Document Detail


Enniatin exerts p53-dependent cytostatic and p53-independent cytotoxic activities against human cancer cells.
MedLine Citation:
PMID:  17326668     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Worldwide, multiple Fusarium mycotoxins occur as contaminants of cereals with important impacts on human and animal health. The aim of this study was to investigate the effects of the widespread Fusarium secondary metabolite enniatin (ENN), a cyclic hexadepsipeptide, on human cell growth and survival. While short-term exposure (up to 8 h) to ENN at nanomolar concentrations slightly but significantly stimulated cell proliferation, it showed profound apoptosis-inducing effects especially against various human cancer cell types at low micromolar concentrations (already after 24 h of treatment). Several cellular changes indicative for programmed cell death such as cell shrinkage, chromatin condensation, DNA fragmentation, and apoptotic body formation were observed. Correspondingly, the cleavage of poly(ADP-ribosyl)polymerase and the activation of multiple caspases accompanied a distinct loss of mitochondrial membrane potential. To investigate the impact of apoptosis- and cell cycle-regulating proteins on ENN activity, HCT116 cells with homozygously disrupted p53, p21, or bax genes were analyzed. In vitality assays, no significant influences of these proteins on the anticancer activity of ENN were detectable. In contrast, 3H-thymidine incorporation revealed a significantly more efficient block of DNA synthesis in p53 wild-type as compared to knock-out cells. Accordingly, fluorescence-activated cell sorting analysis demonstrated a stronger ENN-induced cell cycle arrest in the G0/G1 phase. Profound ENN-mediated induction of p53 and the p53-downstream cell cycle inhibitor p21 were detectable in p53 wild-type cells by Western blotting. P53-independent p21 induction was also detectable at higher ENN concentrations in p53 (-/-) cells. In contrast, bax activation by ENN was independent of the cellular p53 status. In summary, our results suggest that short-term exposure to very low ENN concentrations, for example, via food intake, might have tumor-promoting functions based on growth stimulation. In contrast, elevated ENN concentrations exert profound p53-dependent cytostatic and p53-independent cytotoxic activities especially against human cancer cells, suggesting a potential quality of ENN as an anticancer drug.
Authors:
Rita Dornetshuber; Petra Heffeter; Majid-Reza Kamyar; Thomas Peterbauer; Walter Berger; Rosa Lemmens-Gruber
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Publication Detail:
Type:  Journal Article     Date:  2007-02-28
Journal Detail:
Title:  Chemical research in toxicology     Volume:  20     ISSN:  0893-228X     ISO Abbreviation:  Chem. Res. Toxicol.     Publication Date:  2007 Mar 
Date Detail:
Created Date:  2007-03-19     Completed Date:  2007-05-21     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8807448     Medline TA:  Chem Res Toxicol     Country:  United States    
Other Details:
Languages:  eng     Pagination:  465-73     Citation Subset:  IM    
Affiliation:
Department of Pharmacology and Toxicology, University of Vienna, Althanstrasse 14, Vienna, Austria.
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MeSH Terms
Descriptor/Qualifier:
Antineoplastic Agents*
Apoptosis / drug effects
Blotting, Western
Caspase 3 / metabolism
Caspase 7 / metabolism
Cell Cycle / drug effects
Cell Cycle Proteins / physiology
Cell Survival / drug effects
DNA Fragmentation / drug effects
Depsipeptides / pharmacology*
Fluorescein-5-isothiocyanate
Fluorescent Dyes
Humans
Indoles
KB Cells
Membrane Potentials / drug effects
Mitochondrial Membranes / drug effects
Phalloidine
Signal Transduction / drug effects
Thymidine / metabolism
Tumor Suppressor Protein p53 / genetics*,  physiology*
Chemical
Reg. No./Substance:
0/Antineoplastic Agents; 0/Cell Cycle Proteins; 0/Depsipeptides; 0/Fluorescent Dyes; 0/Indoles; 0/Tumor Suppressor Protein p53; 0/enniatins; 17466-45-4/Phalloidine; 3326-32-7/Fluorescein-5-isothiocyanate; 47165-04-8/DAPI; 50-89-5/Thymidine; EC 3.4.22.-/Caspase 3; EC 3.4.22.-/Caspase 7

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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