中文名 | 變棉子酚 |
英文名 | apogossypol |
别名 | 變棉子酚 变棉子酚 阿朴棉子酚 化合物 T13459 |
英文别名 | NSC736630 apogossypol APOGOSSYPOL (+)-APOGOSSYPOL (+)-3,3'-Dimethyl-5,5'-bis(1-methylethyl)-2,2'-binaphthalene-1,1',6,6',7,7'-hexol [2,2'-Binaphthalene]-1,1',6,6',7,7'-hexol, 3,3'-dimethyl-5,5'-bis(1-methylethyl)-, (2S)- 3-methyl-5-propan-2-yl-2-(1,6,7-trihydroxy-3-methyl-5-propan-2-ylnaphthalen-2-yl)naphthalene-1,6,7-triol |
CAS | 66389-74-0 |
化学式 | C28H30O6 |
分子量 | 462.53 |
密度 | 1.335±0.06 g/cm3(Predicted) |
熔点 | 118-123 °C |
沸点 | 673.3±50.0 °C(Predicted) |
酸度系数 | 8.03±0.50(Predicted) |
体外研究 | In agreement with NMR binding and fluorescence polarization assays (FPAs) data, (+)-Apogossypol displays potent binding affinity to Bcl-xL with K d values of 1.7 µM.To investigate the inhibitory effects of (+)-Apogossypol and Gossypol on LNCaP cell survival, the MTT assay is performed. The results demonstrate that (+)-Apogossypol inhibits the proliferation of LNCaP cells in a time- and dose-dependent manner, in a similar way with Gossypol. The concentration for 50% inhibition (IC 50 ) on LNCaP cells within ~72 h is 9.57 μM, while the IC 50 of Gossypol on LNCaP cells is 10.35 μM. |
体内研究 | Due to its modified structure, (+)-Apogossypol is expected to exhibit lower toxicity while maintaining the significant anti-growth and anti-tumor activities in vitro, similar to those of Gossypol. The anti-cancer effect of (+)-Apogossypol is evaluated in mice bearing subcutaneous LNCaP cell xenografts. The tumor growth is monitored and measured by a caliper and balance. The survival rate of the mice is notably improved by (+)-Apogossypol. Of note, the tumor sizes are also markedly decreased by (+)-Apogossypol treatment (P<0.01). |