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- Suleyman, Halis(167)
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- Ozcicek, Fatih(30)
- Süleyman, Halis(30)
- Onk, Didem(29)
- Ucpunar, Hanifi(29)
Yayınlar
- ArticleAçık Erişim2026Preoperative Geriatric Nutritional Risk Index (GNRI) and Comorbidity Burden as Mortality Risk Markers After Proximal Femoral Nailing in Older Patients with Pertrochanteric Hip Fractures
Gökgöz, Mehmet Burak; Kahraman, Hamit Çağlayan; Gür, Volkan; Öztürk, Akın; Doğan, İbrahim; Gönbe, Alper; Avcı, Berat; Koçkara, Nizamettin; Sofu, Hakan; Yapıcı, Furkan
Background: Mortality after geriatric hip-fracture surgery remains substantial. This study evaluated whether preoperative GNRI, comorbidity burden, and CBC-derived inflammatory indices were associated with one-year and long-term mortality after PFN for pertrochanteric/intertrochanteric fractures. Methods: In this single-centre retrospective cohort study of prognostic risk markers, 248 PFN records were screened. After excluding six incomplete records and 25 patients aged <65 years, 217 older fracture/surgical episodes formed the time-to-event cohort; 194 were evaluable for binary one-year mortality. Living patients/episodes with <365 days of follow-up were censored in survival analyses. Logistic and Cox models were supported by Firth penalized logistic regression, calibration assessment, and internal validation. Results: Median age was 82 years, 65.0% were female, and 68.7% were ASA III–IV. Overall, 96/217 (44.2%) died during median follow-up of 570 days. Thirty-day, 90-day, and one-year evaluable mortality were 7.4%, 15.2%, and 27.3%. GNRI < 82 identified a small high-risk subgroup: 10/13 evaluable patients/episodes (76.9%) died within one year versus 43/181 (23.8%) with GNRI ≥ 82. GNRI < 82 remained associated with one-year mortality in adjusted logistic regression, although with a wide confidence interval due to sparse subgroup size (OR 6.43, 95% CI 1.50–27.55; p = 0.012), and in Firth penalized sensitivity analysis (OR 5.51, 95% CI 1.34–22.61; p = 0.018). In Cox analysis, age, ASA III–IV, available Charlson-domain comorbidity burden, and lower continuous GNRI were associated with long-term mortality, whereas adding GNRI < 82 and NLR did not materially improve cross-validated discrimination. Conclusions: GNRI < 82 identified a small subgroup with high observed mortality after PFN. Because the subgroup was sparse and biomarker addition did not materially improve internally validated discrimination, GNRI should be treated as an alerting clinical flag rather than a stand-alone basis for patient-level risk prediction. External validation is required.
- ArticleAçık Erişim2026Enhanced Surface Properties and In Vitro Corrosion Tests of Ti─Nb─Sn Coating on CoCrMo Alloy for Biomedical Applications
Çakır, Mevra Aslan
Ti–Nb–Sn thin films were deposited onto CoCrMo alloy substrates by magnetron sputtering to enhance surface properties for biomedical applications. Structural and compositional analyses revealed a dense, crack-free, columnar coating with a sharp interface. Potentiodynamic polarization tests in PBS demonstrated a significant improvement in corrosion resistance, with approximately 70% reduction in corrosion current density and more than 10-fold increase in polarization resistance compared to the uncoated alloy. Wear tests under dry and PBS conditions showed that the Ti─Nb─Sn coating reduced the wear rate by more than five times, indicating enhanced wear performance. In vitro cytotoxicity assessments using MTT and LDH assays confirmed high cell viability, indicating non-cytotoxic behavior. Overall, the Ti─Nb─Sn coating offers an effective surface modification strategy for CoCrMo-based biomedical implants.
- ArticleYayıncıda açık erişim2026Redox-mediated activation of PI3K/PTEN pathways by A. baumannii OMV–V. myrtillus conjugate in pancreatic cancer cells
Celebi, Demet; Baser, Sumeyye; Mahmoudnezhad, Aydin; Ari, Betul; Celebi, Ozgur; Genc, Sidika; Nigde, Esmanur; Karabulut, Kubra; Taghizadehghalehjoughi, Ali
Pancreatic cancer (PC) is one of the most aggressive malignancies of the digestive system, characterized by late diagnosis, resistance to conventional therapies, and poor survival outcomes. Therefore, the development of novel, effective, and targeted therapeutic strategies is urgently needed. This study aimed to evaluate the anticancer potential of Acinetobacter baumannii-derived outer membrane vesicles (OMVs) conjugated with Vaccinium myrtillus extract, a low-toxicity natural compound, against pancreatic cancer cells. For this purpose, V. myrtillus was conjugated with A. baumannii-derived OMVs, and the antimicrobial activity of the conjugate was assessed using disk diffusion, minimum inhibitory concentration, time-kill kinetics, and biofilm inhibition assays. The anticancer effects were investigated by treating PANC-1 pancreatic cancer cells and healthy fibroblast cells with OMVs (50 µg/mL) and increasing concentrations of V. myrtillus (5–250 µg/mL). After 24 h, cell viability and cytotoxicity (MTT, LDH), oxidative stress parameters (TAS, TOS, SOD, GR), PI3K/AKT/PTEN signaling pathway components, apoptotic markers (Annexin V/PI, BAX, Bcl-2, Caspase-8), and inflammatory cytokines (IL-1β, IL-10) were analyzed. The OMV–V. myrtillus conjugate (50 µg/mL OMV +250 µg/mL V. myrtillus) significantly reduced cell viability by approximately 60% through disruption of intracellular redox balance. Elevated oxidative stress triggered apoptotic signaling, approximately increased 50% LDH release, and enhanced inflammatory responses. Especially 50 µg/mL OMV +250 µg/mL V. myrtillus treatment group compared to the control group, which approximately increased to 1-fold IL-1β rate. Furthermore, the 50 µg/mL OMV +250 µg/mL V. myrtillus treatment group showed approximately a 0.75-fold increase in PTEN and BAX gene expression, accompanied by a correlated decrease in AKT and BCL-2 gene expression, compared to the control group. These results suggest that OMV-mediated delivery of V. myrtillus represents a promising synergistic therapeutic approach for treatment-resistant pancreatic cancer.
- ArticleAçık Erişim2026Is bone mineral density a risk factor for femoral stem subsidence in primary cementless total hip arthroplasty: a prospective study
Kalyenci, Ahmet Sinan; Dogan, Ibrahim; Tekin, Saltuk Bugra; Ozmen, Zana; Senel, Ahmet; Ozturkmen, Yusuf
Background: The success of primary total hip arthroplasty (THA) in patiens with primary osteoarthritis (OA) of the hip is significantly influenced by stem osseointegration, migration and implantation. Additionally, the bone mineral density (BMD) of the proximal femur, the femoral morphology and stem design play important roles in these outcomes. This study aimed to evaluate the effect of BMD on subsidence who underwent primary cementless THA with a fit-and-fill stem design for primary OA of the hip, assuming that subsidence is not influenced by BMD. Methods: This prospective study included 72 hips from 67 patients who underwent primary cementless THA for OA between May 2019 and March 2022. Two patients were excluded due to intraoperative complications, and the final analysis was conducted on 70 hips. Patients were grouped according to preoperative BMD and proximal femur anatomy based on Dorr classification. Harris Hip Score (HHS), radiological subsidence and Engh score values were used for postoperative clinical evaluation. Results: The mean age was 65.99 ± 8.10 years (range 52 to 83 years). The mean follow-up was 24.6 ± 5.8 months (range, 12 to 34 months). Amongst 70 OA of the hip cases, 22 (31.43%) were Dorr type A, 44 (62.86%) type B, and 4 (5.71%) type C. Forty-three patients (61.43%) had normal BMD, while 27 patients (38.57%) were osteopenic or osteoporotic. The mean axial migration at the latest follow-up was 1.04 ± 0.69 mm (range 0 to 3.1 mm). Total Engh score was 22.89 ± 3.28 (range 14 to 27), and in terms of stabilization bone ingrowth was seen in all of the femoral stems. There was no statistically significant effect of femoral T-score levels (p = 0.853) or femoral morphologies (p = 0.763) on femoral stem subsidence. Conclusions: No statistically significant differences were observed in clinical or radiological outcomes between patients with normal and low BMD. These findings suggest that early stem migration and osseointegration are more closely related to initial mechanical stability than to BMD. Cementless femoral stems can therefore be considered reliable across different bone qualities, offering an innovative perspective that challenges the conventional emphasis on bone density in implant selection.
- ArticleAçık Erişim2026Turkish validation of the internet addiction test-short form (IAT-7): psychometric properties and age-related differences
Gülden, Çiğdem; Köroğlu, Mustafa
The lack of standardized diagnostic criteria hinders Internet addiction research by forcing reliance on varied measurement tools. The Internet Addiction Test (IAT) remains the most widely used tool for assessing this construct. This study examined the psychometric properties of the Turkish version of the Internet Addiction Test–Short Form (IAT-7) in a sample of 664 students, including 279 college and 385 high school students from Ankara and Erzincan, Türkiye. The findings supported the unidimensional structure of the IAT-7 in the combined sample, demonstrating strong structural validity and stable factorial representation across adolescent and emerging adult groups. The study findings revealed that internet addiction was positively correlated with smartphone addiction, internet gaming disorder, and difficulties in emotion regulation and negatively correlated with self-compassion among both high school students and college students. In addition, while there was a positive correlation between Internet addiction and loneliness among college students, there was no significant correlation between internet addiction and loneliness among high school students. Multi-group confirmatory factor analysis supported configural and metric invariance and partial scalar invariance across high school and college student samples. Cronbach’s alpha, McDonald’s omega, and test-retest correlation coefficients were computed to evaluate reliability. Overall, the Turkish IAT-7 is a reliable, valid, and culturally appropriate instrument for assessing Internet addiction among adolescents and college students, suitable for correlational, regression, and structural modeling applications in educational and research settings.
- Review ArticleAçık Erişim2026From nature to nanoscale: advances, challenges, and preclinical translation of nanofiber drug delivery systems containing plant-derived active ingredients
Polat, Heybet Kerem; Turanlı, Yasin; Kurt, Nihat; Gözcü, Sefa; Tunçel, Emre; Bacanak, Hilal; Aytekin, Eren; Ünal, Sedat
Since the early 1960s, nanotechnology has been a critical area of science, allowing for the development of sophisticated nanomaterials. Nanofibers, one of the most widely used nanotechnological drug delivery systems, have emerged as a highly versatile platform within modern pharmaceutical sciences. By combining various polymers with active herbal ingredients, these systems mimic the natural extracellular matrix and provide improved functions such as a high surface area-to-volume ratio, drug targeting, and controlled drug release. Preclinical studies demonstrate that phytochemical-containing nanofibers have improved therapeutic profiles, including higher anti-inflammatory, antioxidant, antimicrobial, and antineoplastic effects. In various biomedical applications, such as promoting tissue engineering (such as bone and nerve regeneration), limiting tumor growth, and accelerating wound closure, it was shown that nanofibers may overcome the physicochemical limitations of herbal drugs such as low solubility and bioavailability. Despite promising preclinical study results, there are significant obstacles in the way of the commercialization of herbal drug-loaded nanofibers. The difficult standardization of multi-component herbal extracts, stabilization drawbacks, and the absence of scalable industrial manufacturing equipment that can maintain repeatable characterization of nanofibers are some of the major obstacles, in addition to a lack of clinical trials. To navigate the clinical translation of nanofibers, interdisciplinary collaboration regarding quality control, safety, and regulatory pathways is strictly necessary due to the case-by-case review approach utilized by regulatory bodies such as the US Food and Drug Administration (FDA) and European Medicines Agency (EMA). This review offers a comprehensive overview of research on herbal drug-loaded nanofibers and contributes a novel perspective with regulatory and clinical translational insights.
- ArticleYayıncıda açık erişim2026Single and multiple investigation activity potential luteolin against Candida albicans, Escherichia coli and Pseudomonas aeruginosa
Celebi, Demet; Celebi, Ozgur; Baser, Sumeyye; Guler, Mustafa Can; Taghizadehghalehjoughi, Ali; Aydin, Elif; Genc, Sidika; Hacimuftuoglu, Ahmet
Candida albicans is an opportunistic pathogen that can cause invasive infections, especially under conditions of immunosuppression and dysbiosis. Its presence alongside Pseudomonas aeruginosa and Escherichia coli may lead to polymicrobial biofilm-related infections. Due to rising antimicrobial resistance, alternative therapies are being explored, including luteolin, a natural flavonoid with reported in vitro antimicrobial activity. This study evaluated the in vitro antimicrobial and antibiofilm effects of luteolin against C. albicans, E. coli, and P. aeruginosa, both individually and in combination. Methods involved determining minimum inhibitory concentrations, using scanning electron microscopy, fibroblast viability tests, ELISA-based cytokine measurements, and RT-qPCR analysis of key biofilm- and quorum-sensing-related genes (luxS, lasI, and ALS1). MIC values were 0.011 mg/mL for individual strains and 0.046 mg/mL for the polymicrobial mixture. Luteolin treatment reduced microbial adherence and improved fibroblast viability compared to infected controls. Infection increased IL-1β levels and decreased IL-10 levels, effects that luteolin partially reversed. RT-qPCR showed downregulation of selected biofilm-related genes at 2×MIC. These findings demonstrate luteolin’s measurable antimicrobial and anti-biofilm effects in vitro under controlled laboratory conditions, supporting further validation in preclinical models to assess translational potential.
- ArticleYalnız künye2026Synthesis and characterization of novel 5-fluoroindolylmethylene hydrazone derivatives as schiff base compounds: In vitro and in silico evaluation as potential cholinesterase (AChE and BChE) inhibitors
Koprulu, Cigdem; Faydali, Nagihan; Muhammed, Muhammed Tilahun; Dilek, Esra; Kucukoglu, Kaan; Sirinzade, Hanif
This study analyzes the inhibitory effects of newly synthesized compounds of the K1–12 series on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes comparatively using IC50 and Kᵢ parameters. Initially, a series of novel 5-fluoroindolylmethylene hydrazone derivatives (K1–12) were designed and synthesized. The structures of the synthesized compounds were elucidated using 1H and 13C NMR spectroscopy as well as mass spectrometric analyses. Subsequently, their inhibitory effects on AChE and BChE were evaluated in vitro . Molecular docking studies performed for all compounds with AChE and BChE enzymes, and pi interactions and conventional hydrogen bonds were involved in protein-ligand interactions. The molecular dynamics (MD) simulation study of the compound with the highest binding potential to the AChE and BChE structures, K10, disclosed that the complexes obtained from docking would be stable. Moreover, the compound is predicted to have a greater tendency to remain within the binding site of the BChE structure. The density functional theory (DFT) study resulted in similar levels of chemical stability and reactivity for the relatively active compounds. The findings revealed that, especially, the K5 and K10 compounds exhibited higher inhibitory activity than donepezil against BChE and AChE, respectively. The results indicate that these compounds could be potential agents for the treatment of neurodegenerative diseases in the future.
- ArticleYalnız künye2026Esculetin attenuates doxorubicin-induced cardiac toxicity: Evidence from gene expression, enzyme activity, and molecular docking analyses
Demir, Yeliz; Ceylan, Hamid; Yeşilkent, Esra Nur; Kizir, Duygu; Karaman, Melike; Türkeş, Cüneyt; Beydemir, Şükrü
Doxorubicin (DOX) is a potent chemotherapeutic agent whose dose-dependent cardiotoxicity is associated with oxidative stress, inflammation, and enzymatic dysfunction. This study evaluates the cardioprotective potential of esculetin, a natural coumarin derivative, against DOX-induced cardiac injury in rats. Forty-eight male Sprague-Dawley rats were divided into six groups, including control, DOX, esculetin (50 and 100 mg/kg), and combination treatments. DOX markedly altered the expression of oxidative stress-related genes (Ache, Ar, Sord upregulated; Pon1, Gst downregulated) and impaired enzyme activities, accompanied by increased malondialdehyde and depleted glutathione levels. Esculetin administration, particularly at 100 mg/kg, reversed these molecular and biochemical disturbances, restoring antioxidant defense and normalizing gene expression. Molecular docking revealed strong binding interactions of esculetin with the active sites of key enzymes including AR, SORD, AChE, GST, and PON1, supporting its regulatory role. These findings suggest that esculetin exerts multi-targeted protective effects and may serve as a promising candidate for mitigating chemotherapy-induced cardiotoxicity. Further research is warranted to explore its integration into clinical cardioprotective strategies.
- Review ArticleAçık Erişim2026High Tibial Osteotomy (HTO) Versus Unicompartmental Knee Arthroplasty (UKA) in Medial-Compartment Knee Osteoarthritis (KOA): A Critical Narrative Review of Comparative Costs and Cost-Effectiveness
Yapıcı, Furkan
Background: Medial-compartment knee osteoarthritis (KOA) carries substantial disability and long-term cost. High tibial osteotomy (HTO) and unicompartmental knee arthroplasty (UKA) are key joint-preserving or joint-replacing options for selected patients, but their comparative economic ranking remains uncertain. Methods: This critical narrative review synthesized comparative economic evidence on HTO versus UKA for isolated medial-compartment KOA. PubMed and Web of Science were searched as primary sources for English-language studies published from 1 January 2000 to 15 January 2026, while Google Scholar and citation tracking were used supplementarily to identify potentially missed records. Eligible studies were direct economic evaluations or comparative cost/resource studies with clear decision relevance to the HTO–UKA choice. Burden and cost-of-illness studies were used for contextual framing only and were not included in the core comparative synthesis. Results: The direct evidence base was small and methodologically heterogeneous and was dominated by decision-analytic models that differed in perspective, time horizon, utility metric, and assumptions regarding reoperation, revision, and conversion to total knee arthroplasty (TKA). These structural differences largely explain why a U.S. lifetime societal model favored HTO, a UK age-stratified 10-year model produced age-dependent findings, and a recent Canadian public-payer model favored UKA. Observational studies suggest that UKA episode costs can fall substantially in outpatient or ambulatory pathways, whereas HTO costs may rise when reoperations and technique-specific resource use are explicitly captured. Conclusions: Current evidence does not support a context-free economic ranking of HTO and UKA. Because the available studies are heterogeneous and incremental utility differences are often small, the findings should be interpreted cautiously and as scenario-dependent rather than definitive. Future comparative analyses should use contemporary pathway data, transparent and standardized costing, and explicit downstream event definitions for both procedures.
- ArticleAçık Erişim2026The Relationship Between Health Literacy and Attitudes Toward Cancer Screening: An Example from the Easternmost Region of Türkiye
Yildirim, Zeynep; Bozcu, Ebru
Objective: This study aimed to examine the relationship between health literacy and attitudes toward cancer screening and to raise awareness on this issue. Methods: This study was descriptive and correlational in design. The study was conducted with 630 adults aged 30–70 years living in a province located in eastern Türkiye. After excluding incomplete questionnaires, the analyses were conducted with 624 participants. The research data were collected through face-to-face interviews between April 2023 and June 2024 after obtaining the necessary legal permissions. A Descriptive Information Form, the Türkiye Health Literacy Scale (THLS-32), and the Attitudes Toward Cancer Screening Scale were used as data collection tools. The data were analyzed using SPSS 23.0 software; descriptive statistics, correlation analyses, and regression analyses were performed to examine the relationships between variables. Results: The mean health literacy score of the participants was 31.84±10.74, while the mean attitude score toward cancer screening was 89.69±16.82. The scores of the Türkiye Health Literacy Scale (THLS-32) and the Attitudes Toward Cancer Screening Scale differed significantly according to employment status, place of residence, educational level, presence of chronic disease, and previous cancer screening status (P<.05). In addition, a moderate positive and statistically significant relationship was identified between health literacy and attitudes toward cancer screening (r=.450, P<.001). Conclusion: The findings of the study showed that as health literacy levels increased, attitudes toward cancer screening became more positive. This result indicates that health literacy plays an important role in the development of positive attitudes toward cancer screening.
- Review ArticleAçık Erişim2026Current Evidence-Based Clinical Nutritional Approaches in Lipedema: A Scoping Review
Atabilen Pınar, Büşra; Çelik, Menşure Nur; Altıntaş Başar, Hilal Betül; Ağagündüz, Duygu; Karaca, Oya Berkay
Lipedema, a chronic condition primarily affecting women, is characterized by abnormal subcutaneous fat accumulation and swelling in the extremities (while sparing the hands, feet, and trunk). This disease is associated with genetic predisposition, hormonal imbalances, impaired lymphatic function, and vascular dysfunction. Lipedema does not directly cause weight gain, but excess weight can worsen symptoms and accelerate disease progression. Bariatric surgery is considered a treatment option for body weight management and reduction of subcutaneous fat; however, reported studies have indicated that this treatment cannot reduce localized fat accumulation or fat cell hypertrophy or alleviate pain symptoms. Although no proven dietary treatment currently exists, nutrition plays a key role in managing lipedema. Certain dietary approaches such as ketogenic, low-carbohydrate, and modified Mediterranean diets have been explored for weight management and inflammation reduction in lipedema, with studies showing positive effects on body composition and pain. However, according to the current literature no evidence-based nutritional treatments or nutritional supplements are effective in this patient group. Nutritional therapy in lipedema is complicated by frequent comorbidities; therefore, precision nutritional therapy should be planned by evaluating the causes and consequences of the disease. In this review, we evaluated reported studies of current evidence-based clinical nutritional approaches to lipedema treatment.
- ArticleYalnız künye2026The role of adenosine triphosphate in the treatment of linezolid-induced ovarian damage and reproductive dysfunction in rats: An investigation into the pathogenesis
Delibasi, Ilhan Bahri; Yavuzer, Bulent; Suleyman, Bahadir; Gumusburun, Neset; Coban, Taha Abdulkadir; Mendil, Ali Sefa; Uyar, Elif Esra; Yucel, Nurinisa; Suleyman, Halis
Linezolid is an oxazolidinone-derived antibacterial agent that inhibits bacterial protein synthesis by binding to the peptidyl transferase center of the 50S ribosomal subunit. This study investigated whether exogenously administered adenosine triphosphate (ATP) mitigates ovarian damage and reproductive dysfunction induced by linezolid in rats. Forty-eight female albino Wistar rats were randomly assigned to four groups (n = 12 each): healthy control (HG), ATP-only (ATPG), linezolid-only (LZDG), and ATP plus linezolid (ATLDG). ATPG and ATLDG received intraperitoneal ATP (4 mg/kg), whereas HG and LZDG received saline (0.9 % NaCl). One hour later, linezolid (125 mg/kg) was administered orally to LZDG and ATLDG, and the regimen was repeated twice daily for 28 consecutive days. At study end, six rats per group were euthanized for ovarian biochemical, histopathological, and immunohistochemical evaluations; prior to euthanasia (i.p. thiopental sodium, 50 mg/kg), blood was collected for serum prolactin and anti-Müllerian hormone (AMH) analysis. For fertility assessment, the remaining six females per group were co-housed with two proven fertile males for seven days and then monitored for pregnancy for one month. Linezolid exposure increased oxidative stress, caused ovarian tissue injury, decreased AMH, elevated prolactin, and resulted in a 66.7 % infertility rate. ATP co-treatment attenuated these alterations and reduced infertility to 33.3 %. These findings suggest that ATP may provide a protective therapeutic approach against linezolid-induced ovarian toxicity and reproductive dysfunction.
- ArticleAçık Erişim2026Phytochemical evaluation via GC-MS and LC-MS/MS: a comprehensive study of antidiabetic, antimicrobial, antioxidant, and genotoxic activities of extracts from endemic species Centaurea amanicola Hub.-Mor. and C. antitauri Hayek (Asteraceae)
Nobarirezaeyeh, Mohaddeseh; Yuca, Hafize; Aydın, Bilge; Civaş, Ayşe; Karakaya, Songül; Karadayı, Mehmet; Demir, Abdussamed Yasin; Bona, Mehmet; Yılmaz, Bilal; Göger, Gamze
The study investigated the antidiabetic, antimicrobial, antioxidant, and genotoxic activities of extracts from Centaurea amanicola and C. antitauri (Asteraceae). Methanol extracts were analysed for phenolic and fatty oil contents. Major components of fatty oils were identified, including methyl hexadecanoate (48.30%) and heptacosane (22.13%) in C. antitauri, and methyl hexadecanoate (16.29%) and methyl linoleate (13.55%) in C. amanicola. The highest α-amylase inhibition was observed in hexane extracts of both species with 55.53% and 41.57% inhibition values, respectively. Antioxidant activity, measured by ABTS•+ and DPPH• scavenging, varied among extracts, with notable efficacy in C. antitauri dichloromethane extract and C. amanicola ethyl acetate extract. The dichloromethane extract of C. antitauri demonstrated effectiveness against Candida albicans with MIC= 156.25 µg/mL. Importantly, all extracts were found to be genotoxicity-safe. Overall, the findings highlight the potential of these extracts for various medicinal applications, particularly in managing diabetes and combating microbial infections.
- ArticleYalnız künye2026Design, synthesis, in vitro and in silico evaluation of thiazole-hydrazine hybrids incorporating an isoindole-1,3-dione scaffold as potent α-glucosidase inhibitors
Aslan, Osman Nuri; Kalın, Şeyda Nur; Kalay, Erbay; Türkeş, Cüneyt; Demir, Yeliz
In this study, a series of novel hybrid molecules ( TR1–14 ) incorporating a thiazole-hydrazine pharmacophore with a bicyclic isoindole-1,3-dione core were designed and synthesized. All compounds were unambiguously characterized by 1H/ 13C NMR, FTIR, and high-resolution mass spectrometry, and their purities (˃95%) were confirmed by HPLC. The synthesized derivatives exhibited potent α-glucosidase inhibition, with K I values ranging from 0.452 to 1.788 μM. Notably, the most active compound, TR6 ( K I: 0.452 ± 0.093 μM), demonstrated approximately 15-fold greater potency compared to the reference drug acarbose ( K I: 6.748 ± 0.167 μM), highlighting the substantial enhancement achieved through the designed scaffold modification. Structure–activity relationship analysis demonstrated that halogen substitution, particularly with chlorine and bromine, significantly enhances inhibitory potency, presumably due to strengthened hydrophobic and electronic interactions within the enzyme active site. Molecular docking and molecular dynamics simulations supported the experimental findings by revealing a conserved binding mode involving key catalytic residues (Arg600, Asp518, and Met519), as well as stabilizing water-mediated interactions, thereby providing a mechanistic rationale for the observed inhibition. In silico ADME predictions indicated favorable drug-like properties for all compounds, with full compliance with Lipinski's and Jorgensen's rules and substantially improved permeability profiles compared to acarbose. Cytotoxicity analyses demonstrated that TR3 , TR6 , TR10 , and TR11 exhibited low cytotoxic effects at concentrations above 100 μM in non-cancerous human lung epithelial BEAS-2B cells. Especially, TR5 and TR9 did not cause significant cytotoxicity even at a concentration of 200 μM in BEAS-2B cells. Overall, this integrated experimental-computational study identifies thiazole-hydrazine-isoindole hybrids, particularly TR5 and TR6 , as promising lead candidates for further optimization toward the development of next-generation α-glucosidase inhibitors with improved efficacy and drug-likeness.
- ArticleAçık Erişim2026Multitarget biological activities and RP-HPLC-Based phytochemical profiling of Glaucium leiocarpum Boiss.
Altın, Sevgi
This study presents a comprehensive evaluation of the phenolic composition and biological activities of methanolic extracts obtained from the aerial (GLM) and root (GLRM) parts of Glaucium leiocarpum. Phenolic profiling was conducted using reversed-phase high-performance liquid chromatography (RP-HPLC), revealing catechin hydrate, 3-hydroxybenzoic acid, syringic acid, hesperidin, chlorogenic acid, caffeic acid, and trans-cinnamic acid as major constituents in GLM. In contrast, GLRM exhibited a more diverse phenolic profile, including epicatechin, benzoic acid, quercetin, gallic acid, and rosmarinic acid. Antioxidant activities were evaluated using DPPH and FRAP assays, with GLRM demonstrating stronger radical scavenging capacity (IC50: 36.96 µg/mL) and higher ferric reducing power (173.20±0.68 mg TE/g extract). GLRM also contained significantly higher levels of total phenolics (142.81±2.87 mg GAE/g) and flavonoids (76.67±0.72 mg QE/g). Antimicrobial assays demonstrated that only GLRM exerted inhibitory effects against Staphylococcus aureus (8.7±0.57 mm), Enterococcus faecalis (7.7±0.57 mm), and Streptococcus pneumoniae (15.0±0.0 mm). Cytotoxicity studies, assessed by the XTT assay, revealed potent antiproliferative effects against HT-29 colorectal cancer cells (IC50: 3.59 µg/mL for GLM, 2.29 µg/mL for GLRM) and moderate activity against A549 lung carcinoma cells (IC50: 36.01 µg/mL for GLM, 21.99 µg/mL for GLRM). Furthermore, GLRM exhibited strong anticholinesterase activity, with IC50 values of 2.85±0.27 µg/mL for acetylcholinesterase (AChE) and 2.47±0.07 µg/mL for butyrylcholinesterase (BChE). Overall, these findings underscore G. leiocarpum, particularly its root extract, as a valuable source of bioactive secondary metabolites, owing to its rich polyphenolic profile and notable antioxidant, antimicrobial, cytotoxic, and cholinesterase inhibitory activities.
- ArticleYalnız künye2026Inhibitory effect of Vaccinium arctostaphylos L. and Vaccinium myrtillus L. extracts on melanogenesis in α-MSH-induced B16F10 melanoma cells: in vitro, molecular docking ADMET and drug-likeness studies
Güven, Zühal Bayrakçeken; Türkmenoğlu, Burçin
BACKGROUND: Vaccinium species are characterised by high nutritional value and rich phytochemical composition of their fruits and are therefore used as food and in folk medicine. The aim of this study was to investigate the potential of fruits and leaves of the Vaccinium arctostaphylos L. and Vaccinium myrtillus L. for use as cosmeceuticals and against hyperpigmentation-related skin diseases. The antityrosinase and melanogenesis effects were determined by inhibition of mushroom tyrosinase enzyme, inhibition of tyrosinase enzyme in α-MSH (melanocyte-stimulating hormone)-induced B16F10 cells and melanin inhibition. RESULTS: The ethyl acetate sub-extract from the fruits of V. arctostaphylos showed very strong tyrosinase enzyme inhibition (median inhibitory concentration (IC50) = 9.71 μg mL−1), which was approximately as high as that of the standard compound, and also showed significant melanin inhibition and antityrosinase effect compared to kojic acid. The ethyl acetate extracts from the fruits and leaves of V. arctostaphylos showed antioxidant effect as strong as the standard compounds gallic acid and Trolox. The phytochemical contents of fruit and leaf extracts were analysed by liquid chromatography–tandem mass spectrometry (LC–MS/MS). ADMET (absorption, distribution, metabolism, excretion, and toxicity) profiles of the compounds were predicted and their likeness to drug candidates were analysed. Finally, molecular docking analysis was performed with the crystal structures of different targets determined for compounds (rutin, protocatechuic acid, gentisic acid, catechin, chlorogenic acid, caffeic acid, p-coumaric acid, taxifolin, salicylic acid, 4-hydroxybenzoic acid, luteolin-7-glycoside, quercetin). CONCLUSION: The fruit extracts of V. arctostaphylos in particular appear to be a potential and promising source for the cosmeceutical and pharmaceutical industry due to their content of active ingredients and strong biological effect.
- ArticleAçık Erişim2026Bioactive Properties of Achillea biserrata M.Bieb. Extracts: Phytochemical Analysis, Antioxidant Activity, Target Enzyme Inhibition, and Cytotoxic Effects
Güven, Zühal Bayrakçeken; Yilmaz, Mustafa Abdullah; Inceer, Huseyin
In this study, the enzyme inhibition and antioxidant capacity of Achillea biserrata were determined, and their relationship with cytotoxic effects was investigated. Antiproliferative activity was evaluated by the MTT assay in L929, A549, B16F10, Hep-3B, PC-3, MCF-7, and CaCo-2 cell lines, and enzyme inhibition was assessed against tyrosinase, urease, PTP-1B, and DPP-4. Ethanol extracts showed the greatest bioactivity, whereas water extracts were the least active. The capitulum ethanol extract (CEE) exhibited the strongest inhibition of tyrosinase, urease, DPP-4, and PTP-1B (IC50: 72.83, 40.84, 70.12, and 302.42 µg/mL, respectively) and the highest cytotoxicity (IC50: 168.42–325.42 µg/mL). LC-MS/MS analysis identified quinic acid as the major constituent in the stem (44.614 mg/g extract) and capitulum (2.063 mg/g extract), and chlorogenic acid in the leaves (45.502 mg/g extract). Principal component analysis (PCA) integrating LC-MS/MS and bioactivity data supported the bioactive potential of A. biserrata, highlighting its promise as a pharmaceutical resource.
- ArticleYalnız künye2026Solution-phase multifunctional modulation of cholinesterases and carbonic anhydrases by thiourea–pyrimidine benzenesulfonamides: Kinetics and explicit-solvent molecular dynamics
Tok, Fatih; Dumani, Alessia; Güney, Sultan; Abas, Burçin İrem; Kozan, Bensu; Türkeş, Cüneyt; Duran, Hatice Esra; Başoğlu, Faika; Çevik, Özge; Ece, Abdulilah
In aqueous media, enzyme–ligand recognition is shaped not only by direct contacts but also by solvent-mediated interaction networks that persist across time scales. Here, cholinesterases (AChE and BChE) and cytosolic human carbonic anhydrases ( h CA I and h CA II) were investigated as two disease-relevant enzyme systems in solution, and twelve thiourea–pyrimidine benzenesulfonamide derivatives were synthesized and structurally characterized. Enzyme inhibition was quantified by steady-state kinetics; inhibition constants ( K I) were obtained by nonlinear global fitting of untransformed rate data, with Lineweaver–Burk plots used only for visualization. To connect solution-phase inhibition with molecular recognition, docking was validated by redocking (heavy-atom RMSD <2.0 Å across targets), and representative complexes were examined by 500 ns explicit-solvent MD simulations (TIP3P, 0.15 M NaCl, NPT), revealing stable binding modes and persistent, frequently water-mediated interaction patterns consistent with experimental trends. Cellular relevance was assessed in MKN-28 gastric cancer cells with L929 fibroblasts as a non-malignant control. Compounds with improved cytotoxic selectivity toward MKN-28 were identified, and the lead compound ( 11 ) was further evaluated by Annexin V/PI flow cytometry, showing a shift from viable cells toward apoptotic populations under the tested conditions. In silico ADMET profiling suggested moderate lipophilicity across the series, while highlighting elevated polar surface area and compound-dependent toxicity flags as parameters to monitor during optimization. Overall, thiourea–pyrimidine benzenesulfonamides emerge as multifunctional modulators of ChEs and cytosolic h CAs within the applied biochemical and cellular assays.
- ArticleYalnız künye2026Comparative liquid chromatography–electrospray ionization–tandem mass spectrometry profiling and bioactivity evaluation of Ebenus macrophylla Jaub. & Spach leaf, stalk and root extracts: an in vitro and in silico approach
Akman, Tugrul Cagri; Simsek, Samed; Aksit, Zeynep; Aksit, Huseyin; Aydin, Ali; Adem, Şevki; Tufekci, Ali Riza; Yıldız, İlyas
BACKGROUND: Ebenus macrophylla Jaub. & Spach (EM), an endemic Turkish plant, is a rich source of bioactive compounds with potential therapeutic applications. This study aimed to analyze the phytochemistry of its leaf, stalk, and root extracts and evaluate their antioxidant, antimicrobial, enzyme inhibitory, and antiproliferative effects. RESULTS: Liquid chromatography–electrospray ionization–tandem mass spectrometry (LC-ESI-MS/MS) analysis identified 39 phenolic compounds. Among the major phenolics identified, hesperidin (in the leaf and stalk), isoquercitrin (in the leaf), catechin (in all parts), and vanillic acid (in the root) were particularly abundant. The leaf extract showed the strongest antioxidant activity (2,2-Diphenyl-1-picrylhydrazyl (DPPH) Half maximal inhibitory concentration (IC50): 14.08 μg mL−1) and the highest phenolic content (62.27 mg GAE g−1), which is attributed to its high levels of hesperidin and shikimic acid. Antimicrobial assays showed significant activity by the leaf extract against Clostridium perfringens and Pseudomonas aeruginosa (Minimum Inhibitory Concentration (MIC): 31.3 μg mL−1). In enzyme inhibition studies, the leaf extract showed stronger effects than standard inhibitors on α-glucosidase (IC50: 1.56 μg mL−1−1) and tyrosinase (IC50: 18.01 μg mL−1). Molecular docking analyses confirmed that hesperidin forms multiple stabilizing interactions with α-glucosidase and blocks substrate access. Antiproliferative studies showed that the root extract was significantly active against A549, A2780, and HeLa cancer cell lines (Growth Inhibition 50% (GI50): 1.00–3.22 μg mL−1) and minimal toxicity toward normal BEAS-2B cells. CONCLUSION: The distribution of phenolic compounds detected in different plant parts is the main factor determining the strong antioxidant, antimicrobial, antidiabetic, and antiproliferative potential of EM. This study demonstrates that the species is a pharmaceutically promising natural bioactive source and provides the scientific basis for further in vivo research.
