Browsing by Author "Özerkan, D."

Now showing 1 - 4 of 4

Correction to: Comparison of Selenic Acid and Pyruvic Acid-Loaded Silver Nanocarriers Impact on Colorectal Cancer Viability
(2023-09-29) Erdemir, G.; Danişman-Kalindemirtaş, F.; Kariper, İ. A.; Kuruca, D. S.; Özerkan, D.
Colorectal cancer (CRC) is a leading cause of morbidity and death worldwide. As current cancer drugs are ineffective, new solutions are being sought in other fields, including nanoscience. Similarly, silver nanoparticles play an important role in the pharmaceutical industry as they act as anti-cancer agents with less harmful effects and are usually 1 to 100 nm in size. Selenic acid (SA) and pyruvic acid (PA) are involved in various metabolic pathways in cancer. For this reason, we decided to detect their influence on colorectal cancer using silver-based (Ag) nanocarriers. DLS, Zetasizer, SEM and UV-Vis analyses were used to characterize AgSA and AgPA. A UV spectrophotometer was used to analyze the release of the NPs. MTT analyses were used to measure the viability of HCT116 and HUVEC cells, and IC50 values were calculated using GraphPad Prism. The indicated dosage and particle size of AgSA NPs proved to be suitable for cytotoxicity. Moreover, injection of these nanoparticles into non-cancer cells proved safe due to their minimal toxicity. In contrast, the AgPA NPs have no cytotoxicity and induce proliferation of HCT116 cells. Finally, only the synthesised AgSA nanoparticles could be used for advanced cancer therapy, which is both inexpensive and has minimal side effects.
Enhanced anticancer effect of newly synthesised albumin-bound Fe(III)-S-Methyl-thiosemicarbazones on breast cancer cells
(2024.01.01) Danisman-Kalindemirtas, F.; Erdem-Kuruca, S.; Cilasun, G.E.; Sert, E.; Özerkan, D.; Demirci, T.B.; Ülküseven, B.; Kariper, I.A.
Thiosemicarbazones and their analogues are of significant interest due to their antiviral, antibacterial and anticancer properties. Recent advancements in nanoparticle-based therapeutics have enabled targeted cancer cell treatment while minimizing harm to healthy cells. This study focused on encapsulating patented N(1)-R1-salicylidene-N(4)-R2-salicylidene-S-methylisothiosemicarbazone complexes into albumin nanocarriers, creating albumin-bound Fe(III)-S-methyl-thiosemicarbazone (ALB-FeTc) nanoparticles via a novel UV-C lamp-assisted method. The nanoparticles were characterized using FTIR, UV-Vis, DLS and EDX-SEM. Cytotoxicity was evaluated in MCF-7 breast cancer cells and HUVEC cells using an MTT assay. Fluorescence microscopy and flow cytometry were employed to investigate the mechanism of cell death. The study demonstrated strong cytotoxicity of FeTcs against cancer cells, with enhanced effects observed for ALB-FeTcs. The ALB-FeTcs induced apoptosis selectively in cancer cells while sparing normal cells. These results suggest that ALB-FeTcs are promising candidates for breast cancer treatment.
Exploring Benzo[b][1,4]Thiazine Derivatives: Multitarget Inhibition, Structure–Activity Relationship, Molecular Docking, and ADMET Analysis
(John Wiley and Sons Inc, 2024) Alishba; Ali, I.; Hameed, S.; Khan, K.M.; Salar, U.; Taha, M.; Sadeghian, N.; Taslimi, P.; Tuzun, B.; Özerkan, D.; Dedeakayogullari, H.; Ulukaya, E.
A series of benzothiazine derivatives (1–17) were synthesized via an intermolecular cyclocondensation reaction involving 2-aminothiophenol (i) and substituted phenacyl bromide (ii). Structural elucidation of these synthetic derivatives utilized EI–MS, HR-EIMS, 1H NMR, and 13C NMR spectroscopic techniques. The synthesized analogs were evaluated against key enzyme targets (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and α-glucosidase (α-Glu)) and tested for cytotoxicity against various cancer cell lines. Six compounds were selected based on their inhibition profiles, exhibiting significant inhibitory potential against enzymes. In silico studies corroborated the observed inhibitory activities, aligning closely with experimental outcomes. Additionally, an ADME/T study provided insights into pharmacokinetic and safety profiles, identifying promising candidates for future drug development efforts.
Exploring Benzo[b][1,4]Thiazine Derivatives: Multitarget Inhibition, Structure-Activity Relationship, Molecular Docking, and ADMET Analysis
(2024.01.01) Alishba, I.; Ali, I.; Hameed, S.; Khan, K.M.; Salar, U.; Taha, M.; Sadeghian, N.; Taslimi, P.; Tuzun, B.; Özerkan, D.; Dedeakayogullari, H.; Ulukaya, E.
A series of benzothiazine derivatives (1-17) were synthesized via an intermolecular cyclo condensation reaction involving 2-aminothiophenol (i) and substituted phenacyl bromide (ii). Structural elucidation of these synthetic derivatives utilized EI-MS, HR-EIMS, H-1 NMR, and C-13 NMR spectroscopic techniques. The synthesized analogs were evaluated against key enzyme targets (acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and alpha-glucosidase (alpha-Glu)) and tested for cytotoxicity against various cancer cell lines. Six compounds were selected based on their inhibition profiles, exhibiting significant inhibitory potential against enzymes. In silico studies corroborated the observed inhibitory activities, aligning closely with experimental outcomes. Additionally, an ADME/T study provided insights into pharmacokinetic and safety profiles, identifying promising candidates for future drug development efforts.