Aurora kinase inhibitor, ENMD-2076 on human acute myeloid leukemia cells in vitro
Observe the Aurora kinase inhibitor ENMD-2076 on human acute myeloid leukemia (AML) cell lines in vitro. Methods: Different concentrations of ENMD-2076 were acting on the logarithmic growth phase AML cells 24 h, 48 h, using the MTT assay of drugs on cell growth inhibition; application Hoechst staining to detect apoptosis rate, Western blot assay after drug treatment pathway and apoptosis-related protein Caspase change. Results: ENMD-2076 significantly inhibited AML cell line THP-1 and Kasumi-1 growth (P0.001), 24 h when THP-1 and Kasumi-1 half inhibitory concentrations were 9.32μmol / L and 7.23μmol / L. Hoechst staining confirmed that ENMD-2076 enables THP-1 cells apoptotic changes such as chromatin condensation. Western blot analysis confirmed that, ENMD-2076 can activate Caspase-3, Caspase-9, Caspase-8 and PARP, increased pro-apoptotic protein Bak, Bax, Bad and Bim, reduced anti-apoptotic protein Mcl-1 expression. Conclusion: Aurora kinase inhibitor ENMD-2076 could significantly inhibit human AML cell line THP-1 and Kasumi-1 proliferation and induce apoptosis, regulation of apoptotic proteins is one of the mechanisms.
Aurora kinase inhibitor, ENMD-2076 on human acute myeloid leukemia cells in vitro
ReplyDeleteObserve the Aurora kinase inhibitor ENMD-2076 on human acute myeloid leukemia (AML) cell lines in vitro. Methods: Different concentrations of ENMD-2076 were acting on the logarithmic growth phase AML cells 24 h, 48 h, using the MTT assay of drugs on cell growth inhibition; application Hoechst staining to detect apoptosis rate, Western blot assay after drug treatment pathway and apoptosis-related protein Caspase change. Results: ENMD-2076 significantly inhibited AML cell line THP-1 and Kasumi-1 growth (P0.001), 24 h when THP-1 and Kasumi-1 half inhibitory concentrations were 9.32μmol / L and 7.23μmol / L. Hoechst staining confirmed that ENMD-2076 enables THP-1 cells apoptotic changes such as chromatin condensation. Western blot analysis confirmed that, ENMD-2076 can activate Caspase-3, Caspase-9, Caspase-8 and PARP, increased pro-apoptotic protein Bak, Bax, Bad and Bim, reduced anti-apoptotic protein Mcl-1 expression. Conclusion: Aurora kinase inhibitor ENMD-2076 could significantly inhibit human AML cell line THP-1 and Kasumi-1 proliferation and induce apoptosis, regulation of apoptotic proteins is one of the mechanisms.
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