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Adaptive and terminal endoplasmic reticulum stress genes methylation levels in Parkinson patients' peripheral blood
(Literatura Medica, 2025) Gemici, Yagmur Inalkac; Dundar, Muhammed; Gozukara, Harika Gozde; Koc, Ahmet
Background and purpose-Misfolded protein stress has come to the fore among the molecular mechanisms that can cause degeneration. Whereas one of the most important protein of adaptive Endoplasmic Reticulum stress (ERS) is XBP1, CHOP and ASK proteins are associated with apoptosis and terminal ERS. To the best of our knowledge, methylation levels of adaptive and terminal ERS genes in Parkinson's Disease (PD) patients' blood are unknown. We aimed to evaluate if there is a difference in the DNA methylation levels of the ERS related protein-coding genes in peripheral blood of PD patients compared with healthy controls. The clinical significance of these gene methylation levels was evaluated as the second aim. Methods-DNA was isolated from the blood of PD patients (n=23) and controls (n=19). We used a methylation-specific qPCR approach to assess the methylation status of the ERS genes. The correlation between clinical findings and the methylation levels in PD patients were evaluated with appropriate statistical methods. Results-Terminal ERS related genes were statistically significantly hypomethylated in PD (ASK1 p=0.020, and CHOP p<0.001) whereas adaptive ERS gene XBP1's methylation level was not different between groups. Except for XBP1 and MMSE positive, and CHOP and depression negative correlation no correlation was found between clinical markers and methylation levels of the selected genes. (p=0.040, p=0.024), Conclusion-PD patients' peripheral blood methylation levels of adaptive and terminal ERS related genes are significantly different from healthy controls'. While XBP1 is known to be neuroprotective, CHOP and ASK are important proteins in apoptosis, and their methylation differences in peripheral blood provide a clue that they could be used as biomarkers in the future. Therefore, further biomarker and treatment studies should be conducted on these proteins and their pathways.
Comparative chemical and biological evaluation of Urtica dioica extracts obtained by methanol and hexane: antioxidant, cytotoxic, apoptotic, and antimicrobial potentials
(Bmc, 2025) Ugur, Yilmaz; Menevse, Irem Nur; Dundar, Muhammed; Karci, Huseyin; Zengin, Rukiye; Guzel, Abdussamat
Background Urtica dioica L. is a widely utilized medicinal plant with potential antioxidant, cytotoxic, and antimicrobial properties. Methods This study aimed to investigate its multi-target biological activities across four cell lines (A549, MDA-MB-231, HCT116, and BEAS-2B) while evaluating the impact of two extraction solvents (acidified methanol and hexane) on activity outcomes. Results The acidified methanolic extract exhibited higher total phenolic (61.25 +/- 3.07 mg GAE/g) and flavonoid (51.20 +/- 2.01 mg CE/g) content, correlating with superior antioxidant activity (DPPH: 84.36 +/- 1.50 mg TE/g; CUPRAC: 174.04 +/- 9.54 mg TE/g). In contrast, the hexane extract demonstrated stronger cytotoxicity across cancer cell lines (IC50: 3.10-4.12 mu g/mL), along with significant induction of apoptosis and G0/G1 cell cycle arrest, despite lower antioxidant capacity. In addition, both extracts increased the protein levels of p21 and cleaved caspase-3, suggesting involvement of cell cycle inhibition and activation of intrinsic apoptotic signalling pathways. Moderate antimicrobial activity was also observed, with inhibition zones ranging from 7 to 10 mm across bacterial and fungal strains. Conclusions These findings highlight the bioactive potential of U. dioica and the critical role of extraction solvent in modulating its total phenolic and flavonoid contents and biological effects. The observed upregulation of p21 and cleaved caspase-3 further supports the notion that U. dioica extracts may exert antiproliferative activity through p21-mediated cell cycle control and caspase-dependent apoptosis. Further in vivo studies and mechanistic investigations are needed to confirm these observations and clarify their potential therapeutic relevance.
Exploring the antimicrobial potential of new selenium- N-heterocyclic carbene complexes and their benzimidazolium salts: synthesis, characterization, biological evaluation, and docking insights
(Springer Int Publ Ag, 2025) Boualia, Boutheina; Sandeli, Abd el-Krim; Boulebd, Houssem; Karci, Huseyin; Dundar, Muhammed; Ozdemir, Ilknur; Gurbuz, Nevin
The present work, describes the synthesis and antimicrobial evaluation of new selenium-NHC adducts (3a-e) and their corresponding benzimidazolium salts (2a-e). Specific synthetic approaches were employed, resulting in compounds with satisfactory stability under humid and aerated conditions. Characterization by spectroscopic methods confirmed structural changes upon selenium incorporation. Biological evaluations revealed varying antimicrobial and antifungal activities among the synthesized compounds. The results indicated that the benzimidazolium salts exhibited significantly enhanced antimicrobial and antifungal activities compared to reference agents. For instance, compound 2a demonstrated an IC50 value of 6.25 mu g/mL against Candida albicans, which was comparable to the reference Caspofungin (6.25 mu g/mL). Similarly, compound 2e demonstrated strong antibacterial activity against Staphylococcus aureus, with an IC50 value of 0.8 mu g/mL, significantly outperforming the reference Ampicillin (1.56 mu g/mL). In contrast, the selenium-NHC adducts exhibited moderate to minimal activity, with compound 3e showing the highest IC50 value of 25 mu g/mL against Staphylococcus aureus, but failing to surpass the activity of the reference agent. To explore the potential mechanism of action, molecular docking studies were conducted against Escherichia coli DNA gyrase and CYP51. The molecular docking results demonstrate that synthesized compounds exhibit significant binding affinity against both enzymes, indicating antibacterial and antifungal potential. These binding affinities suggest that these molecules could be effective dual-action antimicrobial agents.
Global gene expression profiling in congenital diaphragmatic hernia (CDH) patients
(Springer Heidelberg, 2022) Gurunluoglu, Kubilay; Dundar, Muhammed; Unver, Turgay; Akpinar, Necmettin; Gokce, Ismail Kursad; Gurunluoglu, Semra; Demircan, Mehmet
Congenital diaphragmatic hernia (CDH) is an anomaly characterized by a defect in the diaphragm, leading to the passage of intra-abdominal organs into the thoracic cavity. Herein, the presented work analyzes the global gene expression profiles in nine CDH and one healthy newborn. All of the patients had left posterolateral (Bochdalek) diaphragmatic hernia, operated via an abdominal approach, and stomach and bowels in the thorax cavity. Some patients also had additional anomalies. A total of 560 differentially regulated genes were measured. Among them, 11 genes showed significant changes in expression associated with lung tissue, vascular structure development, and vitamin A metabolism, which are typical ontologies related to CDH etiology. Among them, SLC25A24 and RAB3IL1 are involved in angiogenesis, HIF1A and FOXC2-AS1 are related with the alveolus, MAGI2-AS3 is associated with the diaphragm, LHX4 and DHH are linked with the lung, and BRINP1, FZD9, WNT4, and BLOC1S1-RDH5 are involved in retinol. Besides, the expression levels of some previously claimed genes with CDH etiology also showed diverse expression patterns in different patients. All these indicated that CDH is a complex, multigenic anomaly, requiring holistic approaches for its elucidation.
Global gene expression profiling in congenital diaphragmatic hernia (CDH) patients (vol 22, pg 359, 2022)
(Springer Heidelberg, 2022) Gurunluoglu, Kubilay; Dundar, Muhammed; Unver, Turgay; Akpinar, Necmettin; Gokce, Ismail Kursad; Gurunluoglu, Semra; Demircan, Mehmet
[Abstract Not Available]
Integrated chemical and biological characterization of Hypericum perforatum extract using LC-MS/MS and in vitro functional assays
(Nature Portfolio, 2026) Guzel, Mehmet Ali; Kolac, Turgay; Menevse, Irem Nur; Dundar, Muhammed; Zengin, Rukiye; Guzel, Abdussamat; Ugur, Yilmaz
Hypericum perforatum L. (St. John's wort) is a medicinal plant known for its diverse secondary metabolites and pharmacological potential. This study provides a comprehensive evaluation of the phytochemical composition and bioactivities of methanolic extracts from wild H. perforatum. LC-MS/MS analysis identified 36 compounds, including phenolic acids (chlorogenic acid, protocatechuic acid) and flavonoids (rutin, isoquercitrin, quercetin), with the first-time detection of genkwanin, vicenin-2, schaftoside, and afzelin, to the best of our knowledge. The extract demonstrated significant antioxidant activity, with a total phenolic content of 203.04 mg GAE/g DW and strong radical scavenging activity in DPPH (544.78 mg TE/g DW) and ABTS (312.15 mg TE/g DW) assays. In vitro assays showed marked cytotoxicity across multiple cancer cell lines, with IC50 values as low as 3.57 & micro;g/mL in A549 cells, indicating stronger activity compared to cisplatin. Flow cytometric analysis revealed substantial apoptosis induction (up to 53.67% in A549 cells) and G0/G1 cell cycle arrest (76.37% in A549). The extract also exhibited moderate antibacterial activity against E. coli and S. aureus, but no activity against P. aeruginosa or Candida species. These results position H. perforatum as a rich source of bioactive compounds with antioxidant, anticancer, and antimicrobial potential, and suggest further research into its therapeutic applications.
Investigation of the Neuroprotective Effect of N-(p-amylcinnamoyl) Anthranilic Acid on Hippocampal Endoplasmic Reticulum Stress in WAG/Rij Rats with Absence Epilepsy
(Wiley, 2022) Kaya, Gul Busra; Duzova, Halil; Kaya, Mehmet; Dundar, Muhammed; Koc, Ahmet
[Abstract Not Available]
Local ADSC Delivery Methods Accelerate Healing of Large Unburned Full-Thickness Skin Defects by Promoting an Optimal Wound Microenvironment
(Mdpi, 2026) Gurunluoglu, Semra; Satilmis, Basri; Gul, Mehmet; Dundar, Muhammed; Gurunluoglu, Kubilay; Karaaslan, Ezgi; Koc, Ahmet
Background: This study introduces an experimental model of a large, full-thickness skin defect and evaluates how adipose-derived stem cells characterized by high self-renewal and differentiation capacity affect both wound healing and the wound microenvironment when delivered using two different local application methods. Materials and Methods: In this preclinical study, we established an excisional full-thickness skin defect model involving approximately 30% of the total body surface area (TBSA). Five experimental groups were formed, each containing equal numbers of male and female rats: (1) subdermal ADSC injection (ADSC-I) (n = 8), (2) application of an acellular dermal matrix (ADM) seeded with ADSCs (n = 8) (ADSC-ADM), (3) ADM alone (n = 8), (4) subdermal saline injection (n = 8) (SS-I), and (5) an untreated skin-defect sham group (n = 8). Wound healing and wound microenvironment parameters were assessed at regular intervals using macroscopic and microscopic evaluations, as well as various quantitative measurements. The study was terminated when complete wound closure was achieved in all animals of at least one experimental group. Results: The most favorable healing outcomes were observed in the two ADSC-treated groups. More favorable microenvironmental conditions in the stem cell groups were detected from day 14 onward. Complete closure of the dermal defects occurred by day 32 in the ADSC-I group, whereas none of the other groups achieved full wound closure within the study period. Conclusions: Local application of adipose-derived stem cells may accelerate wound healing by favorably modulating the wound microenvironment.
N-alkylbenzimidazole silver(I) complexes: Synthesis, biological evaluation and molecular docking study
(Pergamon-Elsevier Science Ltd, 2024) Ari, Erkan; Sahin, Neslihan; Ustun, Elvan; Dundar, Muhammed; Karci, Huseyin; Ozdemir, Lknur; Koc, Ahmet
A series of N-alkylbenzimidazole silver(I) complexes were synthesized and fully characterized by FT-IR, Mass, 1H, 13C{1H} NMR spectroscopy, and elemental analysis. Synthesized N-alkylbenzimidazole silver(I) complexes were investigated for their antimicrobial activities against bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and the fungal strains Candida albicans and Candida glabrata. All the complexes (2a-f) showed higher antimicrobial activity against bacteria than fungi strains. In particular, complexes 2b and 2e showed comparable activity to Ampicillin against Escherichia coli. Also, all complexes showed better activity than Ampicillin against Pseudomonas aeruginosa. The complex 2e showed remarkable activity against Candida albicans (12.5 mu g/mL) and Candida glabrata (25 mu g/mL). The molecules that were first optimized by DFT-based calculation methods were also analyzed by molecular docking methods against DNA gyrase of E. Coli, CYP51 from Candida glabrata, and Penicillin Binding Protein-3.
Novel N-heterocyclic carbene silver(I) complexes: Synthesis, structural characterization, antimicrobial and cytotoxicity potential studies
(Elsevier Science Sa, 2025) Karaca, Emine Ozge; Mizrak, Ebru; Gurbuz, Nevin; Cetinkaya, Erdem; Karci, Huseyin; Dundar, Muhammed; Ozdemir, Ilknur
In this study, a new series of 1-(2-ethylhexyl)-3-(alkyl)-5,6-dimethylbenzimidazol-2-ylidene]silver(I) complexes has been synthesized and investigated their in vitro antibacterial, antifungal and anticancer properties. All molecules were characterized by 1H NMR, 13C NMR, and IR spectroscopy techniques. In vitro antimicrobial activity of the synthesized compounds investigated in this work was tested against the reference strains: Escherichia coli (ATCC 25922), Staphylococcus aureus (ATCC 29213) and Pseudomonas aeruginosa (ATCC 27853), Candida albicans (ATCC MYA-2876) and Candida glabrata (ATCC 2001). Anticancer properties of samples were evaluated against A549, HCT116 and BEAS-2B cells lines. All silver-NHC complexes showed antibacterial activity against the tested bacterial and fungal strains.
Selenium deficiency is functionally linked with the molecular etiopathogenesis of necrotizing enterocolitis (NEC)
(Springer Heidelberg, 2025) Gurunluoglu, Kubilay; Dundar, Muhammed; Unver, Turgay; Turgut, Hatice; Gurunluoglu, Semra; Akpinar, Necmettin; Ates, Hasan
Necrotizing enterocolitis (NEC) is a severe and often catastrophic gastrointestinal emergency that predominantly affects neonates, especially those born prematurely, and is associated with high rates of morbidity and mortality. Despite its significant clinical impact, the precise etiology and molecular pathogenesis of NEC remain incompletely understood. In this study, we conducted global transcriptomic profiling using high-throughput RNA sequencing in 11 premature neonates diagnosed with NEC, following rigorous inclusion and exclusion criteria. Compared to healthy controls, we identified 1,204 differentially expressed genes (DEGs), including 636 upregulated and 568 downregulated transcripts. Notably, genes involved in hypoxia-induced apoptosis (e.g., HIF1 AAS3, HIF1 AAS1), the caspase cascade (BCL2, BCL6, CASP5, CASP7), and inflammation (IL1RAP, IL6ST, TNFAIP3, TNFRSF10 A, TLR6, TLR10) were significantly upregulated. In contrast, IL18, a key modulator of inflammatory responses, was downregulated. Interestingly, several genes encoding selenoproteins (GPX1, GPX4, SELENON, SELENOM, SELENOF, SELENOW, SELENOT) were also downregulated, suggesting molecular evidence of selenium deficiency. Gene ontology and pathway enrichment analyses revealed widespread dysregulation in pathways related to hypoxia response, systemic inflammation, coagulation, antimicrobial defense, mitochondrial function, autophagy, selenium metabolism, and apoptosis. Collectively, our findings provide novel insights into the molecular underpinnings of NEC in premature infants and suggest that systemic hypoxia, oxidative stress, selenium deficiency, and programmed cell death contribute significantly to its pathogenesis.
Silver (I)-N-heterocyclic carbene complexes: Synthesis and characterization, biological evaluation of Anti-Cholinesterase, anti-alpha-amylase, anti-lipase, and antibacterial activities, and molecular docking study
(Elsevier Science Sa, 2021) Sandeli, Abd El-Krim; Khiri-Meribout, Naima; Benzerka, Saida; Gurbuz, Nevin; Dundar, Muhammed; Karci, Huseyin; Bensouici, Chawki
A series of novel silver(I)-N-heterocyclic carbene complexes have been prepared and fully characterized by spectroscopic methods and X-ray crystallographic analyses. The biological capacity of the synthesized compounds was evaluated in vitro for their anti-microbial, anti-cholinesterase, anti-lipase, anti-diabetic activities in search of potent inhibitors compound. All compounds were tested against two types of fungi and three bacterias. The results proved that most compounds indicated moderate to excellent activity against all types of bacteria and fungi except compound 2f that didn't show any antibacterial activity. The synthesized compound's capacity to inhibit the enzymes AChE, BChE, Lipase, and alpha-amylase were evaluated. The results showed that silver(I)-NHC complexes 3a-f are effective against all types of enzymes. The highest activity was reported toward AChE, BChE, and alpha-amylase enzymes, and at a lower rate against Lipase enzyme compared to the references drug. In contrast, benzimidazolium salts 2a-f, which showed significant inhibitory activity against AChE and BChE enzymes, while all salts were not active against both Lipase and alpha-amylase enzymes. Molecular docking simulations using AutoDock, have been performed of the new compounds as a representative set of our molecules into AChE and BChE enzymes for lead optimization of the binding interaction template of the most active inhibitors docked into the active site of their relevant AChE and BChE enzymes inhibitors.
Single-Chain Variable Fragment-Based Dot Blot, Single, and Multiple Assays for Rapid SARS-CoV-2 Diagnostics
(Oxford Univ Press Inc, 2025) Cam Derin, Dilek; Gultekin, Enes; Taskin, Irmak Icen; Dundar, Muhammed; Otlu, Baris
Background Antigenic detection is reliably utilized in rapid diagnostic tests and provides a significant time advantage during pandemics and epidemics. Therefore, the rapid detection of viral infections is of great importance and will remain crucial in the future. The SARS-CoV-2 outbreak, which resulted in severe losses, is the most recent example of this necessity. Among rapid diagnostic tests, lateral flow assays (LFAs) are the most practical and do not require specialized equipment, typically being developed using antibody pairs.Objective This study aimed to recombinantly produce a single-chain variable fragment (scFv) specific to the SARS-CoV-2 spike receptor-binding domain (sRBD) and to employ it in the development of LFAs utilizing both antibody and aptamer pairs and an aptamer cocktail.Methods Gold nanoparticles were employed as labeling agents, while both the scFv and full length forms of CR3022, along with aptamers specific to the S and N proteins, were utilized in a sandwich assay format.Results scFv was produced at a higher concentration and biologically active. It demonstrated effective viral detection in single LFA, dot blot assay (DBA), and multiplex LFA. While single LFA successfully detected only the synthetic target, DBA and multiplex LFA selectively identified the virus in nasopharyngeal and oropharyngeal swab samples.Conclusion Findings highlight the differences and effectiveness of using scFv in combination with other capture agents and different assay principles for the development of cost-effective and rapid diagnostic tests.Highlights scFvs exhibit variable binding in sandwich assays depending on the combinations employed. When used in combination with an aptamer cocktail, scFvs demonstrate enhanced target binding, which is shown for the first time in this study. The use of multiple testing strategies enables a more effective viral diagnosis.
Synthesis and biological evaluation of pyrazolyl-pyrazolone derivatives: Antioxidant, anticancer activities, and molecular docking insights
(Elsevier, 2025) Benoune, Racha Amira; Boulcina, Raouf; Dems, Mohamed Abdesselem; Ugur, Edanur; Karci, Hueseyin; Dundar, Muhammed; Koc, Ahmet
In this study, a series of novel pyrazolyl-pyrazolone derivatives was synthesized via a Knoevenagel condensation reaction using trisodium citrate as a catalyst, highlighting an environmentally sustainable and cost-effective approach. The synthesized compounds were characterized through comprehensive analytical techniques, including NMR spectroscopy, HRMS, and melting point determination. Biological evaluations demonstrated diverse and promising activities: compound 6i exhibited exceptional antioxidant activity across DPPH, ABTS, and Ferric-phenanthroline assays, outperforming standard antioxidants like BHT and BHA. In parallel, anticancer assays against SH-SY5Y and HCT116 cell lines revealed compounds 6e, 6j, and 6k as potent cytotoxic agents, with IC50 values significantly lower than cisplatin, the reference drug. Notably, compound 6j showed remarkable selectivity towards cancer cells with reduced cytotoxicity on non-cancerous BEAS-2B cells. Molecular docking studies confirmed strong binding interactions of the active compounds with key cancer-related protein targets, shedding light on their mechanisms of action. These findings not only highlight the therapeutic potential of pyrazolyl-pyrazolone derivatives as dual antioxidant and anticancer agents but also emphasize the value of sustainable chemical processes in drug development.
Synthesis of new imidazolidine derivatives: Characterization, anti-cancer potential and molecular docking
(Elsevier, 2025) Slimani, Ichraf; Karci, Huseyin; Dundar, Muhammed; Ustun, Elvan; Ozdemir, Lknur; Gurbuz, Nevin; Koc, Ahmet
Creating safe and effective anticancer pharmaceuticals with an imidazolidine heterocyclic ring was the goal of this project. Starting with 1-(2-hydroxypropyl)imidazoline and N, N-dimethylformamide dimethyl acetal, substituted-imidazolidine derivatives (3a-h) have been generated. The anti-tumor potential of the imidazolidine derivatives (3a-h) was further investigated using the human colon cancer cell line HCT116 and the human neuroblastoma cell line SH-SY5Y. All of the synthesized compounds, except for All synthesized compounds, except for the salt 3f (1-(2-hydroxypropyl)-3-(3,4,5-trimethoxybenzyl) imidazolinium chloride) which was not active against the HCT116 cancer cell line, were active against the two cell lines. According to the results of biological tests, the inhibitory concentration (IC50) values ranged from 45.44 mu M to 663.73 mu M. The salt 3 g showed the highest anticancer effect, particularly against the HCT116 cancer cell line, with a selectivity index reaching 2.75. Also, optimized molecules were analyzed by molecular docking methods against crystal structures of Vascular Endothelial Growth Factor Receptors (VEGFR2) and Cytochrome P450 17A1, and their binding affinities, interaction details and inhibition constants were determined. The molecules were additionally evaluated for possible drug-likeness and bioavailability scores which include absorption, distribution, metabolism, excretion and toxicity aspects.
Synthesis, antimicrobial activity and molecular docking study of benzyl functionalized benzimidazole silver(I) complexes
(Springer, 2023) Ari, Erkan; Sahin, Neslihan; Ustuen, Elvan; Dundar, Muhammed; Karci, Hueseyin; Ozdemir, Ilknur; Koc, Ahmet
In this study, a series of N-functionalized benzimidazole silver(I) complexes were prepared and characterized by FT-IR, H-1, C-13{H-1} NMR spectroscopy, and elemental analysis. Synthesized N-benzylbenzimidazole silver(I) complexes were evaluated for their antimicrobial activities against bacteria Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and the fungal strains Candida albicans and Candida glabrata. The results indicated that N-alkylbenzimidazole silver(I) complexes exhibited good antimicrobial activity compared to N-alkylbenzimidazole derivatives. Especially, complex 2e presented perfect antimicrobial activity than the other complexes. The characterized molecules were optimized by DFT-based calculation methods and the optimized molecules were analyzed in detail by molecular docking methods against bacterial DNA-gyrase and CYP51. The amino acid residues detected for both target molecules are consistent with expectations, and the calculated binding affinities and inhibition constants are promising for further studies.
Synthesis, characterization, and anticancer potential of novel NHC ligands and their selenium complexes: a combined in vitro and in silico investigation
(Royal Soc Chemistry, 2025) Boualia, Boutheina; Sandeli, Abd el-Krim; Evren, Enes; Ozdemir, Ismail; Karci, Huseyin; Dundar, Muhammed; Ozdemir, Ilknur
We report herein the efficient synthesis of new benzimidazolium salts (A1-A6) and their corresponding selenium-NHC complexes (B1-B6), along with the evaluation of their cytotoxicity profiles against two cancer cell lines (HCT116 and SH-SY5Y) and one normal cell line (BEAS-2B). The findings revealed that the benzimidazolium salts (A1-A6) exhibited significantly higher cytotoxicity toward all tested cell lines compared to their selenium derivatives (B1-B6). Among them, compounds A3, A4, and A5 showed the most potent cytotoxic effects, with IC50 values ranging from 3.09 to 26.12 mu M, approximately ten times lower than that of cisplatin. However, these compounds also exhibited relatively low IC50 values in normal BEAS-2B cells, although still higher than those observed in the cancer cell lines, indicating a preferential cytotoxicity toward cancer cells. Structure-activity relationship analysis revealed that the benzimidazolium core acts as the pharmacophore of these compounds, while substitution on the aromatic ring-particularly with bulky groups-enhances cytotoxicity. Conversely, incorporation of the selenium atom was found to markedly reduce or even eliminate cytotoxicity up to concentrations of 800 mu M. Further in silico studies were conducted to gain a deeper understanding of the molecular structures and chemical reactivity of these compounds. In addition, molecular docking studies against PARP-1 and tubulin highlighted the strong inhibitory potential of the most active compounds (A3, A4, and A5) toward both targets, suggesting their potential involvement in the observed cytotoxic effects. Overall, these investigations propose benzimidazolium salts A3, A4, and A5 as promising anticancer agents and highlight the selenium derivatives as non-toxic selenium-based NHC complexes. Further studies should be undertaken to optimize the biological activity of these compounds and to enhance their selectivity toward cancer cells.
Sythesis, characterisation, anticancer and antimicrobial activity of Ag-N-heterocyclic carbene complexes containing benzimidazole derivatives
(Elsevier Science Sa, 2024) Karci, Huseyin; Dundar, Muhammed; Nawaz, Zahid; Ozdemir, Lknur; Gurbuz, Nevin; Koc, Ahmet; Ozdemir, Ismail
To prepare a novel series of silver(I) complexes, the interaction of benzimidazolium salts having their two nitrogen atoms substituted by bulky groups with Ag2O in DCM has been carried out. Their structures were characterized by elemental analyses, 1H NMR, 13C NMR, elemental analysis, and IR spectroscopy techniques. Further, the antimicrobial and antifungal activities properties of both the salts and their silver(I)-NHC complexes were tested against positive and negative bacteria using the Clinical and Laboratory Standards Institute (CLSI) and the European Committee for Antimicrobial Susceptibility Testing (EUCAST) respectively. The results show that silver complexes are effective against E. coli, P. aeruginosa and S. aureus bacterial species with moderate to high activity, and their minimum inhibitory concentrations ranging from 25 to 400 mu g/Ml. It was also observed that 3b compound, which has the best antifungal properties among the synthesized compounds, showed high antimicrobial activity when all bacterial species were taken into account. In addition, the salts and complexes were then evaluated for their ability to inhibit the proliferation of four different cancer cell lines (A549, MCF-7, HCT116, SH-SY5Y and BEAS-2B cells lines). AlamarBlue assay demonstrated that the salts and complexes exhibited potent cytotoxicity towards all cancer lines. 2c compound showed the highest cytotoxic activity against BEAS-2B, A549 and MCF-7 cell lines. Except for 2c, compounds 3d, 3e and 3f showed cytotoxic activity at the lowest concentrations against MCF7 cell line.The study highlights the importance of N-heterocyclic carbene ligands in the development of silver-based drugs with anticancer properties.
The impact of subdermal adipose derived stem cell injections and early excision on systemic oxidative stress and wound healing in rats with severe scald burns
(Elsevier Sci Ltd, 2024) Gurunluoglu, Kubilay; Satilmis, Basri; Gul, Mehmet; Dundar, Muhammed; Gokturk, Nurcan; Akbulut, Sami; Koc, Ahmet
Aim: This study aims to develop an experimental treatment model effective against oxidative stress in the acute period of severe burns and to analyze the mechanisms of healing large wound defects. Methods: Five rats, including 2 females and 3 males, were used as donors to obtain adipose- derived stem cells (ADSC) from the inguinal fat pad. The stem cells were labeled with green fluorescent protein. The study included four groups of 17 rats, each with grade 3 scalding burns on 30 % of their body surface, and a control group of 10 rats with an equal number of males and females. After early excision, 106 6 ADSC-derived stem cells were administered subdermally to the burned wound and autografted to the stem cell group (n = 17). The early excision group (n = 17) received early excision and autograft, with 2 ml of normal saline injected subdermally into the burn wound edge. The PLM group (n = 17) was treated with a polylactic membrane (PLM) dressing after the burn. No treatment was given to the burn group (n = 17). Ten rats from all groups were sacrificed on the 4th day post-burn for oxidative stress evaluation. The control group (n = 10) was sacrificed on day 4. Blood and tissue samples were collected post-sacrifice. Oxidative stress and inflammation in the blood, as well as cell damage in the skin, liver, kidneys, and lungs, were investigated histopathologically and biochemically on the 4th day post-burn. On the 70th day after burn, wound healing was examined macroscopically and histopathologically. Results: On the 4th day, oxidative stress results showed that the levels of Total Oxidative Capacity (TOC) in the blood were lowest in the stem cell (7.4 [6-8.8]), control (6.7 [5.9-7.6]), and early excision (7.5 [6.6-8.5]) groups, with no significant difference between them. The burn group (14.7 [12.5-16.9]) had the highest TOC levels. The PLM group (9.7 [8.6-10.7]) had lower TOC levels than the burn group but higher levels than the other groups. Histopathological examination on the 4th day revealed low liver caspase-3 immunoreactivity in the stem cell and early excision groups among the burn groups. Caspase3 immunoreactivity levels were as follows: stem cell group (20 [10-30]), early excision group (25 [15-50]), PLM group (70 [50-100]), control group (0), and burn group (80 [60-120]). Other oxidative stress and end-organ damage outcomes were consistent with these results. All rats in the stem cell group had burn wounds that healed completely by the 70th day. Examination of the skin and its appendages from the stem cell group with an immunofluorescence microscope demonstrated green coloration, indicating incorporation of stem cells. Conclusion: Stem cells may have the potential to form new skin and its appendages, providing better healing for large skin defects. Early excision treatment, by removing local necrotic tissues after extensive and deep burns, can prevent end-organ damage due to systemic oxidative stress and inflammation. We also believe that when these two treatments are used together, they can achieve the best results. (c) 2024 Elsevier Ltd and ISBI. All rights are reserved, including those for text and data mining, AI training, and similar technologies.
Tris(benzimidazole)(nitrato)silver(I) complexes: Synthesis, catalytic activities, and biological evaluation
(Elsevier, 2026) Boubakri, Lamia; Hallab, Wissem; Karci, Huseyin; Attour, Anis; Dundar, Muhammed; Ozdemir, Lknur Lknur; Gurbuz, Nevin
In this study new N-alkylbenzimidazole derivatives 1a-e and their related tris(benzimidazole)(nitrato)silver(I) complexes 2a-e were prepared and characterized by FT-IR, 1H,13C{1H} NMR spectroscopy, and elemental analysis, which support the proposed structures. Further confirmations of structural details were provided by a single-crystal X-ray. A single crystal of tris(N-alkylbenzimidazole)(nitrato)silver(I) 2e shows that the coordination geometry around Ag slightly distorted tetrahedral geometry. Further, the synthesized compounds were evaluated for their antimicrobial activities against bacteria Escherichia coli, P. aeruginosa, S. aureus, and the fungal strains C. albicans and C. glabrata. The results indicated that the activity shown by the tested compounds, especially against Gram-negative bacteria, is valuable for the development of new treatment options against these microorganisms. Especially, the drug development potential of N-alkyl-5,6-dimethylbenzimdazole 1b and complexes 2b, 2c, and 2e showing the highest antimicrobial activity. Also, the alkylbenzimidazole substituent 1b and 1e and the Tris(1-alkylbenzimidazole)silver(I) 2c showed remarkable activity against fungi strains. Complexes 2a, 2b, 2c, 2d, and 2e also showed high cytotoxicity. The synthesized complexes demonstrated higher cytotoxicity relative to Cisplatin across all tested cell lines. Furthemore, a mild catalytic protocol for benzaldehyde, amine, and phenylacetylene coupling (A3-coupling) allows for the selective synthesis of propargyl amines using N-alkylbenzimidazole silver(I) nitrate catalysts with conversion of 100 %. The present approach is environmentally benign and water is generated as the sole by product.

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