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Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity

  • Authors:
    • Vasilis P. Androutsopoulos
    • Demetrios A. Spandidos
  • View Affiliations / Copyright

    Affiliations: Laboratory of Clinical Virology, Medical School, University of Crete, Heraklion, Voutes 71003, Greece
    Copyright: © Androutsopoulos et al. This is an open access article distributed under the terms of Creative Commons Attribution License.
  • Pages: 3412-3418
    |
    Published online on: October 6, 2017
       https://doi.org/10.3892/or.2017.6015
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Abstract

Inhibition of histone deacetylase enzymes (HDACs) has been well documented as an attractive target for the development of chemotherapeutic drugs. The present study investigated the effects of two prototype hydroxamic acid HDAC inhibitors, namely Trichostatin A (TSA) and Belinostat (PXD‑101) and the benzamide Entinostat (MS‑275) in A2780 ovarian carcinoma and MCF7 breast adenocarcinoma cells. The three HDACi inhibited the proliferation of A2780 and MCF7 cells at comparable levels, below the µM range. Enzyme inhibition assays in a cell‑free system showed that TSA was the most potent inhibitor of total HDAC enzyme activity followed by PXD‑101 and MS‑275. Incubation of A2780 and MCF7 cells with the hydroxamates TSA and PXD‑101 for 24 h resulted in a dramatic increase of acetylated tubulin induction (up to 30‑fold for TSA). In contrast to acetylated tubulin, western blot analysis and flow cytometry indicated that the induction of acetylated histone H4 was considerably smaller. The benzamide MS‑275 exhibited nearly a 2‑fold induction of acetylated histone H4 and an even smaller induction of acetylated tubulin in A2780 and MCF7 cells. Taken together, these data suggest that although the three HDACi were equipotent in inhibiting proliferation of MCF7 and A2780 cells, only the benzamide MS‑275 did not induce acetylated tubulin expression, a marker of class IIb HDACs.
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Copy and paste a formatted citation
Spandidos Publications style
Androutsopoulos VP and Spandidos DA: Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity. Oncol Rep 38: 3412-3418, 2017.
APA
Androutsopoulos, V.P., & Spandidos, D.A. (2017). Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity. Oncology Reports, 38, 3412-3418. https://doi.org/10.3892/or.2017.6015
MLA
Androutsopoulos, V. P., Spandidos, D. A."Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity". Oncology Reports 38.6 (2017): 3412-3418.
Chicago
Androutsopoulos, V. P., Spandidos, D. A."Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity". Oncology Reports 38, no. 6 (2017): 3412-3418. https://doi.org/10.3892/or.2017.6015
Copy and paste a formatted citation
x
Spandidos Publications style
Androutsopoulos VP and Spandidos DA: Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity. Oncol Rep 38: 3412-3418, 2017.
APA
Androutsopoulos, V.P., & Spandidos, D.A. (2017). Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity. Oncology Reports, 38, 3412-3418. https://doi.org/10.3892/or.2017.6015
MLA
Androutsopoulos, V. P., Spandidos, D. A."Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity". Oncology Reports 38.6 (2017): 3412-3418.
Chicago
Androutsopoulos, V. P., Spandidos, D. A."Antiproliferative effects of TSA, PXD‑101 and MS‑275 in A2780 and MCF7 cells: Acetylated histone H4 and acetylated tubulin as markers for HDACi potency and selectivity". Oncology Reports 38, no. 6 (2017): 3412-3418. https://doi.org/10.3892/or.2017.6015
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