Browsing by Author "Ozakpinar, Ozlem Bingol"

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Citation Count: 0
Bangladesh Journal of Pharmacology
(Bangladesh Pharmacological Soc, 2024) Küçükgüzel, İlkay; Guven, Cansu Tamniku; Duracik, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, Ilkay; Eczacılık Meslek Bilimleri Bölümü
[No Abstract Available]
Citation Count: 8
Exercise Improves Testicular Morphology and Oxidative Stress Parameters in Rats With Testicular Damage Induced by a High-Fat Diet
(Wiley, 2022) Şener, Göksel; Ozakpinar, Ozlem Bingol; Kolgazi, Meltem; Sener, Goksel; Arbak, Serap; Ercan, Feriha; Eczacılık Meslek Bilimleri Bölümü
Obesity and male infertility are problems that affect population. Exercise is a nonpharmacological way to reduce the negative health effects of obesity. The purpose of this study was to examine the effects of exercise on hormone levels, blood-testis barrier, and inflammatory and oxidative biomarkers in rats that became obese due to a high-fat diet (HFD). Male rats received a standard diet (STD group) or a HFD (HFD group) for 18 weeks. During the final 6 weeks of the experiment, swimming exercises (1 h/5 days/week) were given to half of these animals (STD + EXC and HFD + EXC groups). Finally, blood and testicular tissues were analysed by biochemical and histological methods. Body weight, leptin, malondialdehyde, interleukin-6, TNF-alpha and myeloperoxidase levels, apoptotic cells and DNA fragmentation were increased, and testis weight, insulin, FSH, LH, testosterone, glutathione and superoxide dysmutase levels, proliferative cells, ZO-1, occludin, and gap junction protein Cx43 immunoreactivity were decreased in the HFD group. All these hormonal, morphological, oxidative and inflammatory biomarkers were enhanced in the HFD + EXC group. It is thought that exercise protected testicular cytotoxicity by regulating hormonal and oxidant/antioxidant balances and testicular function, inhibiting inflammation and apoptosis, as well as preserving blood-testis barrier.
Citation Count: 2
Morphological and Biochemical Investigation of the Healing Effects of Exercise on High Fat Diet Induced Kidney and Bladder Damage
(Marmara Univ, inst Health Sciences, 2022) Şener, Göksel; Ozakpinar, Ozlem Bingol; Kolgazi, Meltem; Sener, Goksel; Ercan, Feriha; Eczacılık Meslek Bilimleri Bölümü
Objective: The aim of this study was to evaluate the ameliorative effects of swimming training on renal and bladder damage caused by a highfat diet (HFD) using morphological and biochemical measurements. Methods: Sprague Dawley rats were fed either standard chow (CONT, 6% fat) or HFD (45% fat) for 18 weeks, these rats were divided into two subgroups at the last 6 weeks of the experiment. The exercise groups (CONT+EXC, HFD+EXC) were trained daily swimming sessions (1 h per day for 5 days/week) during the last 6 weeks. Kidney and bladder samples were prepared for light and electron microscopic examination at the end of experiment. Malondialdehyde, glutathione, interleukin-6, and tumor necrosis factor-a were measured by biochemically. Results: Regular morphology of the renal cortex and bladder mucosa was observed in the CONT and CONT +EXC groups. Degenerated renal corpuscles and proximal tubules in the kidney and degenerated urothelium with leaky tight junctions and mast cell increase in the bladder mucosa were observed in the HFD group. Ameliorated renal cortex and bladder mucosa were observed in the HFD+EXC group. In addition, malondialdehyde, glutathione, interleukin-6, and tumor necrosis factor-a levels were also consistent with the histological findings. Conclusion: HFD-induced renal and bladder damage may be related to increased oxidative damage. It was observed that the histological damage and altered oxidative stress parameters could be reversed by swimming training, and it is thought that moderate swimming exercise may play a role in regulating oxidative stress.
Citation Count: 0
Synthesis and Anti-Hcv Activity of Novel 5-Arylmethylene Derivatives Via Suppression of Ns5b Polymerase and Cox-2
(Elsevier, 2024) Küçükgüzel, İlkay; Lee, Jin-Ching; Ozakpinar, Ozlem Bingol; Kucukguzel, Ilkay; Eczacılık Meslek Bilimleri Bölümü
Hepatitis C (HCV) is a viral infection that leads to forms of acute and chronic liver disease, including cirrhosis (scarring of the liver) and liver cancer. The World Health Organization (WHO) estimated in 2019 that approximately 290,000 people died from hepatitis C (mostly from cirrhosis and hepatocellular carcinoma). Directacting antiviral drugs (DAAs) can cure more than 95% of individuals with hepatitis C infection, while research on the discovery of new antiviral agents is still ongoing. The Hepatitis C virus (HCV) can cause various biochemical changes in liver cells, and some of these changes are associated with the COX-2 enzyme. The identification of its role in promoting growth in liver cells as well as its involvement in various cancer types, including hepatocellular carcinoma, has made COX-2 an important target in the development of new agents effective against HCV. In this study, thirty-six new 5-arylmethylene-2-imino-1,3-thiazolidin-4-one derivatives (5a-s, 6a-s) were synthesized through Knoevenagel condensation of 2-[(4-substitutedpyridin-2-yl)imino]-1,3thiazolidin-4-one derivatives with various aldehydes. Structures of the synthesized compounds were elucidated by the use of spectral and chromatographic techniques, besides elemental analyses. Four compounds were selected for further studies as they were found to suppress the NS5B protein with anti-HCV activity using the Western Blotting method. The selected compounds 5o, 6m, 6r, and 6s inhibited HCV with EC50 values of 8.0 +/- 0.2 mu M, 13.9 +/- 0.45, 9.2 +/- 0.2 mu M, and 12.1 +/- 0.1 mu M, respectively. It was determined that these compounds reduced HCV-induced COX-2 promoter activity in Ava5 cells compared to Huh7 cells. The antiviral effects of the compounds were also investigated on DENV, closely related to HCV due to sharing certain biological, structural, and mechanical properties throughout their life cycles. However, no significant effect was observed in the preliminary screening study, indicating the compounds' specificity for HCV. Considering the relationship between HCV, DENV, and COX-2, the compounds' COX-1 and COX-2 enzyme inhibition potentials were investigated both in vitro and in silico. Compounds 6d, 6e, 6f, and 6m, which exhibited high selective COX-2 inhibition, were discussed for their interactions with the active site. Our study revealed that our target compounds suppressed COX-2 both at the protein level and through enzyme inhibition, thus providing promising findings for the discovery of new anti-HCV effective COX-2 inhibitors.
Citation Count: 25
Synthesis and Anticancer Activity of Novel Hydrazone Linkage-Based Aryl Sulfonate Derivatives as Apoptosis Inducers
(Springer Birkhauser, 2022) Küçükgüzel, Şükriye Güniz; Han, M. Ihsan; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri Bölümü
In the present study, the various 28 hybrid molecules containing hydrazone and sulfonate moieties were synthesized and characterized by FTIR, H-1-NMR, C-13-NMR spectroscopy and LC-MS spectrometry, besides elemental analysis. The compounds were evaluated for their antiproliferative effects against six cancer cell lines, namely A549 (non-small cell lung cancer), MCF-7 (breast cancer), HT-29 (colorectal adenocarcinoma cancer), PC-3 (androgen-independent prostate adenocarcinoma), Hep3B (hepatocellular carcinoma cancer), and HeLa (epitheloid cervix carcinoma cancer). Among all the target compounds, compounds 4g and 4h exhibited more promising effects on MCF-7 cell lines (IC50 = 17.8 mu M and 21.2 mu M, respectively) with high selectivity. Further mechanistic studies proposed that compounds 4g and 4h induced apoptosis is mediated through the intrinsic apoptotic pathway with changes in mitochondrial membrane potential by finally activating caspase-9 and caspase-3. The results have been encouraging enough to merit further investigation. [GRAPHICS] .
Citation Count: 0
Synthesis and Biological Evaluation of New 4-Thiazolidinone Derivatives of Flurbiprofen
(Acg Publications, 2023) Küçükgüzel, Şükriye Güniz; Senkardes, Sevil; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz; Eczacılık Meslek Bilimleri Bölümü
In this study, the synthesis and characterization of 2-(2-fluorobiphenyl-4-yl)-N '-[(substituted methylene]propanehydrazides (3a-s) and 2-(2-fluoro-[1,1'-biphenyl]-4-yl)-N-(5-methyl-2-(substituted aryl)-4oxothiazolidin-3-yl)propanamides (4a-s) are described and also the antiproliferative effect of the compounds on HT 29, HeLa, A549 and MCF-7 cancer cell lines is investigated. Additionally, mouse embryonic fibroblast cells NIH3T3 were also evaluated to determine the selectivity. The results showed that the identified compounds did not cause any toxicity against NIH3T3 cell line. Moreover, N-(2-(3,5-Bis(trifluoromethyl)phenyl)-5-methyl-4-oxothiazolidin-3-yl)-2-(2-fluoro-[1,1'-biphenyl]-4-yl)propanamide (4h) had the most growth inhibitory effect (55.97% inhibition) on HT-29 colorectal adenocarcinoma cell line. The results obtained from the study show that the compound 4h, which has no cytotoxic effect on normal cells, may be an alternative in the treatment of colon cancer.