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Methyl (Z)-2-(Isothioureidomethyl)-2-pentenoate Hydrobromide Induces Cell Cycle Arrest and Disrupts Mitosis in a
Laura Sartori Assunção1,2, Iara Patricia Kretzer3, Jelver Alexander Sierra Restrepo4
1Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Florianopolis, SC 88040-900, Brazil.
Introduction/Objective:
Cancer is a global health burden. Despite advances in early detection and therapeutics, cancer prevalence continues to increase, underscoring the need for innovative therapeutic strategies. Dysregulation of cell death mechanisms is a hallmark of cancer that can lead to apoptosis evasion, which strongly contributes to tumor progression and therapy resistance. Isothiouronium salts have attracted attention as promising antitumor agents. This study aimed to evaluate the in vitro antitumor effect of an isothiouronium salt (ISMF08) on the B16F10 melanoma cell line.
Methods:
The antitumor properties of IS-MF08 were investigated by incubating B16F10 cells with the compound at different concentrations. Cytotoxicity was determined by the (3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide) (MTT) assay, cell cycle arrest and cell death mechanisms by flow cytometry, and morphological alterations by transmission electron microscopy. Physicochemical parameters related to druglikeness were predicted in silico using the SwissADME tool.
Results:
IS-MF08 was cytotoxic to melanoma cells, triggering cell cycle arrest and disrupting mitosis. The mechanism of cell death was compatible with apoptosis, as indicated by annexin V-FITC experiments and the relevant morphological changes in cell structure observed by transmission electron microscopy. SwissADME predicted that IS-MF08 has good physicochemical properties related to absorption and permeation.
Conclusion:
The numerous mechanisms of cell death triggered by IS-MF08 and its drug-likeness make it an interesting molecule in the search for new antitumor compounds, contributing to therapies targeting the dysregulation of cellular mechanisms such as apoptosis.
Insights
A novel isothiouronium salt, ISMF08, demonstrated significant antitumor effects against B16F10 melanoma cells in vitro. This compound induces apoptosis and cell cycle arrest, showing promise as a new therapeutic agent for cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- Cancer remains a significant global health challenge, with increasing prevalence despite advances in treatment.
- Apoptosis evasion is a key factor in tumor progression and resistance to cancer therapies.
- Isothiouronium salts are emerging as potential candidates for novel antitumor agents.
Purpose of the Study:
- To investigate the in vitro antitumor activity of the isothiouronium salt, ISMF08.
- To evaluate the effects of ISMF08 on B16F10 melanoma cells.
- To assess the potential of ISMF08 as a therapeutic strategy targeting cancer cell death mechanisms.
Main Methods:
- Cytotoxicity was assessed using the MTT assay.
- Cell cycle arrest and apoptosis were analyzed via flow cytometry.
- Morphological changes were observed using transmission electron microscopy.
- In silico prediction of physicochemical properties was performed using SwissADME.
Main Results:
- ISMF08 exhibited cytotoxicity against B16F10 melanoma cells.
- The compound induced cell cycle arrest and disrupted mitosis.
- Cell death was consistent with apoptosis, evidenced by annexin V staining and morphological alterations.
- In silico analysis indicated favorable drug-likeness properties for ISMF08.
Conclusions:
- ISMF08 triggers multiple cell death pathways, including apoptosis.
- The compound possesses favorable physicochemical properties, suggesting good drug-likeness.
- ISMF08 represents a promising candidate for developing new antitumor therapies targeting cancer's evasion of cell death mechanisms.
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