Eczacılık Fakültesi / Faculty of Pharmacy
Permanent URI for this collectionhttps://hdl.handle.net/11727/5700
Browse
48 results
Search Results
Item Chymotrypsin and Trypsin Inhibitory Activity of Some Medicinal Plants Collected from Rize (Türkiye)(Başkent Üniversitesi Eczacılık Fakültesi, 2024-02-25) Gunbatan, Tugba; Sucu, Melike; Gokbulut, Alper; Dilmac, Elif; Gurbuz, IlhanIn this research, the evaluation of in vitro chymotrypsin and trypsin inhibitory activities of ten plant species collected from Rize were aimed, and fractions that showed strong activity were analyzed through HPLC. Daphne pontica L. and Mentha longifolia (L.) L. were found to have the highest chymotrypsin inhibitory activities (87.75 and 84.24 % inhibition). Similarly, the highest trypsin inhibitory activity was observed in D. pontica (%99.93 inhibition), followed by Sambucus ebulus L. flowers (87.47 % inhibition). Extracts showing strong enzyme inhibition were fractioned and subjected to activity tests. The highest chymotrypsin inhibitory activity was observed in the n-hexane fraction of D. pontica (%80.70 inhibition), while the highest trypsin inhibitory activity was found in the n-butanol fraction of S. ebulus (%86.81 inhibition). HPLC studies determined that the 80 % ethanol extract of D. pontica and its dichloromethane and ethyl acetate fractions contained umbelliferone. It was found that chlorogenic acid was present in the 80 % ethanol extracts of S. ebulus flowers. M. longifolia was found to contain chlorogenic acid, caffeic acid, luteolin-7-glucoside, and rosmarinic acid. M. longifolia has been identified as the plant exhibiting the highest antioxidant activity in ABTS and CUPRAC tests, consistent with its high phenolic and flavonoid content.Item Antimicrobial De-Escalation in Intensive Care Unit: Theory and The Reality?(Başkent Üniversitesi Eczacılık Fakültesi, 2024-02-01) Pehlivanli, Aysel; Ozgun, Cigdem; Solmaz, Firdevs Gonca Sasal; Yuksel, Didem; Basgut, Bilgen; Ozcelikay, Arif Tanju; Unal, Mustafa NecmettinItem Antimicrobial Use In Palliative Care Service: A Prevalence Study(Başkent Üniversitesi Eczacılık Fakültesi, 2024-02-01) Bicer, Asim Emre; Pehlivanli, Aysel; Basgut, Bilgen; Ozcelikay, Arif TanjuItem An Essential Problem in Antimicrobial Stewardship: Multi-Drug-Resistant Gram-Negative Bacterial Infection in the Intensive Care Unit(Başkent Üniversitesi, 2024-02-01) Pehlivanli, Aysel; Ozgun, Cigdem; Yuksel, Didem; Solmaz, Firdevs Gonca Sasal; Ozcelikay, Arif Tanju; Unal, Mustafa NecmettinItem The Impact of Clinical Pharmacist in Geriatric Drug-Related Problems: A Scoping Review(Başkent Üniversitesi, 2024-02-01) Ediz, Cigdem; Bicer, Asim Emre; Pehlivanli, Aysel; Basgut, Bilgen; Ozcelikay, Arif TanjuItem Electrospun Hesperidin Nanofibers Induce A Cytoprotective Effect On Sodium-Fluoride Induced Oxidative Stress In Vitro(JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, 2024-03-08) Birer, Mehmet; Kara, Adnan Altug; Yurdakok-Dikmen, Begum; Uyar, Recep; Aralan, Gizem; Birer, Yagmur Turgut; Filazi, Ayhan; Acartuerk, FusunAs a bioactive flavonoid in Citrus seeds, hesperidin exerts significant antioxidant, free radical scavenging, and anticancer activity with limited bioavailability. To enhance the stability and improve the bioactive potential of hesperidin, an electrospun nanofiber formulation was developed. Electrospinning solution was characterized by surface tension, viscosity, and conductivity measurements, and these values were found to be 25.18 +/- 0.04 mN/ m 145 +/- 2 cPs and 9.0 +/- 0.4 mu S/cm, respectively. Electrospun hesperidin nanofiber was tested in a coincubation with the cytotoxic agent sodium fluoride (NaF) in Caco-2 cells. Inhibitory concentration-50 (IC50) values of hesperidin nanofiber in Caco-2 cells alone were as low as 30 mu M, indicating its potential anticancer effect, while coincubation with 10 and 20 mu M of hesperidin nanofibers was found to alleviate the cytotoxic effect induced by NaF at 2.1, 1.05 and 0.525 mM concentrations. This effect was in accordance with cellular antioxidant mechanisms; where malondialdehyde (MDA) levels at 10 mu M hesperidin nanofiber were found to be decreased by 55.60% in the thiobarbituric acid reactive substances (TBARS) assay, and the mRNA expression of Thioredoxin1 (TRX1) and Superoxide dismutase-1 (SOD1) were decreased in qPCR. The results revealed that electrospun nanofiber of hesperidin was developed for the first time with useful implications against cellular toxicity by alleviating the cellular antioxidant defense mechanisms, including MDA, SOD1, and TRX1.Item Cerliponase Alfa Decreases Aβ Load And Alters Autophagy- Related Pathways In Mouse Hippocampal Neurons Exposed To Faβ1-42(LIFE SCIENCES, 2024-11-15) Kose, Selma; Cinar, Elif; Akyel, Hilal; Cakir-Aktas, Canan; Tel, Banu Cahide; Karatas, Hulya; Kelicen-Ugur, PelinExtracellular aggregation of amyloid-beta (A beta) in the brain plays a central role in the onset and progression of Alzheimer's disease (AD). Moreover, intraneuronal accumulation of A beta via oligomer internalization might play an important role in the progression of AD. Deficient autophagy, which is a lysosomal degradation process, occurs during the early stages of AD. Tripeptidyl peptidase-1 (TPP1) functions as a lysosomal enzyme, and TPP1 gene mutations are associated with type 2 late infantile neuronal ceroid lipofuscinosis (LINCL). Nevertheless, there is little information about the role of TPP1 in the pathogenesis of AD; therefore, the present study aimed to measure the decrease in intraneuronal A beta accumulation by a recombinant analog of the TPP1 enzyme, cerliponase alfa (CER) (Brineura (R)), and to determine whether autophagy pathways play a role in this decrease. In this study, endogenous A beta accumulation was induced by fA beta(1-42) (a toxic fragment of full-length A beta) exposure, and mouse hippocampal neuronal cells (HT-22) were treated with CER (human recombinant rhTPP1 1 mg mL-1). Soluble A beta, TPP1, and the proteins involved in autophagy, including mammalian target of rapamycin (p-mTOR/ mTOR), p62/sequestosome-1 (p62/SQSTM1), and microtubule-associated protein 1 A/1B-light chain 3 (LC3), were evaluated using western blotting. The sirtuin-1, beclin-1, and Atg5 genes were also studied using RT-PCR. A beta and TPP1 localizations were observed via immunocytochemistry. CER reduced the A beta load in HT-22 cells by inducing TPP1 expression and converting pro-TPP1 into the mature form. Furthermore, exposure to CER and fA beta(1-42) induced the autophagy-regulatory/related pathways in HT-22 cells and exposure to CER alone increased sirtuin-1 activity. Based on the present findings, we suggest that augmentation of TPP1 with enzyme replacement therapy may be a potential therapeutic option for the treatment of AD.Item New Ester-Containing Azole Derivatives With Potent Anti-Candida Effects: Synthesis, Antifungal Susceptibility, Cytotoxicity, and Molecular Modeling Studies(DRUG DEVELOPMENT RESEARCH, 2024-11) Ataker, Yusuf; Oncue, Ozge; Gulmez, Dolunay; Sabuncuoglu, Suna; Arikan-Akdagli, Sevtap; Sari, SuatMortalities due to mycoses have dramatically increased with the emergence of drug-resistant strains and growing immune-compromised populations globally. Azole antifungals have been the first choice against fungal infections of a wide spectrum and several azole derivatives with ester function were reported for their potentially promising and favorable activity against Candida spp. In this study, we designed and synthesized a series of 1-(aryl)-2-(1H-imidazol-1-yl/1H-1,2,4-triazol-1-yl)ethyl esters, and tested them against seven reference Candida strains using EUCAST reference microdilution method. Among the series, 6a, 6d, and 6g proved highly potent in vitro compared to fluconazole; especially against Candida albicans and Candida tropicalis with minimum inhibitor concentration (MIC) values as low as 0.125 and 0.06 mg/L, respectively, although their activities against Candida krusei and Candida glabrata remained limited. The compounds also showed minimal toxicity to murine fibroblasts according to the in vitro cytotoxicity tests. Molecular modeling predicted 6g as an orally available druglike compound according to all parameters and CYP51 inhibition as the likely mechanism for their antifungal effects. The study underpins the promise of azoles with ester functionality as a potential scaffold for small-molecule antifungal drug design.Item Potent Antimicrobial Azoles: Synthesis, In Vitro and In Silico Study(ANTIBIOTICS-BASEL, 2024-11) Ozdemir, Zeynep; Zenni, Yaren Nur; Karakurt, Arzu; Sari, Suat; Sarac, Selma; Akdag, Mevluet; Merde, Irem Bozbey; Kart, Didem; Venanzoni, Roberto; Flores, Giancarlo Angeles; Angelini, Paola; Kabier, Muzammil; Mathew, Bijo; Carradori, SimoneBackground/Objectives: The increase in fungal infections, both systemic and invasive, is a major source of morbidity and mortality, particularly among immunocompromised people such as cancer patients and organ transplant recipients. Because of their strong therapeutic activity and excellent safety profiles, azole antifungals are currently the most extensively used systemic antifungal drugs. Antibacterial properties of various topical antifungals, such as oxiconazole, which features oxime ether functionality, were discovered, indicating an exciting prospect in antimicrobial chemotherapy. Methods: In this study, eleven new oxime ether derivatives with the azole scaffold (5a-k) were synthesized and tested for their antimicrobial effects using the microdilution method to obtain broad-spectrum hits. Results: Although the title compounds showed limited efficacy against Candida species, they proved highly effective against dermatophytes. Compounds 5c and 5h were the most potent derivatives against Trichophyton mentagrophytes and Arthroderma quadrifidum, with minimum inhibitory concentration (MIC) values lower than those of the reference drug, griseofulvin. The MIC of 5c and 5h were 0.491 mu g/mL and 0.619 mu g/mL against T. mentagrophytes (MIC of griseofulvin: 2.52 mu g/mL). The compounds were also tested against Gram-positive and Gram-negative bacteria. Briefly, 5c was the most active against Escherichia coli and Bacillus subtilis, with MIC values much better than that of ciprofloxacin (MIC of 5c = 1.56 mu g/mL and 1.23 mu g/mL, MIC of ciprofloxacin = 31.49 and 125.99 mu g/mL, respectively). Molecular docking suggested a good fit in the active site of fungal lanosterol 14 alpha-demethylase (CYP51) and bacterial FtsZ (Filamenting temperature-sensitive mutant Z) protein. Conclusions: As a result, the title compounds emerged as promising entities with broad antifungal and antibacterial effects, highlighting the utility of oxime ether function in the azole scaffold.Item Development And Uv-Vis Spectrophotometric Analysis Of An Ease-Of-Use Pediatric Oral Solution Of Dexamethasone For Personalized Therapies(JOURNAL OF RESEARCH IN PHARMACY, 2024-10-02) Enes, Duygu; Fidan, Bilge Basak; Kaplan, Ozan; Dogan, Aysegul; Altinoz, Sacide; Celebier, Mustafa; Kaynak, Mustafa SinanThe usage of dexamethasone for pediatric applications is a well-known issue. In the present study, we developed an oral dexamethasone solution formulation especially aimed for dose-dependent personalized therapies and having excipients known as not harmful to be safely used in pediatrics. The aim of this study was to prepare an easy-of-use pediatric oral solution of dexamethasone and develop an UV/VIS Spectrophotometric method for the evaluation of the stability and quality control of the developed formulation. The primary source of dexamethasone for preparation of the oral pediatric solution was the dexamethasone one-time injectable solutions. This allowed the formulation to be easily prepared in basic laboratory conditions. Dexamethasone content and stability of the formulation were ensured by quantification using the developed UV/VIS Spectrophotometric method validated based on ICH Q2 (R1) guidelines. Simple, fast, reliable, and validated spectrophotometric analysis of dexamethasone was carried out at 269 nm wavelength and the method was linear in a range of 1.00 to 50.00 mu g mL-1.The developed formulation was stable at 4 degrees C at least for three weeks when protected from daylight. The other stability conditions (ambient temperature and -20 degrees C) were also evaluated for the assays. Although the methodology used in this study contains simple processes which can be easily adapted to basic laboratory conditions, the results were satisfactory to prepare an ease-of-use pediatric oral solution of dexamethasonefor personalized medicine. The validated UV/VIS Spectrophotometric method was selective for the formulation and easily applied for the quality control and stability studies of the samples. Such formulations could be helpful for health professionals in managing real-life corticosteroid treatment application problems especially for pediatrics in hospital pharmacy.