金雀异黄酮

英文名称：Genistein  
CAS号：446-72-0
分析标准品,≥98%  
分子式 C15H10O5 分子量270.24  

基本信息:

属性  
密度  1.548
熔点   297-298°C
存贮条件   储存温度 -20°C
描述  
产品介绍   溶于乙醇和DMSO， 干冷处保存。
别名   金雀异黄酮 ;4',5,7-三羟基异黄酮,染料木黄酮, 染料木素;4',5,7-Trihydroxyisoflavone 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one
生化机理  
Description:  
IC50 Value: 37.5 uM( Topo II) [3]  
Genistein, a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM. It has been shown that genistein inhibits many type of cancers including prostate cancer (PCa) by regulating several cell signaling pathways and microRNAs (miRNAs).  
in vitro: GEN effectively reversed estrogenicity of BPA by reversing mRNA and protein expressions of ERα, IGF-1R, pIRS-1, and pAkt induced by BPA in cellular model and also significantly decreased tumor growth and in vivo expressions of ERα, pIRS-1, and pAkt in xenografted mouse model [1]. Interestingly, genistein and its analogs induced caspase 3-activation supporting apoptotic mechanism of cell death but SPG-G supported caspase 3-independent apoptosis [2]. Of the compounds tested, only genistein selectively inhibited human topo II activity and had an IC50 value of 37.5 M [3]  
Clinical trial: Cholecalciferol and Genistein Before Surgery in Treating Patients With Early Stage Prostate Cancer. Phase 2  
应用   1、具有雌性激素及抗雌激素性质
2、在体内能抑制结肠癌、乳腺癌、皮肤癌、前列腺癌等  
3、对多种肿瘤细胞株有抑制作用  
4、具有抗氧化作用  
5、可以抑制酪氨酸蛋白激酶（PTK）的活性  
6、可以抑制拓扑异购酶Ⅱ的活性  
7、可以预防绝经后骨质疏松  
8、具有诱发细胞程序性死亡、提高抗癌药效、抑制血管生成等作用，是一种很有潜力的癌症化学预防剂，其抗癌作用及机制具有广泛的应用前景。