Scopus İndeksli Yayınlar Koleksiyonu / Scopus Indexed Publications Collection
Permanent URI for this collectionhttps://hdl.handle.net/11147/7148
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Article Citation - WoS: 1Citation - Scopus: 1Investigation of Cytotoxic Properties of Some Isoindole-Related Compounds Bearing Silyl and Azide Groups With in Vitro and in Silico Studies(Taylor & Francis, 2023) Tan, Ayşe; Köse, Aytekin; Mete, Derya; Şanlı Mohamed, Gülşah; Kışhalı, Nurhan H.; Kara, YunusThis study aims to evaluate the synthesis of isoindole-1,3-dione analogues and their cytotoxic potential. A549 and HeLa cells exposed to 250-100-50-25 mu M doses of each derivative were incubated for 24, 48, and 72 h. The cytotoxicity of the isoindole-1,3-dione derivatives was analyzed using the cell growth inhibition assay and the cell membrane damage test. (3aR,5R,6R,7aS)-5-Azido-2-benzyl-6-hydroxyhexahydro-1H-isoindole-1,3(2H)-dione (1d), (3aR,5R,6R,7aS)-5-azido-6-((tert-butyldiphenylsilyl)oxy)-2-ethylhexahydro-1H-isoindole-1,3(2H)-dione (2a), and (3aR,5R,6R,7aS)-5-azido-6-((tert-butyldiphenylsilyl)oxy)-2-methylhexahydro-1H-isoindole-1,3(2H)-dione (2b) compounds inhibited the growth of the A549 and HeLa cells caused membrane damage and exhibited a dose-dependent cytotoxic effect on lung and cervical carcinoma cells. The effect of tert-butyldiphenylsilyl (TBDPS) groups on cytotoxicity was observed in compounds 2a and 2b, but not in the other compounds. Considering the effect of groups attached to the nitrogen atom, the best activity was exhibited in 2b molecule to which the methyl group is attached. Additionally, the interactions of compounds (3aR,5R,6R,7aS)-5-azido-6-hydroxy-2-methylhexahydro-1H-isoindole-1,3(2H)-dione (1b), 1d, 2a and 2b with mammalian rapamycin target, human ribosomal S6 kinase 1 and human epidermal growth factor receptor were investigated by molecular docking studies, . According to the docking results, 2a and 2b compounds containing a TBDPS group have stronger binding energies than 1b and 1d compounds against all target receptors.Article Citation - WoS: 7Citation - Scopus: 7Synthesis and Characterization of Single-Walled Carbon Nanotube: Cyto-Genotoxicity in Allium Cepa Root Tips and Molecular Docking Studies(Wiley, 2022) İnce Yardımcı, Atike; İstifli, Erman Salih; Açıkbaş, Yaser; Liman, Recep; Yağmurcukardeş, Nesli; Yılmaz, Selahattin; Ciğerci, İbrahim HakkıHerein, single-walled carbon nanotubes (SWCNTs) were synthesized by the thermal chemical vapor deposition (CVD) method, and characterized by scanning electron microscopy (SEM), energy-dispersive X-ray spectroscopy (EDX), transmission electron microscopy (TEM), Raman spectroscopy, dynamic light scattering (DLS), and thermo-gravimetric analysis (TGA). The results indicated that obtained nanotubes were SWCNTs with high crystallinity and their average diameter was 10.15 ± 3 nm. Allium cepa ana–telophase and comet assays on the root meristem were employed to evaluate the cytotoxic and genotoxic effects of SWCNTs by examining mitotic phases, mitotic index (MI), chromosomal aberrations (CAs), and DNA damage. A. cepa root tip cells were exposed to SWCNTs at concentrations of 12.5, 25, 50, and 100 μg/ml for 4 h. Distilled water and methyl methanesulfonate (MMS, 10 μg/ml) were used as the negative and positive control groups, respectively. It was observed that MIs decreased statistically significantly for all applied doses. Besides, CAs such as chromosome laggards, disturbed anaphase–telophase, stickiness and bridges and also DNA damage increased in the presence of SWCNTs in a concentration-dependent manner. In the molecular docking study, the SWCNT were found to be a strong DNA major groove binder showing an energetically very favorable binding free energy of −21.27 kcal/mol. Furthermore, the SWCNT interacted effectively with the nucleotides on both strands of DNA primarily via hydrophobic π and electrostatic interactions. As a result, cytotoxic and genotoxic effects of SWCNTs in A. cepa root meristematic cells which is a reliable system for assessment of nanoparticle toxicology were demonstrated in this study.Article Citation - WoS: 8Citation - Scopus: 9Ligand-Based Virtual Screening and Molecular Docking of Two Cytotoxic Compounds Isolated From Papaver Lacerum(Elsevier Ltd., 2019) Bayazeid, Omer; Bedir, Erdal; Yalçın, Funda N.This study revealed that the Papaver lacerum extract strongly inhibited HeLa cell proliferation, resulting in 13% cell viability. As a result of phytochemical studies, one known compound, Tyrosol-1-O-beta-xylopyranosyl-(1 -> 6)-O-beta-glucopyranoside) (I), and one new compound, 5-O-(6-O-alpha-rhamnopyronosyl-beta-glucopyronosyl) mevalonic acid (II), were isolated. Compounds I and II were found to possess a moderate cytotoxic effect with an IC50 of 66.4 mu M (p < 0.0001) and 54 mu M (p < 0.0001), respectively. The ligand-based virtual screening technique was used to reveal the possible molecular target of compounds I and II. The molecular target was identified as protein-tyrosine kinase Syk for compound I, and aldo-keto reductase family-1 for compound II. Molecular docking was used to assess the binding affinity of the compounds with the targets obtained from ligand-based virtual screening.
