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Updated: May 4, 2026
Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
[Histone deacetylase inhibits the growth and migration of human osteosarcoma cells]
Zhao-liang Zhang1, Ai-hua Zhang1, Zhi-qiang Feng1
1Department of Surgery, Maternity & Child Health Hospital, Tai'an 271000, China.
Objective:
To explore the effects of histone deacetylase inhibitors (HDACIs) on human osteosarcoma in vitro and in vivo.
Methods:
HDACI suberoylanilide hydroxamic acid (SAHA) and sodium butyrate (SB) were employed to examine the effects on human osteosarcoma in vitro and in vivo. The in vitro effects of HDACI SAHA and SB were evaluated in SaOS2 and U2OS human osteosarcoma cell lines. Cell growth, cell cycle progression and histone acetylation were examined by methyl tolyl sulfide (MTS), flow cytometry and Western blot respectively.In addition, SAHA or SB was administered for 4 weeks in a murine xenograph model for assessing the in vitro effects.
Results:
MTS assay revealed that SAHA and SB significantly suppressed the growth of SaOS2 and U2OS cells in a concentration-dependent manner.Western blot analysis indicated that the levels of acetylated H3 increased after HDACI treatment.Flow cytometry showed that SAHA arrested the cell cycle in G1 and G2/M phase, while SB arrested the cell cycle in G2/M phase. The tumor growth of murine xenograph model with SaOS2 was inhibited by SAHA and SB compared with vehicle control.
Conclusion:
HDACI SAHA and SB significantly inhibit the growth of human osteosarcoma cells and induce cell cycle arrest. Meanwhile, the tumor inhibitory effects were also validated in a murine xenograft model.
Insights
Histone deacetylase inhibitors (HDACIs), such as SAHA and SB, effectively inhibit human osteosarcoma cell growth and induce cell cycle arrest. These findings were validated in a murine xenograft model, showing tumor growth inhibition.
Area of Science:
- Oncology
- Molecular Biology
- Epigenetics
Context:
- Osteosarcoma is a primary bone cancer with limited treatment options.
- Histone deacetylase inhibitors (HDACIs) are emerging as a therapeutic strategy.
- Understanding HDACI mechanisms in osteosarcoma is crucial for developing new treatments.
Purpose:
- To investigate the efficacy of HDACIs suberoylanilide hydroxamic acid (SAHA) and sodium butyrate (SB) against human osteosarcoma.
- To evaluate the in vitro and in vivo effects of SAHA and SB on osteosarcoma cell lines (SaOS2, U2OS) and a murine xenograft model.
Summary:
- SAHA and SB demonstrated significant, dose-dependent suppression of osteosarcoma cell proliferation.
- HDACI treatment led to increased histone acetylation (H3) and cell cycle arrest (G1/G2/M for SAHA, G2/M for SB).
- Both SAHA and SB significantly inhibited tumor growth in a murine xenograft model.
Impact:
- HDACIs show promise as a therapeutic approach for human osteosarcoma.
- The study provides evidence for the anti-cancer activity of SAHA and SB in osteosarcoma.
- Further research into HDACI-based therapies could lead to improved patient outcomes.
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