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Semi-synthetic salinomycin analogs exert cytotoxic activity against human colorectal cancer stem cells

Klose, Johannes; Kattner, Sarah; Borgström, Björn LU ; Volz, Claudia; Schmidt, Thomas; Schneider, Martin; Oredsson, Stina LU ; Strand, Daniel LU and Ulrich, Alexis (2018) In Biochemical and Biophysical Research Communications 495(1). p.53-59
Abstract

Salinomycin, a polyether antibiotic, is a well-known inhibitor of human cancer stem cells. Chemical modification of the allylic C20 hydroxyl of salinomycin has enabled access to synthetic analogs that display increased cytotoxic activity compared to the native structure. The aim of this study was to investigate the activity of a cohort of C20-O-acyl analogs of salinomycin on human colorectal cancer cell lines in vitro. Two human colorectal cancer cell lines (SW480 and SW620) were exposed to three C20-O-acylated analogs and salinomycin. The impact of salinomycin and its analogs on tumor cell number, migration, cell death, and cancer stem cell specifity was analyzed. Exposure of human colorectal cancer cells to the C20-O-acylated analogs... (More)

Salinomycin, a polyether antibiotic, is a well-known inhibitor of human cancer stem cells. Chemical modification of the allylic C20 hydroxyl of salinomycin has enabled access to synthetic analogs that display increased cytotoxic activity compared to the native structure. The aim of this study was to investigate the activity of a cohort of C20-O-acyl analogs of salinomycin on human colorectal cancer cell lines in vitro. Two human colorectal cancer cell lines (SW480 and SW620) were exposed to three C20-O-acylated analogs and salinomycin. The impact of salinomycin and its analogs on tumor cell number, migration, cell death, and cancer stem cell specifity was analyzed. Exposure of human colorectal cancer cells to the C20-O-acylated analogs of salinomycin resulted in reduced tumor cell number and impaired tumor cell migration at lower concentrations than salinomycin. When used at higher (micromolar) concentrations, these effects were accompanied by induction of apoptotic cell death. Salinomycin analogs further expose improved activity against cancer stem cells compared to salinomycin.

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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
Apoptosis, Cancer stem cells, Colorectal cancer, Salinomycin, Salinomycin analogs
in
Biochemical and Biophysical Research Communications
volume
495
issue
1
pages
53 - 59
publisher
Elsevier
external identifiers
  • scopus:85032806820
ISSN
0006-291X
DOI
10.1016/j.bbrc.2017.10.147
language
English
LU publication?
yes
id
6aaae7db-8c4e-4ca2-bb4c-7832f45914cc
date added to LUP
2017-11-15 09:24:03
date last changed
2018-02-19 02:53:36
@article{6aaae7db-8c4e-4ca2-bb4c-7832f45914cc,
  abstract     = {<p>Salinomycin, a polyether antibiotic, is a well-known inhibitor of human cancer stem cells. Chemical modification of the allylic C20 hydroxyl of salinomycin has enabled access to synthetic analogs that display increased cytotoxic activity compared to the native structure. The aim of this study was to investigate the activity of a cohort of C20-O-acyl analogs of salinomycin on human colorectal cancer cell lines in vitro. Two human colorectal cancer cell lines (SW480 and SW620) were exposed to three C20-O-acylated analogs and salinomycin. The impact of salinomycin and its analogs on tumor cell number, migration, cell death, and cancer stem cell specifity was analyzed. Exposure of human colorectal cancer cells to the C20-O-acylated analogs of salinomycin resulted in reduced tumor cell number and impaired tumor cell migration at lower concentrations than salinomycin. When used at higher (micromolar) concentrations, these effects were accompanied by induction of apoptotic cell death. Salinomycin analogs further expose improved activity against cancer stem cells compared to salinomycin.</p>},
  author       = {Klose, Johannes and Kattner, Sarah and Borgström, Björn and Volz, Claudia and Schmidt, Thomas and Schneider, Martin and Oredsson, Stina and Strand, Daniel and Ulrich, Alexis},
  issn         = {0006-291X},
  keyword      = {Apoptosis,Cancer stem cells,Colorectal cancer,Salinomycin,Salinomycin analogs},
  language     = {eng},
  number       = {1},
  pages        = {53--59},
  publisher    = {Elsevier},
  series       = {Biochemical and Biophysical Research Communications},
  title        = {Semi-synthetic salinomycin analogs exert cytotoxic activity against human colorectal cancer stem cells},
  url          = {http://dx.doi.org/10.1016/j.bbrc.2017.10.147},
  volume       = {495},
  year         = {2018},
}