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Anticancer Metal Complexes: Synthesis and Cytotoxicity Evaluation by the MTT Assay
Published on: November 10, 2013
Cytotoxic Activity of a Unique Monomeric Heterogeneous Two-Coordinate Ligand Monovalent Gold Complex with Tiopronin
Naoyuki Sano1, Hironori Yoshino2, Yoshiaki Sato2
1Elm Occupational Health Sciences, LLC, 2-9-12, Shimosone, Kokuraminami, Kitakyushu, Fukuoka 800-0217, Japan.
Background:
The importance of the role of NF-κB is recognized in situations such as malignant transformation and metastasis of cancer, and it has been suggested that inhibiting this role can be one of the cancer treatment strategies. Gold preparations such as auranofin are known to have an indirect NF-κB inhibitory effect.
Objective:
We synthesized a novel gold complex [tiopronin monovalent gold-5-mercapto- 1-methyl tetrazole, abbreviated as TPN-Au(I)-MM4], with different physical properties and chemical structure from auranofin, and evaluated its cytotoxic activity and radiation sensitizing effect on human THP1 cells.
Methods:
The number of viable cells was counted by the trypan blue dye exclusion method. The cell death evaluation was performed by FITC-Annexin V+ and PI staining. In investigating the radiation sensitizing effect of TPN-Au(I)-MM4, this compound [10 or 25 μM] was added into the culture medium 1 h before X-ray irradiation.
Results:
In the cells treated with 25 μM TPN-Au(I)-MM4 for 72 h, a decrease in the proliferation of THP1 cells was observed [The relative values of viable cells in the control group and the 25 μM treatment group were approximately 6.8 and 4.2, respectively]. In the combination of 25 μM of the compound treatment and X-ray irradiation, an increase of approximately 3.0-fold was observed in 2 Gy irradiation and approximately 1.4-fold in 4 Gy irradiation as in comparison to the case of irradiation alone.
Conclusion:
These results suggest that TPN-Au(I)-MM4 reduces the proliferation of THP1 cells through the induction of cell death, and the combined use of TPN-Au(I)-MM4 and X-ray irradiation shows effective cytotoxicity against THP1 cells.
Insights
A novel gold complex, TPN-Au(I)-MM4, effectively reduced cancer cell proliferation and enhanced radiation therapy. This compound shows promise as a cancer treatment strategy by increasing cytotoxicity when combined with X-ray irradiation.
Area of Science:
- Oncology
- Pharmacology
- Radiotherapy
Background:
- Nuclear factor-kappa B (NF-κB) plays a crucial role in cancer malignant transformation and metastasis.
- Inhibiting NF-κB is a potential cancer treatment strategy.
- Gold compounds like auranofin exhibit indirect NF-κB inhibitory effects.
Purpose of the Study:
- Synthesize a novel gold complex, TPN-Au(I)-MM4, with distinct properties from auranofin.
- Evaluate the cytotoxic activity of TPN-Au(I)-MM4 on human THP1 cells.
- Assess the radiation sensitizing effect of TPN-Au(I)-MM4 in combination with X-ray irradiation.
Main Methods:
- Cell viability was assessed using the trypan blue dye exclusion method.
- Cell death was evaluated through FITC-Annexin V and PI staining.
- TPN-Au(I)-MM4 (10 or 25 μM) was administered 1 hour prior to X-ray irradiation to determine radiosensitizing effects.
Main Results:
- TPN-Au(I)-MM4 (25 μM) significantly decreased THP1 cell proliferation over 72 hours (viable cell ratio decreased from 6.8 to 4.2).
- Combining TPN-Au(I)-MM4 with X-ray irradiation increased cytotoxicity: a 3.0-fold increase with 2 Gy and a 1.4-fold increase with 4 Gy, compared to irradiation alone.
Conclusions:
- TPN-Au(I)-MM4 induces cell death, reducing THP1 cell proliferation.
- The combination of TPN-Au(I)-MM4 and X-ray irradiation demonstrates significant and effective cytotoxicity against THP1 cells.
- TPN-Au(I)-MM4 presents a potential therapeutic agent for cancer treatment, particularly in conjunction with radiotherapy.
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