(5):e0155352.