TR-Dizin İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/9
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Article Citation - WoS: 1Citation - Scopus: 1Synthesis, Characterization, and Antimicrobial Evaluation of Some Novel Hydrazinecarbothioamides(Galenos Publishing House, 2025) Güler, Emrah; Dinç, Harika Öykü; Dincel, Efe Doğukan; Güzeldemirci, Nuray Ulusoy; Başoğlu-ünal, Faika; Kuran, Ebru Dıdem; Başoğlu, Faika; Ulusoy Güzeldemirci, NurayObjectives: This study focused on synthesizing and characterizing novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety and evaluating their antimicrobial activity against several bacterial strains. The research aimed to identify key structural features that enhance antimicrobial efficacy through structure-activity relationship analysis and identify the minimum inhibitory concentration (MIC) of the most potent compounds to assess their potential for further development as antimicrobial agents. Materials and Methods: Nine novel thiosemicarbazide derivatives containing a 1,2,4-triazole moiety were synthesized by reacting 1,2,4-triazole derivatives with thiosemicarbazide precursors, and the products were characterized using infrared spectroscopy, proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR) spectroscopy, and elemental analysis. The antimicrobial activity of these compounds (5a-i) was tested against Klebsiella pneumoniae (K. pneumoniae), Escherichia coli, Staphylococcus aureus, Enterococcus faecalis, and Pseudomonas aeruginosa (P. aeruginosa), using microdilution, disk diffusion, and broth microdilution methods. Dimethyl sulfoxide was used as a negative control, and Vancomycin and Meropenem were used as positive controls, with all results converted to µM for consistent analysis. Results: The synthesized thiosemicarbazide derivatives (5a-i) were confirmed to be structurally correct through Fourier-transform infrared spectroscopy, 1H-NMR, and 13C-NMR spectroscopy. Among the tested compounds, 5e (4-bromophenyl) and 5g (n-propyl) showed significant antimicrobial activity, with 5g exhibiting the strongest effects against S. aureus and P. aeruginosa. Other derivatives, such as 5b (4-NO2Ph), 5c (4-FPh), and 5d (4-ClPh), showed moderate activity, while no significant activity was observed against K. pneumoniae or E. faecalis. Conclusion: The study successfully synthesized a series of novel thiosemicarbazide derivatives with a 1,2,4-triazole moiety and evaluated their antimicrobial potential. Compounds 5e and 5g exhibited significant antibacterial activity, particularly against S. aureus and P. aeruginosa, with MIC values in the low micromolar range. These findings suggest that the compounds hold promise as potential antimicrobial agents, and further studies should focus on optimizing their efficacy and exploring their mechanism of action.Article Bir Tiyoeter-triazol Hibriti: Güçlü Metap2 Inhibitörü ve Prostat Kanseri için In Vivo Tümör Baskılayıcı Bileşiğin In Silico Çalışmaları ve In Vitro Mikrozomal Metabolizması(2023) Coşkun, Göknil Pelin; Ulgen, Mert; Birgül, Kaan; Evren, Asaf Evrim; Küçükgüzel, Ş.günizArka plan/amaç: Antikanser bir ilaç adayı bileşik olan ( S)-3-((2,4,6-trimetilfenil)tiyo)-4-(4-florofenil)-5-(1-(6-metoksinaftalen-2-)il) etil)-4H-1,2,4-triazol (SGK636), bileşiğinin in vitro mikrozomal metabolizması çalışılmış ve potansiyel S-oksidasyon ve S-dealkilasyon metabolitlerini belirlemek için NADPH ile güçlendirilmiş domuz mikrozomal preparatları kullanılarak incelenmiştir. Gereç ve Yöntemler: Bu çalışmada, sülfoksit metaboliti kromatografik ve spektroskopik yöntemlerle sentezlenmiş, saflaştırılmış ve karakterize edilmiştir. SGK636, S-oksidasyon ve S-dealkilasyon metabolitleri daha sonra ters fazlı bir LC-MS, UV spektroskopisi ve bir HP-TLC sistemi ile ayrılmıştır. In vitro mikrozomal metabolik deneylerin sonuçları, SGK636’nın, aynı Rt ve Rfx100 değerleri ve UV/ ile LC-MS, LC-MS/MS ve HP-TLC tarafından gözlemlenen karşılık gelen S-oksidasyon metabolitini (sülfoksit) ürettiğini göstermiştir. Otantik bileşiklerle karşılaştırıldığında MS spektrumlarında, herhangi bir S-dealkilasyon metaboliti tespit edilmemiştir. Bulgular: Mevcut sonuçlar moleküler doking ve moleküler dinamik çalışmalarla kanıtlanmıştır. Sülfoksidasyon işlemi tersine çevrilebilir olduğundan ve deneyimizdeki düşük miktarda sülfoksit metabolitini kısmen açıklayabildiğinden, sülfoksit bileşiği de inkübe edilmiştir. Substrata (SGK636) geri dönüşüm gözlenmemiş olup, karşılık gelen sülfon metabolitinin oluştuğu gözlenmiştir. SGK636’nın otooksidize olup olmadığını belirlemek için substrat ayrıca standart inkübasyon koşulları altında tampon içinde inkübe edilmiştir, ancak karşılık gelen sülfoksitte herhangi bir oto-oksidasyon gözlenmemiştir. Sülfona herhangi bir olası otooksidasyonu veya tekrar SGK636’ya indirgemeyi görmek için tampondaki SGK636-SO (sülfoksit) için bir stabilite çalışması da yapılmıştır. Her iki şekilde de dönüşüm gözlemlenmemiştir. Substrat, farmakolojik aktivitesi açısından bir avantaj olabilecek metabolik reaksiyonlara ve otooksidasyona karşı kararlı görünmektedir. Sonuç: Mevcut metabolik çalışma, SGK 636’nın S-oksidasyonuna uğradığını göstermektedir. Sorumlu oksidatif enzimi belirlemek için moleküler yerleştirme ve moleküler dinamik çalışmalar yapılmıştır. CYP3A4’ün S-oksidasyonundan sorumlu enzim olduğu bulunmuştur.Research Project Yeşil Kimya Teknikleri ve Moleküler Docking Yöntemleri ile Yeni Florokinolon Hibrit Moleküllerin Sentezi, Dna Giraz, Topoizomeraz Iv İnhibisyonu ve Antibakteriyel Aktivitelerinin Araştırılması(2021) Durukan, İnci; Kulabaş, Necla; Akdemir, Atilla; Faiz, Özlem; Ayvaz, Aslıhan; Kilic, Ali Osman; Demirbaş, Ahmet; Azafad, İmaneBu projede öncelikle, literatür verilerinden ve grubumuzun daha önceki çalışmalardan elde ettikleri sonuçlara (yapı-aktivite ilişkileri, SAR) dayanılarak DNA giraz ve topoizomeraz IV inhibisyonu göstermesi öngörülen ve florokinolon-heterohalka hibrit bileşikleri içeren sanal veribankası oluşturulmuştur. Daha sonra bu veribankasından ön çalışmalarımızda geliştirdiğimiz ve valide ettiğimiz sanal tarama yöntemleri ile E. coli veya S. aureas DNA giraz veya DNA topoizomeraz IV enzimlerini inhibe etme potansiyeline sahip olan 75 bileşik sentez için önerilmiştir. Sentezlenen bütün bileşikler enzim inhibisyonu ve antimikrobial aktivite deneylerinde test edilmiştir. Sentezlenen bileşiklerin bazılarının giraz ve topoizomeraz IV inhibisyonu göstermemesine karşılık bilinen antibakteriyel ilaçlar olan norfloksazin, siprofloksazin kadar veya onlara yakın derecede antibakteriyel aktivite göstermesi, bunların florokinolon antibiyotiklerinden farklı bir mekanizma üzerinden etki ettiklerini göstermektedir ki bu durum özellikle ilaç direnci probleminin üstesinden gelme çalışmalarına katkı sağlama potansiyeli göstermektedir. Sentez çalışmalarında geleneksel ısıtma veya karıştırma yöntemlerine ilaveten mikrodalga veya ultrasonik ışınlandırma tekniklerinin de denenmiş ve geleneksel yöntemlere üstünlük sağlayan sonuçların elde edilmiş olması, bu çalışmayı yeşil kimya tekniklerinin geliştirilmesi açısından da değerli kılmaktadır.Article Citation - Scopus: 2Synthesis and Biological Evaluation of Novel Paracetamol-Triazole Conjugates(Society of Pharmaceutical Sciences of Ankara (FABAD), 2023) Kulabaş, Necla; Gurboga, Merve; Özakpınar, Özlem Bingöl; Liu, Jianyang; Jakobson, Per-johan; Danış, Özkan; Küçükgüzel, İlkay; Jakobsson, Per-Johan; Ogan, AyseBaşlangıç maddesi olarak parasetamol kullanılarak bazı yeni triazol içeren asetamid türevleri 9-20 sentezlendi ve yapıları FTIR, NMR (1H and 13C) ve kütle spektral verileri ile karakterize edildi. Beş insan kanser hücre hattına (akciğer kanseri A549, kronik miyelojenöz lösemi K562, meme kanseri MCF-7, prostat kanseri PC-3, nöroblastoma SH-SY5Y hücre hatları) karşı sentezlenen tüm moleküllerin in vitro sitotoksik aktiviteleri incelendi ve ayrıca seçiciliği tanımlamak için fare embriyonik fibroblast hücreleri (NIH/3T3) üzerinde sitotoksik etkileri MTT yöntemiyle test edildi. Ek olarak, on iki hedef bileşik 9-20, mPGES-1 ve COX-1/2 inhibe edici etkileri açısından tarandı. Sentezlenen bileşiklerin hiçbiri hem kanser hücrelerine hem de mPGES-1 ve COX-1/2 enzimlerine karşı anlamlı bir inhibisyon göstermezken, sağlıklı hücrelere karşı da sitotoksik olmadıkları belirlendi. Son olarak yeni sentezlenen bileşiklerin ADMET özellikleri in siliko yöntemler kullanılarak tahmin edildi.Article Citation - Scopus: 3Therapeutic Effects of Momordica Charantia L. Ethanolic Extract on Acetic Acid-Induced Ulcerative Colitis in Rats(Istanbul University Press, 2021) Ozbeyli, D.; Sen, A.; Aykac, A.; Terali, K.; Cilingir-Kaya, O.T.; Senkardes, I.; Sener, G.Objective: This study aims to investigate the effect of Momordica charantia L. (MoC) ethanolic extract on ulcerative colitis (UC) and was explored in vitro and in vivo. Materials and Methods: The rats were divided into control (C), saline-treated colitis (AA), MoC extract-treated colitis (AA+MoC), and sulfasalazine (SS)-treated colitis (AA+SS) groups. Colitis was induced by acetic acid. MoC extract, SS or saline were given to the related groups for 3 days. Interleukine-1β, malondialdehyde, glutathione levels, myeloperoxidase activity, bax/bcl-2 ratio, caspase-9 and caspase-3 levels were measured in colon and macroscopic and histopathologic examinations were done. Total phenolic/flavonoid content and biological activity of MoC were evaluated by in vitro analysis. Results: Compared to the control group, with acetic acid application interleukin-1β levels, myeloperoxidase activity, malondialdehyde levels, bax/bcl-2 ratio, caspase-9 and caspase-3 levels were significantly upregulated, while glutathione levels were significantly decreased in the AA group. In contrast, MoC and SS treatments reduced interleukin-1β, malondialdehyde levels, myeloperoxidase activity, bax/bcl-2 ratio, and caspase-9 and caspase-3 levels. Glutathione levels increased upon MoC or SS treatment. Increased macroscopic and microscopic scoring with AA improved with MoC or SS treatment, but the MoC or SS treated groups had higher score values than the control. Also, in vitro results showed that MoC exhibited 2,2-diphenyl-1- picrylhydrazyl and 2,2'-azino-bis-3-ethylbenzothiazoline-6-sulfonic acid radical scavenging activity as well as significant antilipoxygenase activity. In addition, MoC extract showed a potent anti-inflammatory activity compared to standard indomethacin. Conclusion: Our biochemical, in vitro and histopathologic analysis indicate that MoC is likely to prove beneficial in UC therapy. © 2021 European Journal of Biology. All rights reserved.Article Citation - WoS: 2Analysis of Selected Steroid Hormones in Sea of Marmara Sediment Samples by Lc-esi/Ms-ms(Istanbul Univ, Fac Pharmacy, 2023) Aysel, Esra; Yurdun, TurkanBackground and Aims: Sediment is the general name given to the muddy structure located at the bottom of aquatic environments such as the sea. In our study, the amounts of steroid hormones were investigated in the sediment samples taken from the Marmara Sea. According to other studies, it has been determined that the excess of the hormone load in the sediments may be an indicator of human/animal sourced pollution, as well as the negative effects of the hormones mixed in the seas with the ecological cycle on the health of humans and animals.Methods: In our study, 31 selected human/animal, plant, natural and synthetic hormone-steroids were studied using Liquid Chromatography Electrospray Ionization Tandem Mass Spectrometry (LC-ESI/MS-MS). Methanol and QuEChERS were used as extraction methods. Sediment samples were taken from a total of 27 points selected for sampling at the Marmara Sea.Results: According to the results we found, the androgens: androsterone (24.50-1718.18 ng g-1), testosterone (86.30-1600.32 ng g-1); the estrogens: mestranol (33.73-228.32 ng g-1), equilin (53.44-1232.53 ng g-1); the progestagens; pregnenolone (37.50374.76 ng g-1), progesterone (39.96-405.60 ng g-1); levonorgestrel (325.25 and 937.93 ng g-1); the fecal sterols: cholestanone (57.57-1726.32 ng g-1), coprostanol + epicoprostanol (51.43-1370.33 ng g-1); and the plant sterol; campesterol (35.30-1859.90 ng g-1) were the compounds detected.Conclusion: Estrogens and progestogens are active components of birth control pills, and cholestanone and coprostanol + epicoprostanol are steroids that are indicative of human/animal pollution. Coprostanol + epicoprostanol and cholestanone, which are indicators of fecal pollution, were detected in all sediment samples. In our study, steroid hormones were detected for the first time in Sea of Marmara sediments and possible environmental risks were evaluated.Article Citation - WoS: 3Citation - Scopus: 3Antioxidants, Enzyme Inhibitory Activities, and Phytochemical Profiles of Seven Medicinal Plants Grown With Organic Farming Techniques(Tubitak Scientific & Technological Research Council Turkey, 2023) Zor, Murat; Ozupek, Burcin; Pekacar, Sultan; Deliorman Orhan, Didem; Orhan, Didem DeliormanIn this study, the potential antihyperlipidemic, antidiabetic, and antiobesity effects of extracts obtained via infusion techniques from Artemisia absinthium L., Achillea millefolium L., Calendula officinalis L., Fumaria officinalis L., Mentha piperita L., Origanum onites L., and Urtica dioica L. grown with organic farming techniques were investigated using enzyme inhibition methods (alpha-glucosidase, pan-creatic cholesterol esterase, pancreatic lipase, and alpha-amylase). It is important that natural compounds or extracts to be used in the treat-ment of metabolic problems have antioxidant effects. The antioxidant effects of these species were tested in terms of ABTS and DPPH radical scavenging activity, ferric reducing power, and metal chelating capacity. Extracts (2 mg/mL) of M. piperita (91.43 +/- 0.90%) and O. onites (70.18 +/- 2.02%) showed potent inhibitory effects on the alpha-glucosidase enzyme. Among all species, only O. onites extract ex-erted an inhibitory effect on the cholesterol esterase enzyme close to that of reference compound simvastatin. While all extracts were effective in the tested antioxidant activity methods, it was determined that the M. piperita and O. onites extracts displayed particularly significantly strong activities in terms of ferric reducing power, ABTS radical scavenging effect, and metal chelating capacity. The total flavonoid and phenolic contents of all extracts were determined. The compositions of the most active extracts were analyzed for pheno-lic acids and flavonoids using RP-HPLC. The results of RP-HPLC analysis showed that the levels of ellagic acid (0.923 +/- 0.000 g/100 g extract) in the M. piperita extract and rosmarinic acid (0.813 +/- 0.003 g/100 g extract) in the O. onites extract were high. As a result, all species grown with organic farming techniques except U. dioica were found to have high antioxidant effects. In light of these findings, it was concluded that M. piperita and O. onites grown with organic farming techniques showed strong inhibitory effects in terms of the tested activities, especially for alpha-glucosidase and pancreatic cholesterol esterase, and that in vivo studies and activity-guided isolation studies should be conducted on these species in the future.Article Citation - WoS: 2Citation - Scopus: 2Rapid Synthesis of Silver Nanoparticles With<i> Rheum</I><i> Ribes</I> L Fruit Peels: Anticancer and Antimicrobial Effects With Biocompatible Structures(Ankara Univ, Fac Agriculture, 2024) Zor, Murat; Baran, Mehmet Firat; Ipek, Duygu Neval S. A. Y. I. N.; Sayin İpek, Duygu NevalSilver nanoparticles (AgNPs) are substances with a wide range of uses. Utilizing extracts obtained from the peels of Rheum ribes L. (Rr) fruit growing in Erzurum region, silver nanoparticles were rapidly created in this study with a quick, easy, and environmentally friendly technique without harmful processes. In order to evaluate the attributes of the synthesized Rr-AgNPs, FE-SEM or TEM micrographs were utilized to characterize their morphology. A UV -visible spectrophotometer was used to assess the highest absorbance bands of RR-AgNPs. These data were used to define RR-AgNPs, which were characterized as having exclusively negative surface charges of -25 mV, spherical shape, maximum absorbance at 428 nm wavelength, and 96 nm size distribution. The effectiveness of the produced AgNPs for use in medical applications was assessed using the MTT technique with microdilution. Minimum inhibition concentrations of Rr-AgNPs for pathogen strains ranged from 0.03 to 0.50 mg/L. Additionally, it was discovered that AgNPs effectively suppressed malignant cells, with rates of 86.27%, 74.67%, and 73.49%, in the investigation of the anticancer effects of AgNPs. Healthy cells were not subject to any inhibitory effects at the same concentrations.Article Citation - WoS: 14Citation - Scopus: 12Synthesis of Some Novel Hydrazide-Hydrazones Derived From Etodolac as Potential Anti-Prostate Cancer Agents(Marmara Univ, 2022) Koc, Hande Cevher; Atlihan, Irem; Mega-Tiber, Pinar; Orun, Oya; Kucukguzel, S. Guniz; Tiber, Pinar Mega(R,S)-Etodolac [1,8-diethyl-1,3,4,9-tetrahydrapyrano(3,4-b)indole-1-acetic acid] is a nonsteroidal anti-inflammatory drug that contains carboxylic acid group with the structure of pyrano[3,4-h]indole. In this study, a series of novel (R,S)-Etodolac derivatives (3a-1) bearing hydrazide-hydrazone moiety were synthesized. The structures of these compounds were characterized by spectral (H-1-NMR and FT-IR analyses) methods. All synthesized compounds were screened for anticancer activity against androgen-independent prostate adenocarcinoma (PC-3, DU-145) and androgen-dependent prostate adenocarcinoma (LNCaP) cell lines by using WST-8 colorimetric method. This method was used for cell viability and cytotoxicity analysis. Compound 3b (SGK-720) [2-(1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(2,6-dichlorophenyl)methylene]hydrazides] showed 10.36, 5.24, 15.53 mu M anticancer activity against PC3, DU145, LNCaP cancer cell lines, respectively. According to JC-1 mitochondrial membrane potential test and Annexin V/PI staining, 3b was found to have apoptotic effect on these cancer cells. It is concluded that compound 3b containing 2,6-dichloro substituents may be one of the candidate molecules to cope with prostate cancer.Article Citation - WoS: 3Citation - Scopus: 3Investigation of the Protective and Therapeutic Efficacy of <i>myrtus Communis</I> Extract in Aluminum Chloride and Dgalactose-Induced Alzheimer's Disease in Rats(Marmara Univ, 2022) Yalman, Kiibra; Sen, Ali; Cevik, Ozge; Kadioclu-Yaman, Beril; Ertas, Biiva; Yildiz, Sila; Sener, Goksel; Yaman, Beril Kadıoğlu; Kadioğlu-Yaman, BerilThis study investigated the possible protective and therapeutic effects of Myrtus communis subsp. communis ethanol extract (MC) in aluminum chloride (AlCl3) and D-galactose (D-Gal) induced Alzheimer's disease in rats. MC was orally given to rats as a protective treatment for 90 days and, in other two groups starting from the 60th day MC (100-200 mg/kg) was administered, concomitantly with AlCl3 and D-Gal. Learning and memory functions were evaluated by the behavioral tests. Biological activities of MC treatment were examined in hippocampal tissues by ELISA tests. D-Gal and AlCl3-treated rats showed increased amyloid beta (A ss) and 8-hydroxy-2-deoxyguanosine (8OHdG) levels, acetylcholinesterase activity and decreased neprilysin, Na+-K+ATPase and SOD levels in parallel with a decrease in Novel Object Recognition Test, Morris Water Maze and Passive Avoidance Test scores. On the other hand, MC administration reversed the behavioral impairments and improved learning and memory. Moreover, MC treatment decreased A ss and 8-OHdG levels and acetylcholinesterase activity and increased neprilysin levels, Na+-K+ATPase and SOD levels. Our results suggest that MC has beneficial effects on cognitive and neuronal functions through its anticholinesterase and antioxidant properties.