A newly synthesized thiosemicarbazide derivative trigger apoptosis rather than necroptosis on HEPG2 cell line
Date Added: 26 February 2024, 09:07

Başoğlu‐Ünal, F., Becer, E., Ensarioğlu, H. K., ‐Güzeldemirci, N. U., Kuran, E. D., & Vatansever, H. S. (2024). A newly synthesized thiosemicarbazide derivative trigger apoptosis rather than necroptosis on HEPG2 cell line. Chemical Biology & Drug Design, 103(1), e14355.

Researchers, including Vatansever from DESAM Institute, Near East University, have conducted a study focusing on the synthesis and evaluation of a novel thiosemicarbazide derivative, TS-1, for its potential anticancer properties. Thiosemicarbazide derivatives have garnered significant attention due to their diverse biological activities, including anticancer effects. In this study, TS-1 was synthesized and characterized using various spectroscopic methods, including FT-IR, 1H-NMR, and 13C-NMR.

The cytotoxic activity of TS-1 was assessed using the MTT assay against the human hepatocellular carcinoma cell line (HEPG2) and human umbilical vein endothelial cell line (ECV-304). Results revealed that TS-1 exhibited significant antiproliferative effects on HEPG2 cells at a concentration of 10 μM for 24 hours, without inducing cytotoxicity in ECV-304 cells. Immunoperoxidase assays supported the apoptotic and necroptotic effects of TS-1 in HEPG2 cells, as evidenced by increased caspase-3 and RIPK1 immunoreactivities.

Molecular docking studies further elucidated the mode of action of TS-1, indicating H-bond interactions with crucial amino acid residues in the active site of RIPK1. These findings suggest that TS-1 holds promise as a potential therapeutic agent for hepatocellular carcinoma, primarily through apoptosis induction.

The study highlights the significance of thiosemicarbazide derivatives in cancer research and underscores the potential of TS-1 as a novel anticancer compound. Further research is warranted to explore its efficacy in vivo and elucidate its mechanism of action in greater detail. This study contributes to the ongoing efforts in developing effective treatments for cancer, particularly hepatocellular carcinoma, addressing an unmet medical need.

More Information:

https://onlinelibrary.wiley.com/doi/full/10.1111/cbdd.14355