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Öğe 6-Phenyl-3-(4-pyridyl)-1,2,4-triazolo-[3,4-b][1,3,4]thiadiazole: Synthesis, experimental, theoretical characterization and biological activities(Pergamon-Elsevier Science Ltd, 2012) Cansiz, Ahmet; Cetin, Ahmet; Orek, Cahit; Karatepe, Mustafa; Sarac, Kamiran; Kus, Alper; Koparir, PelinThe molecular geometry, vibrational frequencies, and gauge including atomic orbital (CIAO) H-1 and C-13 NMR chemical shift values of the title compound in the ground state have been calculated using the Hartree-Fock (HF) and density functional theory (DFT) methods with 6-31G(d) basis sets, and compared with the experimental data. The calculated results show that the optimized geometries can well reproduce the crystal structural parameters and the theoretical vibrational frequencies, and H-1 and C-13 NMR chemical shift values show good agreement with experimental data. To determine conformational flexibility, molecular energy profile of the title compound was obtained by HF/6-31G(d) and (DFT/B3LYP) calculations with respect to selected degree of torsional freedom, which was varied from -180 degrees to +180 degrees in steps of 10 degrees. The energetic behavior of the title compound in solvent media was examined using the B3LYP method with the 6-31G(d) basis set by applying the Onsager and the polarizable continuum model (PCM). The results obtained with these methods reveal that the PCM method provided more stable structure than Onsager's method. The title compound has been tested in vitro for biological effects. (C) 2012 Elsevier B.V. All rights reserved.Öğe Bioactive contents, In vitro antiradical, antimicrobial and cytotoxic properties of rhubarb (Rheum ribes L.) extracts(Taylor & Francis Ltd, 2020) Keser, Serhat; Keser, Fatma; Karatepe, Mustafa; Kaygili, Omer; Tekin, Suat; Turkoglu, Ismail; Demir, ErsinRheum ribes L. (rhubarb) is belonging to Polygonaceae, and its roots and fresh shoots are consumed as vegetable in Turkey. This plant is considered to be one of the most important pharmaceutical raw materials in Middle East. In this study, the antiradical, antimicrobial, cytotoxic and bioactive properties of water, ethanol, and methanol extracts of R. ribes stems were determined. R. ribes stems water, ethanol and methanol extracts are better scavenged ABTS(center dot+) (99.27, 99.91, and 99.88%), DPPH center dot (83.11, 81.42, and 83.26%), and OH center dot radicals (93.49, 94.21, 95.86%) than standard antioxidant BHA (95.32, 80.49, and 93.78%). Stems of R. ribes abundantly include bioactive compounds, dominated by rutin, catechin, caffeic acid, ferulic acid, alpha-tocopherol and vitamin D. These extracts show effective cytotoxic properties against PC-3, A2780, HCT-116 and MCF-7 cancer cell lines at 24h. It is found that R. ribes contain high amount important bioactive contents, and has effective antiradical and cytotoxic properties.Öğe In vitro and histological investigation of antitumor effect of some triazole compounds in colon cancer cell line(Wiley, 2019) Parlak, Akif Evren; Tekin, Suat; Karatepe, Arzu; Koparir, Pelin; Telceken, Hafize; Ceribasi, Ali Osman; Karatepe, Mustafa1,2,4-Triazoles are used as antifungal, antibacterial, antimicrobial, and antioxidant against some oxidative radical species. Recently, many 1,2,4-triazoles continue to be synthesized. In this study, the effect of the 1,2,4-triazole derivatives on human colon cancer (HT29) was investigated in vitro and in vivo in rats. MTT test was applied to in in vitro experiments. For in vivo study, rats were divided into seven groups as follows: Control group (negative control), azoxymethane (AOM), AOM+cisplatin 15, AOM+L1, AOM+L2, AOM+L3, and AOM+L4. To create colon cancer, the AOM injection was injected subcutaneously at a dose of 15mg/kg, three times (once weekly). The in vivo studies were completed at 28 weeks. It was found that the 1,2,4-triazole derivatives reduced the cell viability (P<0.05). In all animals in the experimental groups, mild dysplasia was detected in 100% of the colon mucosal epithelium. Severe dysplasia and adenocarcinoma were observed in L1 groups. As a result, this study determined that the 1,2,4-triazole derivatives exhibit antitumor activity.Öğe In vitro Antiradical, Antimicrobial and Antiproliferative Activities and Phytochemical Compositions of Endemic Alcea calvertii (Boiss) Boiss. Flowers(2020) Keser, Serhat; Keser, Fatma; Tekin, Suat; Kaygılı, Ömer; Turkoglu, Ismail; Demır, Ersin; Karatepe, Mustafa; Kırbağ, Sevda; Yılmaz, Okkes; Sandal, Suleyman; Turkoglu, SemraAbstract: Alcea calvertii (Boiss) Boiss. is belonged to Malvaceae family, and it is a perennial herbaceous endemic plant. Alcea genus plants are grown as ornamental plants in the gardens. In the present study, the antiproliferative, antimicrobial, antiradical activities and phytochemical compositions of ethanol, water, methanol and acet one extracts of A. calvertii flowers were examined. A. calvertii flowers water, ethanol, methanol and acetone extracts are lower scavenged DPPH, ABTS and OH radicals than standard antioxidant trolox. A. calvertii flowers contain vitamins, sterols, flavonoids and phenolic acids, dominated by vanillic acid, gallic acid, catechin, ?-tocopherol, ergosterol and vitamin D. A. calvertii flowers water extract showed better antiproliferative activities than other extracts against to MCF-7 and HCT-116 cell lines. A. calvertii flowers methanol extract showed higher antiproliferative effect against to LNCaP cell lines.Öğe In Vitro Biological Evaluation and Phytochemical Contents of Three Centaurea L. Species Growing from Eastern Anatolia in Turkey(2020) Keser, Serhat; Keser, Fatma; Turkoglu, Ismail; Kaygılı, Ömer; Tekin, Suat; Demır, Ersin; Karatepe, Mustafa; Yılmaz, Ökkeş; Kırbağ, Sevda; Sandal, Suleyman; Turkoglu, SemraAbstract: Centaurea L. species were used as medicinal plants among the people for treatment of the common cold, abscesses, peptic ulcers, hemorrhoid and diabetes etc.. In the present study, antiradical properties, phytochemical contents, antimicrobial and antiproliferative activities of three Centaurea species were investigated. Centaurea saligna (K.Koch) Wagenitz methanol (99.94%), Centaurea virgata Lam. methanol (98.23%) and water (98.10%) extracts were showed higher ABTS scavenging than trolox (96.79%). Centaurea kurdica Reichardt extracts showed lower activity than trolox for all the antiradical assays. Centaurea extracts exhibited antimicrobial activity against to some microorganisms. It was determined that these Centaurea species contain high amount of total flavonoid, phenolic and proanthocyanidin, phenolic acids, phytosterols and unsaturated fatty acids. Also, three Centaurea extracts showed very high antiproliferative property on LNCaP, HCT-116, MCF-7 cancer cell lines.Öğe Investigation of Antiproliferative Properties of Malva neglecta Extracts(Wiley, 2017) Tekin, Suat; Keser, Serhat; Keser, Fatma; Sandal, Suleyman; Turkoglu, Ismail; Karatepe, Mustafa; Turkoglu, Semra[Abstract Not Available]Öğe Investigation of The Anticarcinogenic Effects of Portulaca oleracea Extracts on Different Human Cancer Cell Lines(Wiley, 2017) Sandal, Suleyman; Keser, Serhat; Tekin, Suat; Keser, Fatma; Turkoglu, Ismail; Karatepe, Mustafa[Abstract Not Available]Öğe Rumex acetosella L. (Kuzukulağı)’nın In vitro Antiradikal, Antimikrobiyal, Antikanser ve Fitokimyasal Özellikleri(2022) Keser, Fatma; Karatepe, Mustafa; Keser, Serhat; Tekin, Suat; Turkoglu, Ismail; Kaygılı, Ömer; Demır, ErsinPolygonaceae familyasında yer alan R. acetosella, çok yıllık otsu bir bitkidir ve Türkiye’de halk arasında sebze olarak tüketilmektedir. Bu çalışmada R. acetosella toprak üst kısımlarının etanol, su ve metanol ekstraktlarının antimikrobiyal (Escherichia coli, Bacillus megaterium, Bacillus subtilis, Proteus vulgaris, Pseudomonas aeruginosa, Listeria monocytogenes, Klebsiella pneumoniae, Staphylococcus aureus bakterileri ve Candida albicansmaya-mantarına karşı), antiradikal (DPPH, ABTS ve OH radikallerine karşı), antikanser (insan prostat kanseri (PC-3), insan kolon kanseri (HCT-116), insan yumurtalık kanseri (A2780) ve insan göğüs kanseri (MCF 7) hücre serilerine karşı) ve fitokimyasal özellikleri (yağda çözünen vitaminler, yağ asitleri, flavonoitler,fitosteroller, fenolik asitler, toplam fenolik bileşik, toplam flavonoit ve toplam proantosiyanidinler) incelenmiştir. Sonuçlarımıza göre R. acetosella ekstraktlarının ABTS, DPPH ve OH radikali yok etme testlerinde BHT’den daha yüksek aktiviteye sahip oldukları belirlenmiştir. Ayrıca bu bitkinin yüksek antimikrobiyal aktiviteye ve fitokimyasal içeriğe sahip olduğu, PC-3 insan prostat kanseri hücrelerine karşı etkili antikanser aktivite gösterdiği anlaşılmıştır. Aynı zamanda sunulan çalışma, R. acetosella ekstraktlarının in vitro antikanser aktivitesi ile ilgili ilk çalışma olma özelliği taşımaktadır.Öğe Spectroscopic, antiproliferative and antiradical properties of Cu(II), Ni(II), and Zn(II) complexes with amino acid based Schiff bases(Springer Birkhauser, 2014) Genc, Zuhal Karagoz; Selcuk, Sibel; Sandal, Suleyman; Colak, Naki; Keser, Serhat; Sekerci, Memet; Karatepe, MustafaNovel six Cu(II), Ni(II), and Zn(II) complexes with Schiff bases derived from 4-aminobenzoic acid with terephtaldehyde and amino acids (glycine, beta-alanine). Structures have been proposed from elemental analysis, UV-Vis, IR, NMR, TGA, DTA, and magnetic measurements. Spectroscopic studies suggest that coordination occurs through azomethine nitrogen, hydroxyl group, and carbonyl oxygen of the ligands to the metal ions. The elemental analyses of the complexes where L is Schiff base ligands, are confined to the stoichiometry of the type M2L2(CH3COO)(2) [M = Cu(II)]; and M2L(CH3COO)(2) [M = Ni(II) and Zn(II)]. The cytotoxicity activities of the compounds against human breast carcinoma MCF-7 cell line have been studied. Ligands and their Zn(II) compounds inhibited cell proliferation of MCF-7 cancer cell lines in a dose- and time-dependent manner. The free radical scavenging activity was measured by 1,1-diphenyl-2-picryl-hydrazil. Our results show that the synthesized compounds induced oxidative damage by increasing the lipid peroxidation in yeast since MDA formation was increased, and it could be concluded that the synthesized compounds caused oxidative stress. In addition, the antioxidant activities of the synthesized compounds were very much lower than those of standard antioxidants.
