Cilt:44 Sayı:01 (2020)

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https://dspace.ankara.edu.tr/handle/20.500.12575/70879

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Alzheimer hastalığının gelişiminde biyolojik ajanların olası etkileri
(Ankara Üniversitesi, 2020) Adalı, Ayça; Yirün, Anıl; Gümüşel, Belma Koçer; Erkekoğlu, Pınar; https://orcid.org/0000-0002-8811-6002; https://orcid.org/0000-0002-4050-8832; https://orcid.org/0000-0003-4311-2291; https://orcid.org/0000-0003-4713-7672; Eczacılık Fakültesi
Amaç: Dünya çapında artan nüfusa bağlı olarak yaşlı nüfusun artması Alzheimer hastalığı (AH)’nin görülme sıklığının artmasına yol açmıştır. Son yıllarda, farklı demans türleri ve özellikle de AH konusundaki bilimsel araştırmalar hızlanmıştır. Hastalığın multi-genetik nedenlerle ortaya çıkabileceği bilinse de, birçok biyolojik ajana maruziyetin de AH’nin patofizyolojisinde rol oynayabileceği belirtilmektedir. Literatürde Herpes simplex virüs tip-1 (HSV-1), insan immünoyetmezlik virüsü 1 (HIV-1) ve Helicobacter pylori gibi enfeksiyon etkenlerinin ve vücutta endojen olarak bulunan prion proteinlerinin bu hastalığının gelişimine yol açabileceği belirtilmektedir. Diğer taraftan, diyabet gibi hastalıkların da AH’nin gelişimini hızlandırabileceğine dair araştırmalar bulunmaktadır. Bu derlemede, AH’nin genel özelliklerinden bahsedilecek; bu hastalığın patofizyolojinde rol oynayabileceği bildirilen biyolojik ajanlardan ve bu konuda yapılmış çalışmalardan söz edilmesi amaçlanmıştır. Sonuç ve Tartışma: AH’nin ortaya çıkmasında genetik faktörlerin yanı sıra, birçok biyolojik ajanın rolü olabileceği belirtilebilir. Bu konuda daha ileri düzeyde ve mekanistik çalışmalara ihtiyaç duyulmaktadır
Amelanchier Medik. (Rosaceae) cinsinin farmasötik botanik açısından önemi
(Ankara Üniversitesi, 2020) Herkul, Mesut M.; Köroğlu, Ayşegül; Eczacılık Fakültesi
Amaç: Bu derleme çalışması, Rosaceae familyasına ait Amelanchier cinsine ait bitkiler üzerinde dünya genelinde yapılan etnobotanik, fitokimyasal ve biyolojik aktivite çalışmalarının derlenmesini kapsamaktadır. Türkiye’de de 4 takson ile temsil edilen bu cins üzerinde daha sonra yapılacak çalışmalar için katkı sağlanması hedeflenmiştir. Gereç ve Yöntem: 1998 ve 2018 yılları arasında periyodik olarak yayınlanan basılı ve elektronik dergiler taranmıştır. Sonuç ve Tartışma: Etnobotanik veriler Amelanchier cinsinin dünya genelinde yaygın kullanımının olmadığını göstermiştir. Amelanchier cinsi üzerinde yapılan fitokimyasal ve in vitro biyoaktivite çalışmaları, A. canadensis, A. arborea, A. ovalis ve A. alnifolia’nın meyveleri üzerinde yoğunlaşmıştır. Meyvelerin flavonoid, karotenoid ve siyanogenetik glikozit yapısında bileşikleri taşıdığı tespit edilmiştir. Meyvelerinin yüksek fenolik madde içeriği nedeniyle biyolojik aktivite çalışmalarının antioksidan etki üzerinde yoğunlaştığı görülmüştür.
Applications of miniaturized and portable near infrared (nir), fourier transform infrared (ft-ir) and raman spectrometers for the inspection and control of pharmaceutical products
(Ankara Üniversitesi, 2020) Usman, Abdullahi Garba; Ghali, Umar Muhammad; Işık, Selin; https://orcid.org/0000-0001-5660-4581; https://orcid.org/0000-0002-3500-8075; https://orcid.org/0000-0001-7601-3746; Eczacılık Fakültesi
Objective: In this review, the wide range of different applications of portable and miniaturized Fourier transform infrared (FT-IR), near-infrared (NIR), and Raman spectrometers for quality control, assessment and inspection of pharmaceutical products are discussed. In regard to counterfeiting, these portable spectrometers are utilized for vibrational and scattering spectroscopies in the identification of counterfeits, adulterated, fraudulent, falsified and substandard pharmaceutical products which are becoming significant problems and a danger to general well-being, particularly in the developing nations. Material and Method: Different scientific articles and books were researched and reviewed to explain the applications of miniaturized and portable near infrared (NIR), Fourier transform Infrared (FT-IR) and Raman spectrometers for the inspection and control of pharmaceutical products from past to nowadays. Result and Discussion: Adulterated pharmaceutical products have become the greatest threat for developing countries. This problem can reduce the confidence for pharmaceutical products. The application of mentioned portable devices for determinations the quality control of pharmaceutical product, enables the techniques to be more accessible, quick, accurate, simple, precise, robust and more importantly, efficient.
Chemical characterization of the fatty acid compositions and antimicrobial activity of sumac (rhus coriaria l.) fruits, growing naturally in Turkey and sold in herbalist markets
(Ankara Üniversitesi, 2020) Yılmaz, Gülderen; Ekşi, Gülnur; Demirci, Betül; Demirci, Fatih; https://orcid.org/0000-0002-6569-4766; https://orcid.org/0000-0002-6869-8703; https://orcid.org/0000-0003-2343-746X; https://orcid.org/0000-0003-1497-3017; Eczacılık Fakültesi
Objective: The aim of this study was to compare the fatty acid components and antimicrobial properties of R. coriaria L. samples which were sold as powder and grains that show natural distribution in Tunceli and Siirt. Material and Method: After the seeds were weighed and powdered, fixed oils were obtained by using soxhalet apparatus. Obtained fixed oils were analyzed by GC and GC / MS methods after methylation process. In vitro antimicrobial activity studies of the samples were performed using six different Gram negative and Gram positive bacteria and Candida albicans using EUCAST disc diffusion and CLSI microdilution methods. Result and Discussion: The main fatty acid components of all samples were determined as oleic acid (42.2 - 43.3%), linoleic acid (25.2 - 28.5%) and palmitic acid (18.4-221.5%), respectively. In vitro antimicrobial activity of fixed oils, such as Escherichia coli NRRL B-3008, Staphylococcus aureus ATCC 6538, S. epidermidis ATCC 14990, Pseudomonas aeruginosa ATCC 27853, Bacillus subtilis NRRL B-A78 A78. Results were compared with standard antimicrobial agents and MIC values> 2.5 - 0.22 mg/ml. The results were found to be significant in terms of antimicrobial efficacy
Design, synthesis, antimicrobial and antifungal activities of new 1,2,4-triazole derivatives containing 1h-tetrazole moiety
(Ankara Üniversitesi, 2020) Frolova, Yuliia; Kaplaushenko, Andriy; Nagornaya, Nataliya; https://orcid.org/0000-0002-3995-5088; https://orcid.org/0000-0003-3704-5539; Eczacılık Fakültesi
Objective: Antimicrobials and antifungals are the most acquired drugs in the world. Today, it becomes necessary to create new drugs with antimicrobial and antifungal effect. The purpose of our research is the synthesis of new series of 5-(1Н-tetrazole-1-yl)-4H-1,2,4-triazole-3-amine, the establishment of physicalchemical, antimicrobial and antifungal properties for all synthesized compounds. Material and Method: 5-(1Н-tetrazole-1-yl-methyl)-4H-1,2,4-triazole-3-yl-1-(alkyl-, aryl-)-methanimines were synthesized by reacting of 5-(1H-tetrazole-1-yl-methyl)-4H-1,2,4-triazole-3-amine with aldehydes in acetic acid. Then, sodium borohydride was selected as a reducing agent, which allowed for the restoration of the double bond. The structures of synthesized compounds were confirmed by IR, 1H NMR and mass spectra. The synthesized compounds were evaluated for antimicrobial and antifungal activity by "serial dilutions" method. Result and Discussion: During the synthetic studies the new series of 22 compounds were obtained. The 5- (1Н-tetrazole-1-yl-methyl)-4H-1,2,4-triazole-3-yl-1-(5-nitrofuran-2-yl)methanimine was observed to be most possessing good antimicrobial and antifungal activity and has exceeded the reference standard for Staphylococcus aureus (12,5/25 mg/ml), Escherichia coli (50/100 mg/ml), Pseudomonas Aeruginosa (100/200 mg/ml), Candida albicans (50/50 mg/ml).
Evaluation on gallic acid, egcg contents and antiradical activity of green tea and black tea extracts
(Ankara Üniversitesi, 2020) Ağca, Aslı Can; Batçıoğlu, Kadir; Şarer, Engin; https://orcid.org/0 0000-0002-5710-3479; https://orcid.org/0000-0001-6663-2287; https://orcid.org/0000-0001-6681-2309; Eczacılık Fakültesi
Objective: Tea is very well known and consumed beverage worldwide also cultivated widely. It is one of phytonutrients that has a protective role associated with its antioxidant activity. The aim of this article is to study the gallic acid, epigallocatechin gallate contents and antiradical activity of green tea and black tea extracts from Camellia sinensis cultivated in North Anatolia. Material and Method: Gallic acid and epigallocatechin gallate contents were investigated in ethanol, methanol and water extracts of green tea and black tea by HPLC analysis and the antiradical activities were also examined for scavenging effect on DPPH and ABTS free radicals. Result and Discussion: In total 6 extracts, gallic acid contents were determined in the range of 0.052- 1.341 mg/100 ml and the value of EGCG (epigallocatechin gallate) were found between 0-19.54 mg/100ml. Water extract of green tea exhibited the best antiradical activity on both DPPH and ABTS radicals. Green tea could be evaluated as a good candidate for health prevention but it should be noted that the harvesting method and manufacturing process, optimum conditions on brewing time, the solvent used, chopping grade of tea leaves should also be taken into consideration during formulating both phytonutrient and pharmaceutical grade products.
Formulation and detailed characterization of voriconazole loaded in situ gels for ocular application
(Ankara Üniversitesi, 2020) Okur, Neslihan Üstündağ; Yozgatlı, Vildan; Şenyiğit, Zeynep; https://orcid.org/0000-0002-3210-3747; https://orcid.org/0000-0001-8018-6500; https://orcid.org/0000-0002-4920-2469; Eczacılık Fakültesi
Objective: This study was aimed to prepare, characterize and evaluate in situ gel formulation for a sustained ocular delivery of voriconazole. Material and Method: In situ gels were prepared with three different hydrophilic co-polymers: Poloxamer 188, 407 and 388. The formulations were characterized in terms of their clarity, pH, viscosity drug content uniformity and mechanical/rheological properties. Moreover, in vitro drug release and stabilitystudies were performed. Result and Discussion: The results showed that the optimized in situ gel formulation had desired in vitro properties and a good stability over the period of 3 months. Texture profile analysis presented that formulations offered suitable adhesive and mechanical properties. P2-V formulation exhibited pseudoplastic flow and typical gel-type mechanical spectra (G′ > G″) at different frequecy values and at different temperatures. Moreover, all formulations showed a sustained drug release for 24 hours. In conclusion, voriconazole loaded in situ gel could be offered as an encouraging strategy as ocular systems for ocular infections treatment.
Histological study of a corrective influence of a compound potassium 2-((4-amino-5-(morpholinomethyl)- 4h-1,2,4-triazol-3-yl)thio)acetate (pkr-173) on the state of chicken's liver under infection by pseudomonas aeruginosa
(Ankara Üniversitesi, 2020) Vashchyk, Yevgenia; Shcherbyna, Roman; Parchenko, Volodymyr; Bushueva, Inna; Gutyj, Bogdan; Fotina, Hanna; Fotina, Tatiana; Stronskyi, Yuriy; Eczacılık Fakültesi
otassium 2((4-amino-5-(morpholinomethyl)-4H-1,2,4-triazol-3yl)thio)acetate (PKR-173) with different antibiotics on the state of chicken's liver under infection by Pseudomonas aeruginosa. Material and Method: The histological study was carried out on the levers of intact chickens (intact control); chickens that were infected by the strain of Pseudomonas aeruginosa (controlled pathology); chickens that had (before being infected by Pseudomonas aeruginosa) preventive input of the compound PKR-173 with the classic antibiotic Enrofloxacin or with Saroflox (undergoing research); or were input Thiotriazolin with the classic antibiotic Enrofloxacin. Result and Discussion: As a result, it is stated, that preventive input of the compound PKR-173 with reseachable antibiotic Saroflox, as well as with classic antibiotic Enrofloxacin and Thiotriazolin with antibiotic Enrofloxacin, to chickens infected with pseudomonas aeruginosa, prevents from chickens' livers developing stereotypical morphological changes characteristic of nonspecific reactive hepatitis. Analysis of quantitative characteristics of pathological process that developed in chicken's liver infected with pseudomonas aeruginosa, and the corrective influence of researched methods showed that the compound PKR-173 with antibiotic Saroflox believably lowers displays of all signs of pathology compared to the controlled pathology
Kenevir ve sağlık alanında kullanımı
(Ankara Üniversitesi, 2020) Yıldırım, Selda; Çalışkan, Ufuk Koca; https://orcid.org/0000-0002-5216-7588; https://orcid.org/0000-0002-1611-5617; Eczacılık Fakültesi
Amaç: Kenevir, binlerce yıldır özellikle liflerinden ve tohumları olmak üzere tüm kısımlarından çeşitli amaçlarla (yapı-tekstil malzemesi, kağıt, besin, insan ve hayvan sağlığında ilaç vb.) yararlanılan, ilk kültürü yapılan bitkilerdendir. 1930’lu yıllarda öforik amaçla kullanımının suistimal edilmesi ve ticari kaygılardan dolayı uzun yıllar yasaklı/kısıtlı bitki olarak kalan kenevir, yeni nesil kullanım alanları ve özellikle insan sağlığıyla ilgili etkilerinin bilimsel araştırmalarla kanıtlanmasıyla son yıllarda tekrar ön plana çıkmıştır. Günümüzde pek çok ülke kenevirle ilgili yasaların güncellenmesiyle kenevirin hem endüstriyel hem de medikal etkilerinden faydalanmaya başlamıştır. Ülkemizde ise son yıllarda endüstriyel kenevir üretimi ve kullanımı ile ilgili birtakım gelişmeler yaşanmaktadır. Gereç ve Yöntem: Bu çalışmada, kenevirin botanik özellikleri, tarihçesi, fitokimyasal içeriği, terapötik kullanımları ve sağlık alanında yapılan bilimsel çalışmalar derlenmiştir. Sonuç ve Tartışma: Kenevir bitkisinin botanik özellikleri, genel kullanım alanları ile birlikte geçmişten günümüze sağlık alanında kenevirden elde edilen kullanımda olan ilaçlardan örnekler verilerek fitokimyasal içeriği ve etkileri detaylı olarak verilmiştir. Kenevir tohumu yağı ve kökündeki aktif bileşenlere de değinilmiş, kenevirin terapötik kullanımı tartışılmıştır. Hem endüstriyel hem sağlık alanında kullanılan fakat üretimi ve kullanımı ülkemizde kısıtlı olan kenevir ile ilgili yasaların bilimsel destekli olarak yeniden gözden geçirilmesi ülke ekonomisi ve sağlık sektörü için oldukça önemli sonuçlar sağlayacaktır
Medicinal plants traditionally used to treat skin diseases in Turkey – eczema, psoriasis, vitiligo
(Ankara Üniversitesi, 2020) Eraslan, Zeynep Büşra; Genç, Gülay Ecevit; Kültür, Şükran; https://orcid.org/0000-0001-7541-2569; https://orcid.org/0000-0002-1441-7427; https://orcid.org/0000-0001-9413-5210; Eczacılık Fakültesi
Objective: Different types of skin diseases negatively affect the lives of many people, both physically and mentally. Here, we aimed to document medicinal plants used as traditional folk medicine for the treatment of eczema, psoriasis and vitiligo in Turkey. Material and Method: Literature search was conducted by screening ethnobotanical studies. Moreover, pharmacological and phytochemical studies were reviewed to assess the efficacy of the most commonly used plants on skin diseases. Result and Discussion: In total, 191 taxa belonging to 134 genera and 64 families were determined as being traditional herbal medicines used in defined skin diseases. Based on their number of citations, the most frequently used medicinal plant species are Juglans regia L. (19), Urtica dioica L. (18), Juniperus oxycedrus L. (9), Chelidonium majus L. (8), Dracunculus vulgaris Schott (7), Ecballium elaterium (L.) A. Rich. (6), Ficus carica L. (6), Malva sylvestris L. (6) and Rosa canina L. (6), respectively. It is concluded that several pharmacological and phytochemical studies support the traditional usage of plants, but further studies are needed. All findings are expected to be the basis for novel pharmaceutical products and a handbook for healthcare professionals
Microwave synthesis of new 3-(alkylthio)-5-(thiophen2-ylmethyl)-1,2,4-triazol-4-amines
(Ankara Üniversitesi, 2020) Safonov, Andrii A.; https://orcid.org/0000-0003-2861-1826; Eczacılık Fakültesi
Objective: The aim of this work is to synthesize 3-(alkylthio)-5-(thiophen-2-ylmethyl)-1,2,4-triazol-4- amines by the Milestone Flexi Wave microwave synthesis system and to prove structure synthesized compounds. Material and Method: The initial compounds 3-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-5-thioles (1-5) were synthesized at the Department of Toxicological and Inorganic Chemistry of the Zaporizhzhya State Medical University (Ukraine). Milestone Flexi Wave microwave synthesis system was used to synthesize 3- (alkylthio)-5-(thiophen-2-ylmethyl)-1,2,4-triazol-4-amines. The elemental analysis of synthesized compounds was established by the universal analyzer Elementar Vario L cube (CHNS). The 1 H spectra (at 400 MHz and 100 MHz) were recorded in DMSO-d6 on a Varian MR-400 spectrometer and analysed with ADVASP™ Analyzer program. The completeness of the reactions and the individuality of the resulting compounds were controlled by the gas chromatograph Agilent 7890B with a 5977B mass spectrometry detector. Result and Discussion: The reaction was carried out in an alcoholic medium by adding a catalytic amount of HCl to 5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiols. Methyl and i-propyl alcohols were used as alcohols. The mixture was heated for 45 minutes at a temperature of 150°C, a pressure 14.4 bar, ΔMW = 200 W. The signals of 1 H NMR for (4a-b, 6a-j) are consented with the proposed structure. The elemental analysis (CHNS) was accomplished for synthesized compounds to confirm their basic chemical structures and revealed acceptable agreement with the calculated percentages.
Novel tacrine and hesperetin analogues: design, molecular docking and in silico adme studies to identify potential acetyl choline esterase inhibitors for alzheimer’s disease
(Ankara Üniversitesi, 2020) Naresh, Kondapalli; Sruthi, Kanna; https://orcid.org/0000-0002-6454-5291; Eczacılık Fakültesi
Objective: Present investigationis aimed to design and identify new potential molecules to treat Alzheimer’s disease from the Tacrine and Hesperetin structures via molecular modification. Acetyl cholinesterase (AChE) enzyme was selected as target, since inhibitors of AChE were successful in the management of dementia and alleviation of other symptoms. Material and Method: In this study, two series of new Tacrine (T1-T9) and Hesperetin (H1-H9)derivatives on the basis of the structural characteristics of acetyl cholinesterase (AChE) inhibitors were designed and screened to identify potential analogues as Anti-Alzheimerdrug on the AChE (PDB ID:1DX4) using GLIDE employing extra-precision docking. The docking results (Glide score, XPscore, docking score and binding interactions) were compared with standard drug, Tacrine. Result and Discussion: From the docking results it was found that T9 showed highest docking score among the designed compounds. The ADME properties also predicted using Qikprop application, from the above studies’ potential analogues with highest AChE inhibition and excellent pharmacokinetic properties were identified.

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