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Updated: Jul 16, 2026
Intramucosal Inoculation of Squamous Cell Carcinoma Cells in Mice for Tumor Immune Profiling and Treatment Response Assessment
Published on: April 22, 2019
Antitumor effects of Nafamostat mesilate on head and neck squamous cell carcinoma
Yukiko Yamashita1, Yukari Ishiguro, Daisuke Sano
1Department of Biology and Function in the Head and Neck, Yokohama City University Graduate School of Medicine, 3-9 Fukuura, Kanazawa-ku, Yokohama 236-0004, Japan. t036048f@med.yokohama-cu.ac.jp
Objective:
Nafamostat mesilate (FUT-175), a synthetic serine protease inhibitor, has antitumor activities toward adenocarcinoma, e.g., colon cancer. However, its antitumor effects on other types of cancer have been less extensively studied. We investigated the biological activities of Nafamostat mesilate on cell proliferation, cell-invasive potential and growth factor production in head and neck squamous cell carcinoma (HNSCC).
Methods:
Two human HNSCC cell lines established in our department, YCU-L891 and -H891, and a human vulvar squamous cell carcinoma cell line, A431, were examined for the effect of Nafamostat mesilate. The effects on cell growth were evaluated using the MTT assay. The effects on the relative expression levels of mRNA were measured by quantitative RT-PCR. Cytokine secretion was analyzed by enzyme-linked immunosorbent assay.
Results:
Nafamostat mesilate inhibited the proliferation of two HNSCC cell lines, YCU-L891 and YCU-H891, and A431. In these cell lines, Nafamostat mesilate down-regulated both matrix metalloproteinase (MMP)-2 and -9. In addition, it reduced the productions of vascular endothelial growth factor (VEGF) and transforming growth factor beta1 (TGF-beta1) by the tumor cells.
Conclusion:
Our results suggest that Nafamostat mesilate has potential for use as a treatment against local growth, invasion and metastasis of squamous cell carcinoma.
Insights
Nafamostat mesilate effectively inhibited head and neck squamous cell carcinoma (HNSCC) growth and invasion. This serine protease inhibitor reduced tumor cell proliferation, matrix metalloproteinase (MMP) expression, and key growth factor production.
Area of Science:
- Oncology
- Biochemistry
- Molecular Biology
Background:
- Nafamostat mesilate (FUT-175), a serine protease inhibitor, demonstrates antitumor activity in adenocarcinoma.
- Its effects on head and neck squamous cell carcinoma (HNSCC) are less understood.
- Investigating FUT-175's impact on HNSCC is crucial for expanding its therapeutic potential.
Purpose of the Study:
- To evaluate the biological activities of Nafamostat mesilate on HNSCC.
- To assess its effects on cell proliferation, invasion, and growth factor production.
- To determine FUT-175's potential as an HNSCC treatment.
Main Methods:
- Utilized two human HNSCC cell lines (YCU-L891, YCU-H891) and one vulvar SCC line (A431).
- Assessed cell growth inhibition via MTT assay.
- Quantified mRNA expression of MMP-2, MMP-9, VEGF, and TGF-beta1 using RT-PCR.
- Measured cytokine secretion using ELISA.
Main Results:
- Nafamostat mesilate significantly inhibited proliferation in all tested squamous cell carcinoma lines.
- FUT-175 down-regulated matrix metalloproteinase (MMP)-2 and MMP-9 expression.
- It also reduced tumor cell production of vascular endothelial growth factor (VEGF) and transforming growth factor beta1 (TGF-beta1).
Conclusions:
- Nafamostat mesilate exhibits potential for treating HNSCC.
- It may serve as a therapeutic agent against local tumor growth, invasion, and metastasis.
- Further research into FUT-175 for squamous cell carcinoma is warranted.
