金雀異黃酮

英文名稱(chēng)：Genistein  
CAS號(hào)：446-72-0
分析標(biāo)準(zhǔn)品,≥98%  
分子式 C15H10O5 分子量270.24  

基本信息:

屬性  
密度  1.548
熔點(diǎn)   297-298°C
存貯條件   儲(chǔ)存溫度 -20°C
描述  
產(chǎn)品介紹   溶于乙醇和DMSO， 干冷處保存。
別名   金雀異黃酮 ;4',5,7-三羥基異黃酮,染料木黃酮, 染料木素;4',5,7-Trihydroxyisoflavone 5,7-Dihydroxy-3-(4-hydroxyphenyl)-4H-1-benzopyran-4-one
生化機(jī)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  
應(yīng)用   1、具有雌性激素及抗雌激素性質(zhì)
2、在體內(nèi)能抑制結(jié)腸癌、乳腺癌、皮膚癌、前列腺癌等  
3、對(duì)多種腫瘤細(xì)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?fù)洚愘?gòu)酶Ⅱ的活性  
7、可以預(yù)防絕經(jīng)后骨質(zhì)疏松  
8、具有誘發(fā)細(xì)胞程序性死亡、提高抗癌藥效、抑制血管生成等作用，是一種很有潛力的癌癥化學(xué)預(yù)防劑，其抗癌作用及機(jī)制具有廣泛的應(yīng)用前景。