(-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2-10 μg/mL; 12-48 hours) treatment significantly reduces the viability of all cell lines in a dose- and time-dependent manner, whereas the effect is not significant in a control cell line K562 without constitutive NF-κB activity.
(-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1 and K562 cells) treatment significantly increases the Annexin V-positive cells in MT-1 and TL-Om1 cell lines.
(-)-DHMEQ (10 μg/mL; 4-16 hours; MT-1 cells) treatment down-regulates Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53, and up-regulates proapoptotic genes such as caspase-3, -8, and-9.
(-)-DHMEQ treatment increases cells in G0 /G1 phase in a time-dependent manner, demonstrating antiproliferative effects of (-)-DHMEQ.
(-)-DHMEQ binds to p65, cRel, RelB, and p50, but not to p52 at specific cysteine residues. (-)-DHMEQ inhibits not only DNA-binding of RelB, but also its interaction to importin. (-)-DHMEQ also induces instability of RelB.
Cell Proliferation Assay
Cell Line: |
TL-Om1, MT-1, KK-1, ST-1 and K562 cells |
Concentration: |
2 μg/mL, 5 μg/mL, 10 μg/mL |
Incubation Time: |
12 hours, 24 hours, 48 hours |
Result: |
Significantly reduced the viability of all cell lines in a dose- and time-dependent manner.
|
Apoptosis Analysis
Cell Line: |
TL-Om1, MT-1 and K562 cells |
Concentration: |
10 μg/mL |
Incubation Time: |
0 hours, 24 hours, 48 hours |
Result: |
Annexin V-positive cells were significantly increased after 24 to 48 hours.
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Western Blot Analysis
Cell Line: |
MT-1 cells |
Concentration: |
10 μg/mL |
Incubation Time: |
4 hours, 8 hours, 16 hours |
Result: |
Annexin V-positive cells were significantly increased after 24 to 48 hours.
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