WoS İndeksli Yayınlar Koleksiyonu

Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6

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Subject: search.filters.subject.AntioxidantWoS Q: search.filters.wosQuartile.Q1

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  • Article
    Low Dose Ionising Radiation Elicits MPTP Comparable Alterations in Locomotor Function, Oxidative Balance and Mitochondrial Homeostasis in Zebrafish Embryos
    (Nature Portfolio, 2025) Cahide, Ezgi; Bayramov, Aydas; Beler, Merih; Cansiz, Derya; Unal, Ismail; Egilmezer, Gizem; Yalcinkaya, Sebnem Ercalik
    Prenatal exposure to environmental factors including low-dose ionising radiation and neurotoxins may disrupt the oxidant-antioxidant balance. Our aim was to assess the effects of exposure to low-dose ionising radiation (LDIR) and 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP), which is a neurotoxin used to model Parkinson's disease (PD), on developing zebrafish embryos, focusing on the oxidant-antioxidant system and markers of mitochondrial damage associated with PD. Zebrafish embryos were divided into four groups: control, LDIR, MPTP, and LDIR combined with MPTP (LDIR + MPTP). A dental x-ray unit (60 kVp, 7 mA) was used for the exposures. The 0.08 s LDIR exposure was measured as 0.065 mGy using optically stimulated dosimeters. At the end of 72 h after fertilization, locomotor activities, acetylcholine esterase (AChE) activity, oxidative stress and antioxidant status were assessed. Expressions of genes associated with in PD as markers of mitochondrial damage (pink1, parkin, dj1 and lrrk2) were determined by RT-PCR. Developmental toxicity was observed in all exposure groups as evidenced by pericardial edema, yolk sac edema and spinal curvature. LDIR exposure in zebrafish embryos affected oxidative and mitochondrial stress markers, as well as locomotor activity and AChE as a marker of cognitive function at levels comparable to the MPTP exposure. Our study is the first to determine the effects of LDIR from a dental x-ray unit on the response to MPTP, and we aim to further elucidate the mechanism of these changes observed particularly in the LDIR + MPTP group.
  • Article
    Design and Synthesis of Thiosemicarbazides and 1,2,4-Triazoles Derived From Ibuprofen as Potential Metap (Type II) Inhibitors
    (Elsevier Ireland Ltd, 2025) Yilmaz, Ozgur; Biliz, Yagmur; Ayan, Sumeyra; Cevik, Ozge; Karahasanoglu, Mufide; Cotuker, Reyhan; Kucukguzel, S. Guniz
    In the present study, a range of novel thiosemicarbazides 4a-i and 1,2,4-triazoles 5a-i derived from ibuprofen, were synthesized. Structural elucidation of these synthesized compounds was performed utilizing a variety of spectroscopic methods, including FTIR, 1H NMR, 13C NMR and HR-MS. The synthesized compounds were tested for cytotoxicity in five different cancer cell lines (cervical cancer (HeLa), human breast cancer (MCF-7), human gastric adenocarcinoma (MKN-45), human metastatic prostate cancer (PC3) and human glioblastoma (U87)). The compounds were compared with healthy cells (NIH-3T3) and the most effective compounds were determined by means of the selectivity index. Thiosemicarbazides derived form ibuprofen 4i and 4d showed anticancer activity, while 1,2,4-triazoles derived form ibuprofen 5b, 5c, 5d, 5e, 5h, 5g showed anticancer activity in HeLa, MCF-7, MKN-45, PC3 and U87 cells. To test the stability of the protein-drug complexes all 18 compounds 4a-i and 5a-i were docked into the active site of the MetAP2 enzyme In general, computational inhibition constants values were correlated with the experimental values. The dynamic behavior of MetAP2-inhibitor complexes was analyzed using all atoms Molecular Dynamic (MD) simulations for 200 ns duration. MD revealed that the drugs bind in the active center of MetAP2 with stable RMSD and RMSF. In conclusion, in-silico results and in-vitro studies suggests that thiosemicarbazides and 1,2,4-triazoles derived from ibuprofen may be novel anticancer drug candidates for treating cervical, breast, prostate, gastric and glioblastoma. Compounds provided induction of apoptotic proteins in the cell by inhibiting MetAP2 enzyme. Furthermore, the potential antioxidant activities of the compounds were evaluated using the 2,2-Diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity assay. Among the compounds tested, 4a, 4b, 4e, 4f, 4h, and 4i exhibited values closely resembling the DPPH activity of the standards.