Browsing by Author "Arslan, Sevki"

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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.
Design, Synthesis and Pharmacological Evaluation of Novel Artemisinin-Thymol
(Taylor & Francis Ltd, 2022) Kavak, Emrah; Mutlu, Dogukan; Ozok, Omruye; Arslan, Sevki; Kivrak, Arif
A molecular hybridization of natural products is a new concept in drug discovery and having critical roles to design new molecules with improved biological properties. Hybrid molecules display higher biological activities when compared to the parent drugs. In the present study, two natural products (thymol and artemisinin (ART)) are used for the synthesis of new hybrid thymol-artemisinin. After characterization, the cytotoxic activity of ART-thymol was tested against different cancer cell lines and non-cancerous human cell line. ART-Thymol show the cytotoxic effect with EC50 values 70,96 mu M for HepG2, 97,31 mu M for LnCap, 6,03 mu M for Caco-2, 77,98 mu M for HeLa and 62,28 mu M for HEK293 cells, respectively. Moreover, ART-Thymol was checked for drug-likeness, and the kinase inhibitory activity. ART-Thymol is investigated by using molecular docking. The results of qPCR was indicated CDK2 and P38 were inhibited by ART-Thymol. These results improved that thymol-artemisinin may be new candidates as an anticancer agents. [GRAPHICS] .
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.
Identification of 3-Bromo as a Potent Anticancer Agent With Promising Inhibitory Effects on Gst Isozymes
(Bentham Science Publ Ltd, 2021) Yilmaz, Can; Arslan, Sevki; Mutlu, Dogukan; Konus, Metin; Kayhan, Abdussamet; Kurt-Kizildogan, Aslihan; Kivrak, Arif
Background: Indole-based heterocyclic compounds play important roles in pharmaceutical chemistry due to their unexpected biological and pharmacological properties. Objective: Herein, we describe novel biological properties (antioxidant, antimicrobial and anti-cancer) of 3-bromo-1-ethyl-1H-indole (BEI) structure. Method: BEI was synthesized from 1-Methyl-2-phenylindole and N-bromosuccinimide and was characterized by using 1H and 13C NMR. Cytotoxicity was determined by MTT assay. Apoptosis analysis of BEI was determined by Arthur (TM) image-based Cytometer. Different methods were applied to assess the antioxidant activity of BEI. Molecular docking studies were conducted to determine the interactions of bonding between GST isozymes and BEI. Results: According to the antioxidant and antimicrobial activity assays, BEI compound showed reduced total antioxidant activity compared to the Trolox standard, whereas it showed moderate antimicrobial activity against Aspergillus niger and Phytophora eryhtrospora. Notably, the BEI compound demonstrated substantial selective cytotoxicity for the first time towards cancer cell lines, and there existed a significant decrease in the percentage of live cells treated with BEI, in comparison to the control ones. Interestingly, BEI exhibited a promising glutathione S-transferase isozymes inhibition. Conclusion: The results of this study suggest that BEI seems to be a promising molecule to be used in the design of new anti-cancer agents that provide superiority to present commercial anti-cancer drugs.
A Novel 4h-Chromen Derivative From Marine Streptomyces Ovatisporus S4702t as Potential Antibacterial and Anti-Cancer Agent
(Bentham Science Publ Ltd, 2022) Kurt-Kizildogan, Aslihan; Akarsu, Neslihan; Otur, Cigdem; Kivrak, Arif; Aslan-Ertas, Nevroz; Arslan, Sevki; Sahin, Nevzat
Background: Marine actinomycetes are among indispensable sources of natural bioactive compounds with unique antimicrobial and anti-cancer activities. Objective: Herein, it was aimed to elucidate the bioactive potential of a marine-derived Streptomyces ovatisporus Methods: Streptomyces ovatisporus S4702T was cultured in N-Z Amine broth, and extraction was carried out using different organic solvents. Bioassay-guided purification was followed by chemical characterization using NMR and LC-MS/MS. The compound was then evaluated for its antibacterial, antioxidant and cytotoxic activities. Results: Etyl acetate extracts gave the highest antibacterial activity, and chemical characterization of this extract indicated the formula as C15H29O5N3 and the corresponding possible molecular structure as 4H-chromen-4-one derivative. It was found highly potent against Bacillus subtilis ATCC 6633 (MIC: 0.25 mu g ml-1) and Micrococcus luteus ATCC 9341 (MBC: 0.5 mu g ml-1). It has no remarkable antioxidant activity, but a higher EC50 value and less cytotoxicity against normal cells. The EC50 values of this chromen derivative were found as 9.68 mu g ml-1 for human colon carcinoma, 9.93 mu g ml-1 for human prostate adenocarcinoma and 25.5 mu g ml-1 for human embryonic kidney cells. Conclusion: Overall, the presented 4H-chromen-4-one derivative is a remarkable bioactive compound with potent antibacterial and cytotoxic activity. With its high bioactive potential, it is proposed as a good candidate in medicine.
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, 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.
Synthesis, Cytotoxicity, Antioxidant and Antimicrobial Activity of Indole Based Novel Small Molecules
(Bentham Science Publ Ltd, 2021) Kurt-Kizildogan, Aslihan; Otur, Cigdem; Yilmaz, Can; Arslan, Sevki; Mutlu, Dogukan; Kivrak, Arif; Konus, Metin
Aims: In this study experiments were carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1Hindole (EPI) together with its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells. Background: Indoles probably represent one of the most important heterocyclic structures that have been attracting the interest of many scientists in drug discovery. Objective: The present study was carried out to explore antioxidant, antimicrobial, cytotoxic properties of novel indole derivative 1-ethyl-2-phenyl-3-phenylethyl-3-thiophen-2-yl-1H-indole (EPI) and its effect on glutathione S-transferases (GST) activities in human liver carcinoma (HepG2) cells. Materials and Methods: Pd-catalyst Sonogashira coupling reactions, MTT Assay, Antioxidant capacity test, Antimicrobial test, GST enzyme activity test Results: 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties. It displayed significant induction in glutathione S-transferases (GST) enzyme activity in human liver cancer cell lines (HepG2), but cytotoxic effect on all tested cancer cell lines could not be observed. Conclusion: All of these results showed that 1-ethyl-2-phenyl-3-(phenylethynyl)-1H-indole had antioxidant and antimicrobial properties without cytotoxic effect, which could make it a promising active component with further studies..