Sürdürülebilir Kalkınma Amaçları
Alt birimler
Araştırmacılar(20)
- Akman, Tugrul Cagri
- Akşit, Hüseyin
- Aydemir, Emircan
- Baser, Sumeyye
- Colak, Suat
- Dilek, Esra
- Elmastas, Mahfuz
- Erken, İrem Nisa
- Gergin, Ömer
- Gursoy, Sule
- Gülaboğlu, Mine
- Karakoç, Barış
- Kılıç, Engin
- Özli, Semih
- Taşkor Önel, Gülce
- Türkeş, Cüneyt
- Türkmenoğlu, Burçin
- Yıldırım, Sümeyra Tuna
- Yılmaz, Ali Osman
- Yilmaz, Mustafa Abdullah
Birim yayınları
314 →- ArticleAçık Erişim2027From extraction to ocular delivery: An integrated approach using apigenin and apigenin 7-O-glucoside nanosuspensions to treat corneal neovascularization
Aytekin, Eren; Gözcü, Sefa; Polat, Heybet Kerem; Akşit, Hüseyin; Karakuyu, Nasıf Fatih; Kurt, Nihat; Sofu, Gülşah Usta; Akkaya, Züleyha Yalnız; Tebrizi, Behzat; Çalış, Sema
Corneal neovascularization (CV) is a vision-threatening condition characterized by the pathological ingrowth of blood vessels. While corticosteroids and anti-VEGF agents are standard treatments, their prolonged use is associated with significant ocular side effects. This study aimed to develop and optimize nanosuspensions of Apigenin (APG) and Apigenin-7-O-glucoside (APG 7) to enhance their ocular bioavailability and evaluate their efficacy in the treatment of CV. APG and APG 7 were isolated from Petroselinum crispum . Nanosuspensions were formulated using an anti-solvent precipitation method, optimized via a 23 factorial design considering PVA concentration, Span 80 concentration, and homogenization speed. The physical properties, including particle size, PDI, and zeta potential, were characterized. In vivo efficacy was assessed over a 7-day treatment period in an alkali-burn induced rat CV model through clinical scoring, histopathology, and immunohistochemical analysis of VEGFA and IL-6 expression. The optimized APG nanosuspensions exhibited a mean particle size of ∼166.9 nm with high stability. In vivo studies demonstrated that 0.05% APG nanosuspension significantly inhibited corneal angiogenesis, reduced stromal edema, and downregulated VEGFA and IL-6 expression compared to the untreated injury group (p < 0.05). Conversely, APG 7 formulations failed to show significant therapeutic efficacy, likely due to limited corneal permeability attributed to the glycoside moiety. The 0.05% APG nanosuspension presents a promising, non-invasive therapeutic alternative for CV management, offering effective anti-angiogenic activity with improved ocular delivery characteristics.
- ArticleYalnız künye2027Synthesis, structural characterization, and in vitro and in silico anticancer evaluation of chalcone-based heterocyclic and boron difluoride derivatives
Serdaroğlu, Vildan; Demir, Fatma; Aydın, Ali; Türkmenoğlu, Burçin; Kahriman, Nuran
In this research, a series of novel bioactive heterocyclic polar compounds were designed and synthesized by incorporating various functional groups to enhance their biological and functional properties. The work involved the synthesis of chalcone (1–9, 10–18), boron difluoride complex (19–21), pyrazoline (22–25), and pyrimidine (26–37) compounds with their structures characterized through spectral techniques including NMR (1H, 13C (APT), 1H–1H COSY), FT-IR spectroscopies, LC-MS spectrometry. The anticancer potential of all compounds was assessed using lung cancer cell lines (A549, Calu1, H1650), brain cancer cell lines (A172, C6, B35), as well as normal lung (Beas2B) and chondrocyte (HC) cell lines. Compounds exhibiting a GI50 value below 3.0 µg/mL and a TGI value under 100 µg/mL were classified as having anticancer activity, based on comparisons with the reference drug 5-fluorouracil (5FU). Overall, compounds 24, 34, and 36 emerged as the most promising lead candidates by combining potent antiproliferative activity, favorable GI50-derived selectivity indices, and low toxicity toward normal cells, whereas compounds 2, 32, and 35 demonstrated the highest overall biological potency across multiple cancer cell lines. Representative GI50 values as low as 1.0–1.2 µg/mL, TGI values as low as 1.3–2.5 µg/mL, and LC50 values generally exceeding 500 µg/mL in normal cell lines were obtained in the most responsive models, supporting the potential of these derivatives for further anticancer development. To support these detailed in vitro studies, the most active compounds targeting TP53, EGFR, Akt1, mTOR, ERK2, and caspase 3, which are effective in lung and brain cancer pathways, were interacted via in silico molecular docking. Through molecular docking, the interaction values of compounds 2, 6, 7, 8, 13, 14, 17, 18, 24, 27, 32, 35, 36, and 37 with the determined targets were calculated, and their potential as promising lead candidates for drug development was analyzed.
- ArticleYayıncıda açık erişim2026Investigation of the Effect of Akkermansia muciniphila Muc T (ATCC BAA-835) on TLR4/NF-Kappa B/NLRP2 Signaling Pathway and Intestinal Microbiota in Diarrhea-Predominant Irritable Bowel Syndrome in Rats
Ucar, Mahmut; Celebi, Demet; Celebi, Ozgur; Baser, Sumeyye; Guler, Mustafa Can; Tanyeli, Ayhan; Kılıclıoglu, Metin; Yıldırım, Serkan
Diarrhea-predominant irritable bowel syndrome (IBS-D) is a functional gastrointestinal disorder associated with gut microbiota dysbiosis, intestinal barrier dysfunction, and low-grade inflammation. This study aimed to evaluate the effects of Akkermansia muciniphila Muc T (ATCC BAA-835) on gut microbiota composition, intestinal barrier integrity, and TLR4/NF-κB/NLRP2-mediated inflammatory signaling in a stress-induced rat model of IBS-D. IBS-D was induced in rats using combined chronic and acute stress paradigms. Animals received A. muciniphila supplementation during the experimental period. Serum inflammatory cytokines and tight junction–related proteins were quantified by ELISA. Protein expression levels of TLR4, NF-κB, and NLRP2 were assessed by Western blotting. Gut microbiota composition was analyzed using 16 S rRNA gene sequencing of fecal samples. Histopathological and immunofluorescence analyses were performed to assess tissue inflammation and cellular damage. IBS-D rats exhibited increased inflammatory cytokine levels, impaired tight junction protein expression, activation of the TLR4/NF-κB/NLRP2 pathway, and significant alterations in gut microbiota diversity. A. muciniphila supplementation significantly attenuated inflammatory responses, restored intestinal barrier–associated proteins, and suppressed inflammatory signaling. Microbiota analysis revealed partial correction of dysbiosis, including increased abundance of beneficial taxa such as Faecalibacterium prausnitzii. A. muciniphila alleviates IBS-D–associated intestinal inflammation and barrier dysfunction by modulating gut microbiota composition and inflammatory signaling pathways, supporting its potential as a microbiota-based therapeutic strategy for IBS-D.
- ArticleAçık Erişim2026Phytochemical profiling of Artemisia absinthium essential oils from different regions of Türkiye and preliminary evaluation of their antibacterial and honeybee locomotor effects
PORTAKAL, Pınar; TUFEKCI, Ali Rıza; ARSLAN, Okan Can; AKŞIT, Hüseyin; GÖÇERI, Ali; KÜRSAT, Murat
This study aimed to determine the phytochemical composition of essential oils obtained from Artemisia absinthium collected in Sivas (AAS), Erzincan (AAE) and Hakkari (AAH) and to evaluate their effects on honeybee locomotor activity. The chemical composition of the essential oils was analyzed by GC–MS, revealing notable regional differences. Chamazulene was identified as the predominant compound in all samples, with the highest concentration in AAH (64.6%), while AAE was characterized by a high β-thujone content (18.3%). Locomotor activity assays showed no significant differences between control and treated groups over a 24-hour period (H (3) = 4.270, p=0.234; F (3,121)=0.867, p=0.460), indicating no detectable acute locomotor alterations under the tested conditions. The antibacterial activity of the essential oils was evaluated using the disc diffusion method against both Gram-positive and Gram-negative bacteria. Antibacterial effects varied depending on the oils' geographical origin and chemical composition. AAE and AAS essential oils showed comparatively larger inhibition zones, particularly against Staphylococcus aureus and Bacillus cereus, whereas AAH showed selective activity against Pseudomonas aeruginosa. No inhibition of Listeria monocytogenes was observed with any of the tested oils. Overall, the oils' antibacterial activity was moderate and selective compared with the positive control, imipenem. These findings suggest that regional variation significantly influences the chemical composition and biological activity of A. absinthium essential oils. Furthermore, the tested oils did not produce detectable acute locomotor alterations in honeybees under the conditions tested. These findings provide preliminary insight into the relationship between regional phytochemical variability and the biological properties of A. absinthium essential oils.
- ArticleAçık Erişim20261,4-Naphthoquinone thiazole urea hybrids bearing morpholine/piperazine: synthesis, crystal structure, aldose reductase and α-glycosidase enzyme inhibition, molecular docking, and electrochemical interaction with dsDNA
Efeoglu, Cagla; Sadak, Selenay; Sahin, Ertan; Demir, Yeliz; Türkeş, Cüneyt; Uslu, Bengi; Nural, Yahya
In this study, new 1,4-naphthoquinone thiazole urea hybrids bearing morpholine (3a–d) or piperazine (3e–h) moiety were synthesized in 76–89 % yields and characterized by 1H NMR, 13C NMR, FT-IR, HRMS, and elemental analysis. The stereochemistry of 3d was determined by single crystal x-ray diffraction study. We evaluated the inhibitory potential of these compounds 3a–h on aldose reductase (ALR2) and α-glycosidase enzyme (α-GLY) activity. Our results indicate that these compounds substantially inhibit ALR2 at micromolar doses, with inhibition constants (KIs) between 0.79 and 2.20 μM and inhibit α-GLY KI between 0.67 and 2.82 μM. Molecular docking simulations were utilized to elucidate inhibitory effects and establish structure-activity relationships for the synthesized compounds. DNA interaction studies are of great importance for the synthesis of new drugs and for studying the behavior and mechanisms of action of synthesized drug molecules. Herein, the interaction of 3d selected as a model compound with ct-dsDNA was investigated in the solution phase by the electrochemical method of differential pulse voltammetry (DPV). The decrease in the peak current value of 3d after the addition of the DNA solution confirmed the interaction. Limits of detection (LOD) and quantification (LOQ) for the interaction were found to be 0.099 ppm and 0.327 ppm in the concentration range of 0.348 ppm to 0.739 ppm, respectively. To determine the binding constant, cyclic voltammetry (CV) was utilized and found to be 8.6 × 102 M−1. Additionally, the type of interaction between the 3D molecule and DNA was investigated and supported by molecular docking and Fourier transformed infrared spectroscopy (FTIR).
- ArticleAçık Erişim2026Isovanillin-derived bis-hydrazones as dual cholinesterase and carbonic anhydrase inhibitors: synthesis, enzymatic profiling, and computational insights from molecular docking and dynamics
Türkeş, Cüneyt; Yapar, Gönül; Duran, Hatice Esra; Lolak, Nebih; Akocak, Suleyman
Aims: To develop isovanillin-based bis-hydrazones as multitarget inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I/II (hCA I/II). Materials & methods: Twelve bis-hydrazones (4a–4l) were synthesized in two steps and evaluated by spectrophotometric enzyme assays, Lineweaver–Burk kinetics, molecular docking, MM-GBSA, molecular dynamics simulations, and in silico ADME/Tox profiling. Results: All compounds showed nanomolar inhibition. Compound 4d was the most potent AChE/BChE inhibitor (KI = 10.46 and 3.56 nM), while 4a and 4j led the hCA I/II panel (KI = 3.46 and 16.12 nM). Docking, MM-GBSA, and molecular dynamics supported dual-site cholinesterase engagement and non-zinc, peripherally anchored hCA inhibition. Conclusions: Isovanillin-based bis-hydrazones, particularly 4d, 4a, and 4j, represent promising multitarget leads for cholinergic and hCA-linked disorders.
- ArticleYalnız künye2026Chemical Composition and Antibacterial Activity of Rosa villosa subsp. mollis R. Keller & Gams., Rosa hemisphaerica J. Herrm. and Natural Hybrid Rosa ozcelikii Korkmaz & Kandemir Essential Oil
Gözcü, Sefa; Akşit, Zeynep; Akşit, Hüseyin; Şimşek, Samed; Korkmaz, Mustafa
This study explores the essential oils (EOs) of Rosa hemisphaerica (RH), Rosa villosa subsp. mollis (RV) and the newly identified hybrid Rosa ozcelikii (RO). The major components of the EOs were found to be nonadecane (22.45%), viridiflorol (19.37%) and heneicosane (11.72%) in RH; α-muurolene (14.72%), σ-cadinene (17.88%) and farnesol (9.94%) in RV; and heptacosane (27.63%), heneicosane (12.42%) and α-citronellol (11.90%) in RO. Antibacterial activities were evaluated using the disc diffusion method. The EOs demonstrated moderate antibacterial effects: RV and RH exhibited inhibition zones of 8.0 ± 0.4 mm against Pseudomonas aeruginosa, while RO showed stronger activity with inhibition zones of 11.0 ± 0.5 mm against Staphylococcus aureus, 12.0 ± 0.4 mm against Clostridium perfringens and 9.0 ± 0.5 mm against Bacillus cereus. These findings highlight the chemical diversity and potential therapeutic applications of these Rosa species, emphasising their relevance in the search for natural antimicrobial agents.
- ArticleAçık Erişim2026Evaluation of the Efficacy of Acarbose on Ovarian Microbiota Profile, Ovary–Gut Axis, and SAP (1–10) Gene Expression in Rats Administered With Candida albicans Exosomes
Dabanlioglu, Bulent; Celebi, Demet; Celebi, Ozgur; Baser, Sumeyye; Guler, Mustafa Can; Tanyeli, Ayhan; Ari, Betul; Kalayci, Sıla Ektas; Fakirullahoglu, Mesud; Kiliclioglu, Metin
Candida albicans is a commensal fungus of the vaginal and reproductive tract microbiota, but its overgrowth contributes to mucosal infections and reproductive dysfunctions. The fungus secretes exosomes carrying virulence factors, including secreted aspartyl proteinase (SAP) genes, which are critical for tissue invasion and immune modulation. Acarbose, an α-glucosidase inhibitor, has been shown to suppress C. albicans biofilm formation and hyphal transition. This study is aimed at evaluating the effects of acarbose on the ovarian microbiota, gut–ovary axis, and SAP gene expression profile in a rat model following exposure to C. albicans exosomes. Rats were divided into two groups: the control group received intraperitoneal C. albicans exosomes (8 log10 CFU/mL), whereas the acarbose group received the same exosomes followed by oral acarbose (25 mg/kg/day). Exosomes were characterized by NTA and SEM. Ovarian tissue gene expression (SAP1–10) was analyzed by qRT-PCR. Inflammatory cytokines and tight junction proteins were assessed via ELISA, and microbiota composition was determined using 16S rRNA sequencing. Acarbose significantly reduced IL-8 and TNF-α levels while increasing IL-10, ZO-1, claudin-5, and occludin expression compared with Candida-infected controls (p < 0.05). Gut microbiota diversity and classification success were higher in the acarbose group, indicating microbial balance restoration. Acarbose mitigated C. albicans exosome-induced inflammation and barrier dysfunction while enhancing microbial diversity, suggesting its potential role in modulating the ovarian–gut axis and reducing fungal virulence through SAP gene suppression.
- ArticleYalnız künye2026Novel Imino Derivatives of Thymol: Synthesis, in vitro Cytotoxic Activities, Molecular Docking Analysis and ADME Prediction
Başaran, Eyüp; Türkmenoğlu, Burçin; Akkoc, Senem
Cancer is a significant global health challenge that affects millions of individuals every year. The development of new anticancer drugs is imperative to address the issue of drug resistance in cancer therapy. Therefore, in this study, novel imino derivatives of thymol (3a-c) were synthesized and evaluated as anticancer agents. These compounds were structurally elucidated using elemental analysis and various spectroscopic methods, including 1H and 13C Nuclear Magnetic Resonance (NMR) and Fourier Transform Infrared Spectroscopy (FT-IR). The cytotoxic activities of the new compounds on human liver cancer (HepG2) and healthy human kidney (HEK-293T) cell lines were investigated. Compounds were tested at various concentrations to determine their IC50 values. Among the tested new compounds, 3a and 3b demonstrated cytotoxicity in HepG2, with IC50 values of 88.97 µM and 106.10 µM, respectively. Furthermore, compound 3a also exhibited significant toxicity against the HEK-293T cell line, suggesting that further modifications are needed to improve selectivity for healthy cells. ADME properties analysis resulted in the detection of two lead compounds (3a and 3b) among compounds 2a-c and 3a-c. For the most active compounds 3a and 3b, molecular docking study on epidermal growth factor tyrosine kinase receptor (PDB ID: 3POZ), PI3K alpha (PDB ID: 4FA6), c-kit tyrosine kinase (PDB ID:1T46) was performed to verify the in vitro experimental results.
- ArticleYayıncıda açık erişim2026Evaluation of gossypetin’s effects on gut microbiota profile and TLR4, Myd88, NFKB, and NLRP3 signaling pathways in rats
Akkas, Onder; Celebi, Demet; Celebi, Ozgur; Baser, Sumeyye; Kalayci, Sıla Ektas; Ari, Betül; Guler, Mustafa Can; Dabanlıoglu, Bulent; Celebi, Selahattin; Kılıclıoglu, Metin
Gut microbiota plays a crucial role in maintaining host homeostasis by regulating metabolic processes and immune responses. Disruptions in microbial composition are closely associated with inflammatory diseases and are often linked to the activation of key signaling pathways such as Toll-like receptor 4/myeloid differentiation primary response 88/nuclear factor kappa TLR4/MyD88/NF-κB and NLR family pyrin domain-containing 3 (NLRP3) inflammasome. Natural bioactive compounds, particularly flavonoids, have gained attention due to their potential to modulate both gut microbiota and inflammation-related pathways. In this context, the present study aimed to evaluate the effects of gossypetin on gut microbiota composition and its regulatory role on TLR4, MyD88, NF-κB, and NLRP3 signaling pathways in a rat model. Adult female Wistar albino rats were divided into control and gossypetin-treated groups (50 mg/kg, oral gavage/56 days dose). Gut microbiota was analyzed by 16S rRNA sequencing, and protein expression levels were assessed using Western blot. Histopathological, immunohistochemical, and immunofluorescence analyses were also in liver, intestinal, and spleen tissue performed. Gossypetin administration reduced microbial diversity and altered microbiota composition, with increases in Mediterraneibacter spp., Blautia spp., and Lactobacillus spp. Western blot results showed significant decreases in NLRP3 (p ≤ 0.01) and NF-κB (p ≤ 0.05) levels, while TLR4 and MyD88 remained unchanged. Histological analyses revealed mild tissue alterations and increased oxidative stress markers. These results suggest that gossypetin modulates microbiota composition and exerts selective anti-inflammatory effects, highlighting its potential in microbiota-associated inflammatory regulation.
Tam Kayıt
| Alan | Değer | Dil |
|---|---|---|
| dc.date.accessioned | 2026-10-21T10:21:54.175495069Z | |
| dc.date.available | 2026-10-21T10:21:54.175495069Z | |
| dc.identifier.uri | https://rdlopen.rawdatalibrary.net/r/ebyu/28102 | |
| dc.rights | info:eu-repo/semantics/openAccess | |
| dc.title | Temel Eczacılık Bilimleri Bölümü | tr |
| dspace.entity.type | OrgUnit | |
| organization.identifier.code | eczacilik-temel-eczacilik-bilimleri | |
| organization.unitType | department | |
| rdl.unit.alias | \btemel eczacilik bilimleri bolumu\b |





