金雀异黄酮

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]
in vivo: Genistein significantly decreased the blood levels of total cholesterol, triglycerides, homocysteine and visfatin compared with placebo, while blood adiponectin levels were increased [4]. Leucine and genistein significantly (p<0.05) reduced the number of fights and increased latency to fights in foot shock-induced aggression; it also decreased apomorphine (5mg/kg, i.p.) induced stereotyped behavior and apomorphine induced (10mg/kg, s.c.) locomotor activity when compared with the positive control group [5].
Clinical trial: Cholecalciferol and Genistein Before Surgery in Treating Patients With Early Stage Prostate Cancer. Phase 2