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A trans-platinum(II) complex induces apoptosis in cancer stem cells of breast cancer.

Abstract：

:Recent accumulating evidence has supported the notion that tumors have hierarchically organized heterogeneous cell populations and a small subpopulation of cells, termed cancer stem cells (CSCs), are responsible for tumor initiation, maintenance as well as drug resistance. Therefore, targeting the CSCs along with the other cancer cells has been the most important topic during the last decade. In the present study, we evaluated the cytotoxic activity of trans-[PtCl2(2-hepy)2] [2-hepy=2-(2-hydroxyethyl) pyridine] complex and the mechanism of cell death in breast CSCs. Stemness markers, Oct-4 and Sox2, were determined in mammospheres by western blotting. Cytotoxicity was assessed using the ATP viability assay. Cell death was fluorescently visualized and further confirmed by flow cytometry as well as gene expression analysis. The Pt(II) complex significantly reduced the cell viability, prevented mammosphere formation and disrupted mammosphere structures in a dose-dependent manner (0-100μM). The mode of cell death was apoptosis and it was shown by the presence of caspase 3/7 activity, Annexin V-FITC positivity, decreased mitochondrial membrane potential and increased expressions of pro-apoptotic genes (TNFRSF10A and HRK). Interestingly, necroptosis was also observed by the evidence of increased MLKL expression. In conclusion, the Pt(II) complex seems to be a highly promising anticancer compound due to its promising cytotoxic activity on CSCs. Therefore, it deserves in vivo further studies for the proof-of-concept.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Aztopal N,Karakas D,Cevatemre B,Ari F,Icsel C,Daidone MG,Ulukaya E

doi

10.1016/j.bmc.2016.10.032

subject

Has Abstract

pub_date

2017-01-01 00:00:00

pages

269-276

issue

1

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)31077-X

journal_volume

25

pub_type

杂志文章

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