變棉子酚
變棉子酚 性质
| 熔点 | 118-123 °C |
|---|---|
| 沸点 | 673.3±50.0 °C(Predicted) |
| 密度 | 1.335±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | >16.2mg/mL，溶于 DMSO，温和加热 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 8.03±0.50(Predicted) |
變棉子酚 用途与合成方法
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Mcl-1 2.6 μM (EC 50 ) |
Bcl-2 2.8 μM (EC 50 ) |
Bcl-xL 3.69 μM (EC 50 ) |
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.
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).
