Uses of aromatic nitrovinyl compounds
A technology for compounds and uses, applied in the directions of active ingredients of nitro compounds, medical preparations containing active ingredients, and drug combinations, etc.
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Embodiment 1
[0263] Example 1. Z-10 induces differentiation and apoptosis of APL cells
[0264] 1. NB4 cells (a kind of APL cells) were treated with DMSO, ATRA (1 μM), Arsenic (1 μM) or Z-10 (3 μM) for two days respectively, then labeled with anti-CD11b antibody, counted by flow cytometry, and the results were as follows figure 1 As shown in B, the red curve in the figure is the DMSO control group, and the green curve is the compound treatment group.
[0265] figure 1 B shows that compounds ATRA, Arsenic and Z-10 are all able to induce the differentiation of NB4 cells.
[0266] 2. NB4 cells were treated with ATRA (1 μM), Arsenic (1 μM) or Z-10 (1 μM, 2 μM or 3 μM) for 36 hours, then double-stained with Annexin V-FITC and Propidium iodide (PI), and analyzed by flow cytometry analysis, the result is figure 1 C shown.
[0267] figure 1 C shows:
[0268] (1) The ratios of early apoptotic cells and late apoptotic cells in DMSO group were 2.82% and 1.39%, respectively. And the proportion ...
Embodiment 2
[0275] Example 2. Z-10 can induce the cleavage and degradation of PML-RARα protein
[0276] 1. After NB4 cells were treated with Z-10 (5μM) for 2h, 4h or 8h, the cell lysate was collected and detected by western blot with anti-RARα antibody to determine the expression of PML-RARα. The results are shown in 2A.
[0277] figure 2 A shows that after NB4 cells were treated with Z-10, the band of PML-RARα became lighter as time went on, while the band of the cleaved fragment of PML-RARα became deeper. This shows that Z-10 can time-dependently induce the cleavage and degradation of PML-RARα.
[0278]2. After NB4 cells were treated with 2 μM, 4 μM or 8 μM Z-10 for 4 hours, the cell lysate was collected and detected by western blot with anti-RARα antibody to determine the expression of PML-RARα, the results are shown in 2B.
[0279] figure 2 B shows that after NB4 cells were treated with Z-10, the higher the concentration of Z-10, the lighter the band of PML-RARα, and the darker t...
Embodiment 3
[0289] Example 3. RXRα stabilizes PML-RARα, while Z-10 induces PML-RARα degradation by inhibiting the interaction between RXRα and PML-RARα
[0290] 1. Three days after NB4 cells were infected with shRXRα lentivirus, the expression of each protein was detected by western blot, the results are as follows image 3 As shown in A.
[0291] image 3 A shows that, compared with the control group, when the expression of RXRα in NB4 cells was inhibited by shRXRα, the expression levels of PML-RARα and RARα were significantly reduced. This shows that RXRα can stabilize PML-RARα.
[0292] 2. Transfect the expression plasmids of PML-RARα or PML-RARα and Myc-RXRα in Cos7 cells respectively, treat with Z-10 (5μM) for 4h after 24h, then collect the cell lysate and detect it with anti-Myc antibody co-immunoprecipitation The interaction of RXRα and PML-RARα was determined as image 3 Shown in B.
[0293] image 3 B shows that in the test group co-transfected with PML-RARα and Myc-RXRα, b...
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