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Simultaneous Measurement of HDAC1 and HDAC6 Activity in HeLa Cells Using UHPLC-MS
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HDAC6 inhibitor WT161 performs anti-tumor effect on osteosarcoma and synergistically interacts with 5-FU
Jun Sun1,2, Wei Wu3, Xiaofeng Tang1
1Jiangxi Key Laboratory of Cancer Metastasis and Precision Treatment, Center Laboratory, The Third Affiliated Hospital of Nanchang University, Nanchang 330008, China.
Background:
WT161, as a selective HDAC6 inhibitor, has been shown to play anti-tumor effects on several kinds of cancers. The aim of the present study is to explore the roles of WT161 in osteosarcoma and its underlying mechanisms.
Methods:
The anti-proliferative effect of WT161 on osteosarcoma cells was examined using MTT assay and colony formation assay. Cell apoptosis was analyzed using flow cytometer. The synergistic effect was evaluated by isobologram analysis using CompuSyn software. The osteosarcoma xenograft models were established to evaluate the anti-proliferative effect of WT161 in vivo.
Results:
WT161 suppressed the cell growth and induced apoptosis of osteosarcoma cells in a dose- and time-dependent manner. Mechanistically, we found that WT161 treatment obviously increased the protein level of PTEN and decreased the phosphorylation level of protein kinase-B (AKT). More importantly, WT161 showed synergistic inhibition with 5-FU on osteosarcoma cells in vitro and in vivo.
Conclusions:
These results indicate that WT161 inhibits the growth of osteosarcoma through PTEN and has a synergistic efficiency with 5-FU.
Insights
WT161, an HDAC6 inhibitor, effectively reduces osteosarcoma growth and induces apoptosis. It works by increasing PTEN and decreasing AKT phosphorylation, showing synergistic effects with 5-FU.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- WT161 is a selective HDAC6 inhibitor with demonstrated anti-tumor activity in various cancers.
- Osteosarcoma remains a challenging malignancy requiring novel therapeutic strategies.
Purpose of the Study:
- To investigate the efficacy of WT161 in osteosarcoma.
- To elucidate the underlying molecular mechanisms of WT161's action in osteosarcoma.
Main Methods:
- Cell proliferation was assessed using MTT and colony formation assays.
- Apoptosis was analyzed via flow cytometry.
- In vivo anti-tumor effects were evaluated in osteosarcoma xenograft models.
Main Results:
- WT161 exhibited dose- and time-dependent suppression of osteosarcoma cell growth and induced apoptosis.
- WT161 increased PTEN protein levels and decreased AKT phosphorylation.
- Synergistic anti-cancer effects were observed when WT161 was combined with 5-FU in vitro and in vivo.
Conclusions:
- WT161 effectively inhibits osteosarcoma growth.
- The mechanism involves the PTEN/AKT pathway.
- WT161 demonstrates synergistic potential with 5-FU for osteosarcoma treatment.
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