Phenoxodiol是合成genestein的类似物,激活线粒体Caspase系统,抑制XIAP,使癌细胞对fas介导的凋亡敏感。它在细胞周期的G1/S期诱导细胞周期阻滞,通过独立于p53的方式上调p21WAF1。它通过稳定可分裂复合物抑制DNA拓扑异构酶II,从而阻止DNA复制。
产品描述
Phenoxodiol activates the mitochondrial caspase system, inhibits X-linked inhibitor of apoptosis(XIAP), disrupts FLICE inhibitory protein(FLIP) expression, and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner. Phenoxodiol also inhibits DNA topoisomerase II.
体外活性
Phenoxodiol, at concentrations >or=1 microg/ml (4 microM), inhibited proliferation and reduced the viability of healthy donor-derived PBMC. In contrast, lower Phenoxodiol concentrations (0.05-0.5 microg/ml) augmented, upon 3-day incubation, peripheral blood mononuclear cells cytotoxicity. Experiments with purified CD56(+) lymphocytes revealed that Phenoxodiol enhanced the lytic function of natural killer cells by directly stimulating this lymphocytic subpopulation[3].
体内活性
Balb/C mice administered low-dose Phenoxodiol exhibited significantly reduced tumour growth rates and prolonged survival (in 40% of the animals) in a colon cancer model[3].
Cas No.
81267-65-4
分子式
C15H12O3
分子量
240.25
别名
Haginin E;脱氢雌马酚;Dehydroequol;Idronoxil
储存和溶解度
DMSO:50 mg/mL (208.12 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years