A newly synthesized thiosemicarbazide derivative trigger apoptosis rather than necroptosis on HEPG2 cell line

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dc.contributor.authorBaşoğlu-Ünal F.
dc.contributor.authorBecer E.
dc.contributor.authorEnsarioğlu H.K.
dc.contributor.author-Güzeldemirci N.U.
dc.contributor.authorKuran E.D.
dc.contributor.authorVatansever H.S.
dc.date.accessioned2024-07-22T08:02:06Z
dc.date.available2024-07-22T08:02:06Z
dc.date.issued2024
dc.description.abstractThiosemicarbazide derivatives have been the focus of scientists owing to their broad biological activities such as anticancer, antimicrobial, and anti-inflammatory. Herein, we designed and synthesized a new thiosemicarbazide derivative (TS-1) and evaluated its antiproliferative potential against the human hepatocellular carcinoma cell line (HEPG2) and human umbilical vein endothelial cell line (ECV-304). Also, it was aimed to investigate the necroptotic and apoptotic cell death effects of TS-1 in HEPG2 cells, and these effects were supported by molecular docking. The new synthesized compound structure was characterized using various spectroscopic methods such as FT-IR, 1H-NMR, 13C-NMR, and elemental analysis. The cytotoxic activity of the tested compound was measured by the MTT assay. Apoptotic and necroptotic properties of the TS-1 were evaluated by indirect immunoperoxidase method using antibodies against Ki-67, Bax, Bcl-2, caspase-3, caspase-8, caspase-9, RIP3, and RIPK1. Apoptotic and necroptotic effects of TS-1 were supported by molecular docking. Compound TS-1 was synthesized as a pure compound with a high yield. The effective value of TS-1 was 10 μM in HEPG2 cells. TS-1 did not show any cytotoxic effect on ECV-304. Caspase-3 and RIPK1 immunoreactivities were significantly increased in HEPG2 cells after being treated with TS-1. As the results of the molecular docking studies, the molecular docking showed that the TS-1 exhibits H-bond interaction with various significant amino acid residues in the active site of both RIPK1. It could be concluded that TS-1 could be a promising novel therapeutic agent by inducing apoptosis rather than necroptosis in HEPG2 cells. © 2023 John Wiley & Sons Ltd.
dc.identifier.DOI-ID10.1111/cbdd.14355
dc.identifier.issn17470277
dc.identifier.urihttp://akademikarsiv.cbu.edu.tr:4000/handle/123456789/11721
dc.language.isoEnglish
dc.publisherJohn Wiley and Sons Inc
dc.rightsAll Open Access; Bronze Open Access
dc.subjectAntineoplastic Agents
dc.subjectApoptosis
dc.subjectCaspase 3
dc.subjectCell Line, Tumor
dc.subjectCell Proliferation
dc.subjectHep G2 Cells
dc.subjectHumans
dc.subjectLiver Neoplasms
dc.subjectMolecular Docking Simulation
dc.subjectMolecular Structure
dc.subjectNecroptosis
dc.subjectSemicarbazides
dc.subjectSilicates
dc.subjectSpectroscopy, Fourier Transform Infrared
dc.subjectTitanium
dc.subject4 allyl 1 [[6 (4 methoxyphenyl)imidazo[2,1 b]thiazol 3 yl]acetyl]thiosemicarbazide
dc.subjectamino acid
dc.subjectcaspase 3
dc.subjectcaspase 8
dc.subjectcaspase 9
dc.subjectKi 67 antigen
dc.subjectprotein Bax
dc.subjectprotein bcl 2
dc.subjectthiosemicarbazide derivative
dc.subjectunclassified drug
dc.subjectantineoplastic agent
dc.subjectcaspase 3
dc.subjectsemicarbazide derivative
dc.subjectsilicate
dc.subjectthiosemicarbazide
dc.subjecttitanium
dc.subjecttitanium silicide
dc.subjectantiproliferative activity
dc.subjectapoptosis
dc.subjectArticle
dc.subjectcarbon nuclear magnetic resonance
dc.subjectcell structure
dc.subjectcontrolled study
dc.subjectcytotoxicity
dc.subjectdrug binding
dc.subjectdrug design
dc.subjectdrug structure
dc.subjectdrug synthesis
dc.subjectECV-304 cell line
dc.subjectelemental analysis
dc.subjectFourier transform infrared spectroscopy
dc.subjectHep-G2 cell line
dc.subjecthuman
dc.subjecthuman cell
dc.subjectimmunocytochemistry
dc.subjectimmunoperoxidase staining
dc.subjectimmunoreactivity
dc.subjectmolecular docking
dc.subjectMTT assay
dc.subjectnecroptosis
dc.subjectproton nuclear magnetic resonance
dc.subjectstructure analysis
dc.subjectapoptosis
dc.subjectcell proliferation
dc.subjectchemical structure
dc.subjectchemistry
dc.subjectHep-G2 cell line
dc.subjectliver tumor
dc.subjectmetabolism
dc.subjecttumor cell line
dc.titleA newly synthesized thiosemicarbazide derivative trigger apoptosis rather than necroptosis on HEPG2 cell line
dc.typeArticle

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