Browsing by Author "Cetin, Dogan"

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Cytotoxicity, Apoptotic, Antioxidant and Antimicrobial Activity of Dictyota Dichotoma (Hudson) Jv Lamouroux 1809 Collected From Antalya Coast, Turkiye
(Pleiades Publishing inc, 2025) Arslan, Sevki; Abdelsalam, Amine Hafis; Kizildogan, Aslihan Kurt; Otur, Cigdem; Konus, Metin; Cetin, Dogan; Okudan, Emine Sukran
Current study was purposed to reveal the cytotoxic, apoptotic, antimicrobial and antioxidant potentials of oil extracted from Dictyota dichotoma (Hudson) J.V. Lamouroux 1809 collected from Antalya coast of Turkiye. Dictyota dichotoma oil showed better cytotoxic activity towards two different adenocarcinoma cell lines (Caco-2 (8.83 mu g/mL) and LnCap (10.86 mu g/mL)) compared to HEK293 cells (non-cancerous). Annexin V/PI staining and qPCR studies revealed that oil caused induction of apoptosis. Dictyota dichotoma oil inhibited the growth of Aspergillus niger ATCC 16404 and Enterococcus faecalis ATCC 29212. Nevertheless, the lower antioxidant activity of Dictyota dichotoma oil was determined compared with trolox standard for both DPPH and ABTS assays (4.8 fold less). In conclusion, Dictyota dichotoma oil has a promising potential in medical usage.
Determination of Antioxidant, Antimicrobial and Anticancer Properties of Newly Synthesized 2-Methoxyphenyl Thiophene Derivatives
(Wiley-v C H verlag Gmbh, 2024) Cetin, Dogan; Konus, Metin; Yilmaz, Can; Arslan, Sevki; Abdelsalam, Aminehafis; Hutanu, Elena Daniela; Kivrak, Arif
In this study, antioxidants, anticancer, and antimicrobial properties of four newly synthesized thiophene derivatives were investigated. In addition, basic ADME properties were calculated in silico. According to the study's findings, tested compounds antioxidant activity was weaker than the standards in both the FRAP and ABTS assays. The MTT analysis revealed that the chemicals 3 and 4 were cytotoxic to every cancer cell line that was tested. 3 and 4 increased the rate of apoptosis in the tested cancer cells at levels close to that in the positive control group. The gene expression levels of apoptotic markers (BAX, Bcl-2, Casp-3, -8, and -9) detected at all cell lines after incubation with 3 and 4 were changed as expected for apoptotic agents, except Bcl-2 of HT-29. It was concluded that the addition of bromine to C2 of thiophene cycle of 3, resulted 4 with greater apoptotic potential probably because of a change in molecular conformation and ligand exchange kinetics. Compound 3 was found to have antifungal activity against Aspergillus niger, while 4 was found to have antibacterial activity on gram-positive bacteria. In silico ADME/T analysis revealed that 3 and 4 were able to pass through the gastrointestinal tract lumen and blood-brain barrier.
The Effects of Different Charleston Pepper Cultivars on the Demographic Parameters and the Antioxidant Levels of Myzus Persicae (Sulzer, 1776) (Hemiptera: Aphididae)
(Entomological Soc Turkey, Ege Univ, 2023) Ozgokce, Mehmet Salih; Kusoglu, Duygu; Konus, Metin; Kara, Hilmi; Risvanli, Mehmet Ramazan; Cetin, Dogan
Host plant diversity causes differences in the biology and adaptation of insects. In this study, variations in some biological properties and adaptive antioxidative response of Myzus persicae (Sulzer,1776) (Hemiptera: Aphididae) on five Charleston pepper, Capsicum annuum L. (Solanaceae) cultivars were investigated under laboratory conditions (25 & PLUSMN;1 & DEG;C, 60 & PLUSMN;5% RH). The lowest intrinsic rate of increase (r = 0.193 d-1) of M. persicae was estimated in the tested cohort fed with the Kanyon cultivar, while the highest intrinsic rate of increase (r = 0.248 d-1) was found on the Tufan cultivar. The cohort fed with Safkan cultivar exhibited the highest levels of GST-CDNB and EST-PNPA at 562.80 and 207.64 nmol/mg protein, respectively, whereas the cohort fed with Kanyon cultivar showed the lowest levels at 317.04 and 132.14 nmol/mg protein, respectively. Analysis of life table parameters and enzymatic/non-enzymatic antioxidant levels of M. persicae showed that among the cultivars we tested, the Tufan cultivar was the most preferred host by M. persicae, while Kanyon cultivar was a less suitable host.
The Effects of Water Quality and Brewing Type on Total Antioxidant Capacity in Herbal Teas
(Kahramanmaras Sutcu Imam Univ Rektorlugu, 2021) Yilmaz, Can; Konus, Metin; Fidan, Ceylan; Ergin, Derya; Cetin, Dogan; Dilek, Zeynep; Elasan, Esma
The antioxidant capacity of the polyphenols is the basis of the potential health benefits of herbal tea consumption. In this study. the effects of infusion time. presence of tea packs and water quality on the extraction yield of polyphenolic compounds providing antioxidant activity of melissa, rosehip, fennel, camomile and white tea, which are commonly consumed in Turkey. were investigated. Antioxidant activities were determined by using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The results of the study showed that the antioxidant activity of herbal teas brewed with distilled water was higher than that in tap water, and that antioxidant activity increased for these teas due to the increased infusion time. When tap water was used, it was determined that a higher antioxidant activity was obtained as a result of brewing for 3 minutes for rosehip and melissa tea and 10 minutes for white tea. The results also showed that packaged brewing for rosehip and fennel tea; and, unpackaged brewing for chamomile, melissa, and white tea resulted in higher antioxidant activity.
Synthesis and Biological Activity of New Indole Based Derivatives as Potent Anticancer, Antioxidant and Antimicrobial Agents
(Elsevier, 2022) Konus, Metin; Cetin, Dogan; Kizilkan, Nurhan Didem; Yilmaz, Can; Fidan, Ceylan; Algso, Muheb; Arslan, Sevki
Indoles have very critical roles to design new biologically active molecules in medicinal chemistry. They display higher biological activities or create new biological properties when compared to the other heteroaromatic compounds. In the present study, 1-ethyl-2-phenyl-3-(thiophen-2-yl)-1H-indole (3), 8-ethyl-8H-benzo[a]thieno[3,2-c]carbazole (4), 1-ethyl-2-phenyl-3-(5-(phenylethynyl)thiophen-2-yl)-1H-indole (6) and 1-ethyl-3-(furan-2-yl)-2-phenyl-1H-indole (7) are prepared via Pd-catalyzed cross-coupling reactions and iodocyclization reactions. It was determined that compound 3 and 7 were also seemed to be better drug candidates at the end of in silico evaluation. Furthermore, compound 7 provided the best antibacterial and antifungal activity against the test indicator strains. It showed a potent antifungal effect on Aspergillus niger ATCC 16404 (MIC: 1.17 mu g mL(-1); MFC: 2.7 mu g mL(-1)). In addition, while compounds 3, 6 and 7 showed significantly high molybdenum reducing activity compared to trolox, 7 exhibited almost the same antioxidant activity (EC50 = 7.1 mu M) compared to the trolox standard (EC50 = 5.07 mu M). After characterization, the cytotoxic activities of novel indoles were tested against different cancer cell lines and non-cancerous human cell line. Compound 3 and 7 had selective cytotoxic activity towards cancer cells. EC50 values of compound 3 were found to be 248.15 mu M for LnCap, 139.81 mu M for HepG2, and 164.72 mu M for the Caco-2 cell line. Similarly, The EC50 value of 7 was found as 38.725 mu M for LnCap, 70.02 mu M for HepG2, and 86.98 mu M for Caco-2, and 90.97 mu M for Hek293 cell line. Moreover, it was revealed that these two compounds showed strong apoptotic properties towards these cancer cell lines as described by image cytometry and real time PCR. Consequently, these results improved that our molecules 3 and 7 could be new candidates as anticancer agents and apoptosis inducers. (C) 2022 Elsevier B.V. All rights reserved.
Synthesis of Ethynyl-Thiophene Derivatives, Antioxidant Properties and Adme Analysis
(Wiley-v C H verlag Gmbh, 2022) Konus, Metin; Algso, Muheb; Yilmaz, Can; Khorsheed, Bahzad Ahmed; Koroglu, Asli; Cetin, Dogan; Kivrak, Arif
Herein, novel alkyne based organic compounds, 2-((2-(methylthio)phenyl)ethynyl)thiophene (MAT) and 2-ethynyl-3-(phenylethynyl)thiophene (DAT), were designed and synthesized via Pd-catalyst cross-coupling reactions. The isolated yields of MAT and DAT were obtained as 77 % and 96 %, respectively. After chemical characterization, radical scavenging activities and reduction power capacities of them were determined by DPPH, TEAC, phosphomolybdenum and reducing power methods. MAT showed higher radical scavenging activities than DAT, and comparable with the standard. Moreover, basic ADME properties were calculated in silico. Both of the newly synthesized derivatives were reported with the same moderate to good drug score of 0.42; and, having potential to pass through BBB and GI with no appointed toxic effects.
Synthesis, Biological Evaluation and Molecular Docking of Novel Thiophene-Based Indole Derivatives as Potential Antibacterial, Gst Inhibitor and Apoptotic Anticancer Agents
(Wiley-v C H verlag Gmbh, 2020) Konus, Metin; Cetin, Dogan; Yilmaz, Can; Arslan, Sevki; Mutlu, Dogukan; Kurt-Kizildogan, Aslihan; Kivrak, Arif
Heteroaromatic indoles play a leading role in the development of pharmaceutical, medical, chemical and agricultural fields due to their structural properties. In this study, it was first time that biological properties of (antioxidant, antimicrobial, cytotoxic and apoptotis-induced anticancer) 3-(5-bromothiophen-2-yl)-1-ethyl-2-phenyl-1H-indole 4 and 3-([2,2 '-bithiophen]-5-yl)-1-ethyl-2-phenyl-1H-indole 5 were described. According to the overall results, while 4 did not show any significant cytotoxic, antioxidant and antimicrobial activities, 5 showed high reducing activity and very strong antibacterial activity against Enterococcus faecalis. Furthermore, 5 showed dose-dependent cytotoxic effect in all tested cell lines. The EC50 values of the 5 were found to be 16 mu M for CaCo-2, 29 mu M for LnCaP, 14 mu M for MDA-MB231, 21 mu M for HepG2 and 87 mu M for HEK293 cells, respectively. 5 also caused induction of apoptosis and promising glutathione S-transferase (GST) enzyme inhibition in HepG2 cells. Consequently, 5 could be also considered as a promising medical agent in cancer treatment.
A Thiophene Derivative, 2-Bromo Has Effective Anticancer Potential With Other Biological Properties
(Wiley-v C H verlag Gmbh, 2022) Yilmaz, Can; Pirdawid, Ahmed Othman; Babat, Ceylan Fidan; Konus, Metin; Cetin, Dogan; Kivrak, Arif; Kizildogan, Aslihan Kurt
Thiophene derivatives are studied intensively due to their anticancer, antimicrobial, antioxidant and some other clinically important properties. In this study, the biological properties of a new thiophene derivative, so called BMPT, with a moderate drug score of 0.29 were tested. BMPT showed selective cytotoxicity for LnCap, HepG2 and Caco-2 cancer cell lines with EC50 values of 138.573 mu M, 185.931 mu M, and 108.657 mu M, respectively, but not on the control cell line HEK293. The increased expressions were detected for caspase3, caspase8, caspase9 and Bax; but Bcl-2 expressions were decreased at cancer cell lines. BMPT decreased the total thiol content and total GST activities at HepG2 47 % and 40 %, respectively, and, molecular docking supported inhibitory models for GSTP1-1, GSTA1-1 and GSTM2-2 were mixed, uncompetitive and uncompetitive, respectively. BMPT also showed potent antibacterial activity against Staphylococcus aureus. Related with its selective inhibition on GST activities, BMPT is proposed to have significant apoptotic effect leaded by changes, especially, in caspase 3, Bcl-2 and Bax expressions.