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Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Design and biological evaluation of novel water-soluble complexes based on thiosemicarbazone as prospective
Sima Feizpour1, Seyed Abolfazl Hosseini-Yazdi2, Behzad Baradaran3
1Department of Inorganic Chemistry, Faculty of Chemistry, University of Tabriz, Tabriz, 51666-14766, Iran.
Abstract:
The widespread success of platinum-based drugs in the clinical treatment of different neoplasia has led the inorganic metal complexes to be at the forefront of the fight against cancer. In this context, thiosemicarbazones and their metal derivatives serve as promising starting points for developing anticancer agents. In current study, the new fluorescent thiosemicarbazone ligand L and its complexes with some non-toxic first row transition metals such as Mn(II), Fe(III), Ni(II), Cu(II), and Zn(II) metal ions were attained as LMn, LFe, LNi, LCu, and LZn complexes. The molecular structures of the compounds were proved by chemico-physico techniques. The anti-proliferative activity of these compounds has been evaluated on human liposarcoma (SW-872) and human breast adenocarcinoma (MCF-7) using the MTT assay. The morphology of cell death and cell cycle studied in SW-872 cancerous cells was performed via flow cytometry. Eventually, imaging of treated cancerous cells with LMn and LZn complexes was performed by fluorescence microscopy. Compounds were designed in order to achieve a hydrophilic/lipophilic balance and synthesized through a condensation reaction. All compounds revealed high solubility in water and remained stable for more than 72 h in water as a neutral biological solvent. LMn and LZn complexes manifested good activity on SW-872 cancerous cells after 48 h exposure time ( IC50: 134.8 ± 2.82 µg/mL and IC50: 144.6 ± 2.07 µg/mL, respectively). The morphology of cell death in SW-872 cancerous cells treated with the LZn complex showed an apoptosis type cell death. Additionally, cell cycle studies declared the cell cycle arrest in the S phase for LZn. In conclusion, the development of water-soluble thiosemicarbazone complexes with intrinsic fluorescent properties promises to facilitate the detection of these compounds in living cells, aiding the investigation of their wide-ranging biological activities.
Insights
New fluorescent thiosemicarbazone metal complexes show promise as anticancer agents. The LMn and LZn complexes effectively reduced proliferation in SW-872 cancer cells, inducing apoptosis and cell cycle arrest.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Cancer Research
Background:
- Platinum-based drugs are successful in cancer treatment, highlighting inorganic metal complexes as potential anticancer agents.
- Thiosemicarbazones and their metal derivatives are promising scaffolds for developing novel anticancer drugs.
Purpose of the Study:
- Synthesize and characterize novel fluorescent thiosemicarbazone ligand (L) and its transition metal complexes (Mn(II), Fe(III), Ni(II), Cu(II), Zn(II)).
- Evaluate the anti-proliferative activity of these compounds against human liposarcoma (SW-872) and breast adenocarcinoma (MCF-7) cancer cell lines.
- Investigate the mechanism of cell death and cell cycle effects induced by the complexes in SW-872 cells.
Main Methods:
- Condensation reaction for synthesis of thiosemicarbazone ligand and its metal complexes.
- Chemico-physico techniques for structural elucidation.
- MTT assay for anti-proliferative activity evaluation.
- Flow cytometry for cell death morphology and cell cycle analysis.
- Fluorescence microscopy for imaging of treated cells.
Main Results:
- Synthesized water-soluble and stable thiosemicarbazone ligand (L) and its metal complexes (LMn, LFe, LNi, LCu, LZn).
- LMn and LZn complexes exhibited significant anti-proliferative activity against SW-872 cells (IC50: 134.8 ± 2.82 µg/mL and 144.6 ± 2.07 µg/mL, respectively).
- LZn complex induced apoptosis and S-phase cell cycle arrest in SW-872 cells.
Conclusions:
- Water-soluble thiosemicarbazone metal complexes with fluorescent properties are promising anticancer agents.
- The intrinsic fluorescence aids in tracking compounds within living cells for further biological activity studies.
- LMn and LZn complexes demonstrate potential for targeted cancer therapy.
