Eczacılık Fakültesi / Faculty of Pharmacy
Permanent URI for this collectionhttps://hdl.handle.net/11727/5700
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Item Anti-Tyrosinase and Antimelanogenic Effect of Cinnamic Acid Derivatives from Prunus Mahaleb L.: Phenolic Composition, Isolation, Identification And Inhibitory Activity(2023) Guven, Zuhal Bayrakceken; Saracoglu, Iclal; Nagatsu, Akito; Yilmaz, Mustafa Abdullah; Basaran, A. Ahmet; 36924865; AAI-6606-2021Ethnopharmacological relevance: The traditional use of Prunus species against skin diseases and especially for skin lightning cosmeceutical purposes is widespread in many cultures. Prunus mahaleb L. is a well known food plant and used in the baking industry for flavoring. The fruit kernels (endocarp) are used in India for hyperpigmentation. Aim of the study: To investigate the chemical composition with the antimelanogenesis effect of P. mahaleb seed and kernel extracts and isolated compounds. Materials and methods: Isolation studies performed from the methanol extracts obtained from kernels and structures were determined using NMR and MS analysis. Antimelanogenesis effect was determined by mushroom tyrosinase assay, cellular tyrosinase assay and melanin content assay using B16F10 murine melanoma cells. Results: Five cinnamic acid derivatives were isolated and their structures (2-O-& beta;-glucopyranosyloxy-4-methoxyhydrocinnamic acid (1), cis-melilotoside (2), dihydromelilotoside (3), trans-melilotoside (4), 2-O-& beta;-glucosyloxy4-methoxy trans-cinnamic acid (5)) were elucidated using advanced spectroscopic methods. Mushroom tyrosinase enzyme inhibition of extracts, fractions and pure compounds obtained from P. mahaleb kernels were investigated and structure-activity relationship revealed. According to a detailed, comprehensive and validated LC-MS/MS technique analysis, vanilic acid (41.407 mg/g), protocatechuic acid (8.992 mg/g) and ferulic acid (4.962 mg/g) in the kernel ethylacetate fraction; quinic acid (14.183 mg/g), fumaric acid (8.349 mg/g) and aconitic acid (5.574 mg/g) were found as major phenolic compounds in the water fraction. The correlation of trace element copper content in extracts and fractions with mushroom enzyme activity was determined. By examining the enzyme kinetics of the compounds with effective cinnamic acid derivatives, inhibition types and enzyme binding constants Ki were calculated. Compounds 1,3 and 5 exhibited high noncompetitive tyrosinase inhibitory activity against L-tyrosine substrates, with IC50 values of 0.22, 0.31 and 0.37 mM respectively. In addition compounds 1, 3 and 5 showed dose-dependent inhibitory effects on intracellular tyrosinase and melanin levels in & alpha;-melanocyte-stimulating hormone (& alpha;-MSH)-induced B16F10 melanoma cells. Conclusions: Potent tyrosinase inhibitory compounds and extracts of P. mahaleb kernels suggest that it could be a new, non-toxic and inexpensive resource for the cosmeceutical industry and in skin diseases associated with hyperpigmentation.Item Evaluation of Possible Immunomodulatory Changes in Carbon Monoxide Poisoning(2023) Girgin, G.; Teksam, O.; Ozgunes, H.; Baydar, T.; Sabuncuoglu, S.Item Community Pharmacists Preparedness and Barriers for Cancer Health Promotion in North Cyprus(2023) Bosah, Dubem Henry; Birand, Nevzat; Basgut, Bilgen; https://orcid.org/0000-0002-5883-5583; 35234102; JKS-4834-2023Introduction The role of a community pharmacist is well recognized in the literature as the most accessible health care provider that promotes health wellness and disease prevention. Evidence supports their role in cancer health promotion though this is not seen yet in practice. The aim of the study was to assess community pharmacists' preparedness in terms of knowledge, role perception and barriers for providing cancer health promotion in North Cyprus. Methods A cross-sectional face-to-face questionnaire-based study was carried among a randomly selected representative sample of community pharmacists in North Cyprus between June 2020 and August 2020. A pre-validated 31-item questionnaire tool was revised by an expert panel and adopted for purpose of this study. Results 200 (64.5%) out of 310 approached community pharmacists' have accepted and responded to the questionnaire of which 183 were fully answered. The community pharmacists' awareness of cancer was moderate, as 70% answered correctly. Most respondents (93.4%) agree that pharmacists should be involved in cancer health promotion. Most respondents (> 90%) agree that pharmacist's lack of interest in oncology, lack of educational material and pharmacist's hesitancy about their knowledge of cancer are respectively the most important barriers for cancer health promotion. Conclusion The study shows that community pharmacist well perceives their role in cancer health promotion despite moderate awareness of cancer related facts and hesitancy of their knowledge necessary for assuming their role. Lack of interest, motivation and cancer educational materials availability are also major barrier to address.Item A Bayesian Estimation Framework for Pharmacogenomics Driven Warfarin Dosing: A Comparative Study(2015) Oztaner, Serdar Murat; Temizel, Tugba Taskaya; Erdem, S. Remzi; Ozer, Mahmut; 0000-0002-7537-2170; 25020183; AAJ-2370-2021The incorporation of pharmacogenomics information into the drug dosing estimation formulations has been shown to increase the accuracy in drug dosing and decrease the frequency of adverse drug effects in many studies in the literature. In this paper, an estimation framework based on the Bayesian structural equation modeling, which is driven by pharmacogenomics, is proposed. The results show that the model compares favorably with the linear models in terms of prediction and explaining the variations in warfarin dosing.Item Ritonavir Nanosuspensions Prepared By Microfluidization With Enhanced Solubility And Desirable Immunological Properties(2022) Karakucuk, Alptug; Canpinar, Hande; Celebi, Nevin; https://orcid.org/0000-0002-6402-5042; 35924723The objective of this study was to develop ritonavir (RTV) nanosuspensions (NSs) by microfluidization method. Particle size (PS) measurements were performed by photon correlation spectroscopy. Amorphous properties of the particles were evaluated by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The dissolution studies were conducted in fed state simulated intestinal fluid (FeSSIF) medium. The flow cytometry was utilized to determine the lymphocyte sub-groups and immune response of NSs. RTV NSs were obtained with 400-500 nm PS. The crystal properties of RTV remain unchanged. The solubility of NS was enhanced five times. 57% and 18% of RTV were dissolved in FeSSIF medium for NSs and coarse powder. According to immunological studies, the prepared NSs did not significantly alter the ratio of CD4(+)/CD8(+). Therefore, NSs may be a beneficial approach for the oral administration of RTV.Item Cyclodextrin-Based Nanogel Of Flurbiprofen For Dermal Application: In Vitro Studies And In Vivo Skin Irritation Evaluation(2022) Oktay, Ayse Nur; Celebi, Nevin; Ilbasmis-Tamer, Sibel; Kaplanog, Guelnur TakeThe aim of this study was to develop and characterize flurbiprofen (FB)-loaded cyclodextrin (CD) based nanogel formulations for dermal application. Nanogels were produced via emulsification solvent evaporation and then incorporated into a hydroxypropyl methyl cellulose (HPMC) gel. The visual examination, pH, viscosity, dynamic rheological measurements and drug content analysis of nanogels were assessed. In vitro and ex vivo permeation, stability, and skin irritation were performed. pH of the FB-loaded nanogel and the nanogels in HPMC were 10.6 +/- 0.1 and 7.5 +/- 0.1 (neutral) respectively. The highest and lowest viscosities were observed in FB-loaded nanogels and in FB-free nanogels in HPMC, respectively. The tangent delta and storage modulus values of FB-loaded nanogel in HPMC were higher than those of FB-loaded nanogel. FB from nanogels in HPMC was 100% by 48 h. The final nanogel formulation was physically and chemically stable over 12 months. Skin irritation test showed no skin irritation or cellular infiltration on the histological level. In vitro and ex vivo permeation showed that the nanogels could be effective and stable formulations, especially in the dermal application of a hydro-phobic molecule.Item Test Performance Of Self-Report Adherence Tools In Patients With Hypertension: A Systematic Review And A Meta-Analysis(2022) Al-Alaili, Mohammed Khaled; Abdi, Abdikarim Mohamed; Basgut, Bilgen; 000888656300001What Is Known and ObjectivesAdherence has proved to have a positive influence on achieving plausible treatment outcomes. Self-report questionnaires are widely used in evaluating adherence, creating thus a high-powered research field. This review aims to provide an update of scales used in hypertension, which are compared and analysed against reliability and validity. MethodsPubMed, Web of Science and Cochrane Library were searched in May 2022 to identify studies. We extracted the study characteristics and evaluated their quality. A random-effects model with subgroup analysis was used to calculate estimates and heterogeneity parameters as well as regressions, funnel and forest plots. A bivariate model was selected to conduct validity analyses and draw receiver operating characteristic (ROC) curves. Results and DiscussionFifty-five articles were identified and classified into 22 different reliable and validated tools. Pooled analyses predicted an overall good Cronbach's alpha of 0.76 (95%CI:0.67-0.83), a good ICC of 0.8 (95%CI:0.72-0.86) and an excellent correlation coefficient of 0.91 (95%CI:0.86-0.95), which all showed high heterogeneity and slight detection of asymmetry. Regression analyses showed that only time and the number of items/scale type influenced significantly retest and alpha, respectively. Overall validity showed acceptable sensitivity of 0.65 (95%CI:0.53-0.75) and specificity of 0.57 (95%CI:0.47-0.67) with a good Area Under Curve (AUC) of 0.637. Upon comparison, four tools showed superiority over Morisky's scale. What Is New and ConclusionAdherence is a multi-dimensional phenomenon, which deems scales to be highly variable or complex; thus, complicating the selection process. Adherence to Refills and Medications Scale (ARMS) is the most promising free non-inferior alternative to Morisky, the most used scale.Item Food plant with antioxidant, tyrosinase inhibitory and antimelanoma activity: Prunus mahaleb L(2022) Guven, Zuhal Bayrakceken; Dogan, Zeynep; Saracoglu, Iclal; Picot, Laurent; Nagatsu, Akito; Basaran, A. AhmetPrunus mahaleb L. seeds are used as spice and folk remedies in many countries. The aim of this study was bioactivity guided isolation and characterization phytoconstituents of P. mahaleb which have been studied very limited so far. The antioxidant capacities of seed and kernel (endocarp) extracts were studied by DPPH, nitric oxide (NO), superoxide (SO), TEAC, CUPRAC methods. The antiproliferative activity were investigated for the first time against B16F10, A2058, HeLa and L929 cell lines using MTT assay. Gallic acid and ursolic acid which have strong antioxidant and cell growth inhibitory effect, were isolated from the most active fractions. From the inactive fractions, quercetin-3-O(2-O,6-O-alpha-dirhamnopyranosyl beta-glucopyranoside), kaempferol-3-O(2-O,6-O alpha-dirhamnopyranosyl beta-glucopyranoside) and beta-sitosterol-3-O-beta-glucopyranoside were isolated. Our study is the first record for the isolation of ursolic acid from all parts of P. mahaleb, gallic acid from P. mahaleb kernels, two flavonol triglycosides from the Prunus species and their analysis by advanced NMR spectroscopic methods. Ursolic acid (IC50 : 170.2 mu M) and gallic acid (IC50 : 10.5 mu M) showed strong tyrosinase inhibition, gallic acid being 5.4 times more effective than standard compound. Kernel extracts have strong antioxidant activity, showed high growth inhibitory activity with dose-dependent manner on melanoma cells but no growth inhibitory on healthy L929 and HeLa cancer cells. The high antioxidant capacity of kernel, its selective growth inhibition of B16F10 and A2058 melanoma cells and its strong tyrosinase inhibitory compounds suggest that it could be a new, non-toxic and inexpensive resource for melanoma treatment and cosmetic industry.Item Theoretical and experimental investigation of 1,4-dihydropyridine-based hexahydroquinoline-3-carboxylates: Photophysics and bovine serum albumin binding studies(2022) da Luz, Lilian Camargo; Gunduz, Miyase Gozde; Beal, Roiney; Zanotto, Gabriel Modernell; Kuhn, Eduardo Ramires; Netz, Paulo Augusto; Safak, Cihat; Bruno Goncalves, Paulo Fernando; Santos, Fabiano da Silveira; Rodembusch, Fabiano SeveroIn this article, the binding affinity of 1,4-dihydropyridine-based hexahydroquinoline-3-carboxylates with bovine serum albumin (BSA) was studied by electronic spectroscopies, quantum calculations, and molecular docking. These compounds were obtained by the one-pot microwave-assisted method via a modified Hantzsch reaction. The photophysical characterization showed in organic solutions absorption maxima in the UV region, ascribed to spin and symmetry allowed electronic transitions (1)pi-pi*. In addition, they presented a main fluorescence emission in the violet-blue regions (406-445 nm), with a relatively large Stokes shift (54-81 nm), depending on the structure of the compounds. BSA fluorescence quenching experiments based on the intrinsic fluorescence of the Trp residues were successfully applied to these compounds, indicating strong interaction with BSA by a static mechanism. The docking simulations corroborated the strong interaction between the studied compounds and BSA, where the surroundings of Trp213 seemed to be the preferred interaction site for all compounds and were responsible for the fluorescence quenching effects.Item Exometabolomic analysis of susceptible and multi-drug resistant Pseudomonas aeruginosa(2022) Kocak, E.; Nigiz, S.; Ozkan, E.; Kablan, S. Erdogan; Hazirolan, G.; Nemutlu, E.; Kir, S.; Sagiroglu, M.; Ozkul, C.; 35419823Multidrug resistant (MDR) Pseudomonas aeruginosa strains have recently become one of the major public health concerns worldwide leading to difficulties in selecting appropriate antibiotic treatment. Thus, it is important to elucidate the characteristics of MDR isolates. Herein, we aimed to determine the unique exometabolome profile of P. aeruginosa clinical isolates in monocultures that comprise high resistance to multiple antibiotics, and compare the differential metabolite profiles obtained from susceptible isolates by using GC/MS. Our results showed that partial least square-discriminant analysis (PLS-DA) score plot clearly discriminated the MDR and susceptible isolates indicating the altered exometabolite profiles, and highlighted the significantly enriched levels of trehalose and glutamic acid in MDR isolates. Expression of trehalose synthase (treS) was also 1 center dot 5-fold higher in MDR isolates, relatively to susceptible isolates. Overall, our study provides insights into the distinct footprints of MDR P. aeruginosa isolates in mono-culture.
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