Abstract:
:Cardiac steroids are used to treat various diseases including congestive heart failure and cancer. The aim of this study was to investigate the anti-leukemic activity of UNBS1450, a hemi-synthetic cardenolide belonging to the cardiac steroid glycoside family. Here, we report that, at low nanomolar concentrations, UNBS1450 induces apoptotic cell death. Subsequently, we have investigated the molecular mechanisms leading to apoptosis activation. Our results show that UNBS1450 inhibits NF-κB transactivation and triggers apoptosis by cleavage of pro-caspases 8, 9 and 3/7, by decreasing expression of anti-apoptotic Mcl-1 and by recruitment of pro-apoptotic Bak and Bax protein eventually resulting in cell death.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Juncker T,Cerella C,Teiten MH,Morceau F,Schumacher M,Ghelfi J,Gaascht F,Schnekenburger M,Henry E,Dicato M,Diederich Mdoi
10.1016/j.bcp.2010.08.025subject
Has Abstractpub_date
2011-01-01 00:00:00pages
13-23issue
1eissn
0006-2952issn
1873-2968pii
S0006-2952(10)00656-8journal_volume
81pub_type
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