Related Experiment Video
Updated: Jul 4, 2026
05:17
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, Cytotoxicity, and Apoptosis-Associated Cell Death Activity of an Isatin-Containing Pyrimidine-Derived
Müjgan Kesik Oktay1, Cansu Topkaya2, Elif Kağa1
1Department of Medical Services and Techniques, Suhut Health Services Vocational School, Afyonkarahisar Health Sciences University, Afyonkarahisar, Türkiye.
Journal of Applied Toxicology : JAT
|July 2, 2026
Summary
A novel copper(II) complex exhibits significant anticancer potential by inducing cell death and cell cycle arrest in lung and breast cancer cells. This compound shows promising selectivity, being more toxic to cancer cells than healthy cells.
Area of Science:
- Inorganic Chemistry
- Medicinal Chemistry
- Cancer Biology
Background:
- Developing novel metal-based anticancer agents is crucial for overcoming drug resistance and improving therapeutic outcomes.
- Pyrimidine and isatin derivatives have shown diverse biological activities, including anticancer properties.
Purpose of the Study:
- To synthesize and characterize a novel copper(II) complex incorporating pyrimidine and isatin moieties.
- To evaluate the cytotoxic effects of the synthesized Cu(II) complex on A549 lung and MCF-7 breast cancer cell lines.
- To investigate the compound's impact on apoptosis-associated cell death and cell cycle regulation in A549 cells.
Main Methods:
- Cytotoxicity was assessed using MTT assays at multiple time points (24, 48, 72 hours) to determine IC50 values.
- Selectivity was evaluated by comparing cytotoxicity against cancer cells and normal human dermal fibroblasts (HDFa).
- Apoptosis and cell cycle distribution were analyzed via flow cytometry using Annexin V/PI and propidium iodide staining, respectively.
Main Results:
- The Cu(II) complex demonstrated time-dependent cytotoxicity against both A549 and MCF-7 cell lines, with lower IC50 values indicating higher potency over time.
- The compound exhibited selectivity, being 2-4 times more effective against cancer cells compared to HDFa cells.
- Flow cytometry revealed significant apoptosis-associated cell death (approx. 60% combined apoptotic and necrotic cells) and G2/M phase cell cycle arrest (26%) in A549 cells at the IC50 concentration.
Conclusions:
- The synthesized Cu(II) complex possesses significant cytotoxic activity against lung and breast cancer cell lines.
- The compound induces apoptosis-associated cell death and G2/M phase cell cycle arrest, suggesting potential anticancer mechanisms.
- This Cu(II) complex represents a promising candidate for further investigation as an anticancer therapeutic agent.
More Related Videos
Related Concept Videos
01:28Inhibitors of Bacterial DNA Synthesis
Bacterial pathogens depend on precise and efficient DNA replication to sustain infection. Two type II topoisomerases—DNA gyrase and topoisomerase IV—are critical to this process, as they resolve DNA supercoiling and unlink chromosomes during replication. Fluoroquinolones, synthetic derivatives of quinolones, exploit this mechanism by stabilizing the transient DNA–enzyme cleavage complex, preventing strand religation, and causing lethal double-strand breaks. These antibiotics are selectively...
01:22Antiviral Nucleoside Inhibitors
Antiviral Nucleoside InhibitorsAntiviral nucleoside inhibitors are structural analogs of natural nucleosides that interfere with viral DNA or RNA synthesis. These compounds selectively target viral polymerases due to their resemblance to host nucleosides, thereby disrupting viral genome replication.Mechanism of Acyclovir ActionAcyclovir is a guanosine analog with a three-carbon acyclic side chain. It selectively targets herpes simplex virus type 1 (HSV-1), herpes simplex virus type 2 (HSV-2),...
01:46Electron Transport Chain: Complex I and II
The mitochondrial electron transport chain (ETC) is the main energy generation system in the eukaryotic cells. However, mitochondria also produce cytotoxic reactive oxygen species (ROS) due to the large electron flow during oxidative phosphorylation. While Complex I is one of the primary sources of superoxide radicals, ROS production by Complex II is uncommon and may only be observed in cancer cells with mutated complexes.
ROS generation is regulated and maintained at moderate levels necessary...
ROS generation is regulated and maintained at moderate levels necessary...
01:19Allosteric Proteins-ATCase
Binding sites linkages can regulate a protein's function. For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...