Browsing by Author "İlhan S."

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    Cytotoxic, genotoxic, oxidative, and irritant effects of zinc pyrithione in vitro
    (Taylor and Francis Ltd., 2020) Güner A.; İlhan S.
    Zinc pyrithione is an organometallic compound with antimicrobial activity used in many industrial products. In this study, cytotoxicity (cell viability, lactate dehydrogenase release, proliferation rate, and mitotic index) and genotoxicity (sister chromatid exchange and micronucleus test) of zinc pyrithione on human lymphocytes were determined. Intracellular zinc concentrations were determined by inductively coupled plasma-optical emission spectrometry. Intracellular antioxidant/oxidant status was evaluated by total antioxidant capacity and total oxidative status assays. Its irritation potential was investigated using the hen’s egg test chorioallantoic membrane model. Up to the highest concentration of 1000 nmol/L, ZnPT did not cause genotoxicity and did not change the proliferation index. Above 500 nmol/L, zinc pyrithione caused an increase in lactate dehydrogenase, oxidative stress, and intracellular zinc levels, while decreasing cell viability and mitotic index level. At 1000 nmol/L, zinc pyrithione caused slight irritation. These results suggest that zinc pyrithione may exert toxic effects via increased oxidative stress on human cellular systems. © 2020 Informa UK Limited, trading as Taylor & Francis Group.
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    Novel benzimidazole derivatives: Synthesis, in vitro cytotoxicity, apoptosis and cell cycle studies
    (Elsevier Ireland Ltd, 2020) Atmaca H.; İlhan S.; Batır M.B.; Pulat Ç.Ç.; Güner A.; Bektaş H.
    The aim of the study was to synthesize a new series of benzimidazole derivatives and to investigate the underlying molecular mechanisms of the potential cell cycle inhibition and apoptotic effects against a panel of selected human cancer cell lines along with HEK-293 human embryonic kidney cells. MTT assay was used to evaluate cytotoxic effects. Muse™ Cell Analyzer was used to assess cell cycle progression. Annexin-V/PI staining assay was used for detecting apoptosis. All the synthesized compounds showed a significant cytotoxic effect against cancer cells with the IC50 values between 9.2 and 166.1 μg/mL. Among the tested derivatives, compound 5 showed significant cytotoxic activity against MCF-7, DU-145 and H69AR cancer cells with the IC50 values of 17.8 ± 0.24, 10.2 ± 1.4 and 49.9 ± 0.22 μg/mL respectively. The compounds 5 was also tested on HEK-293 human embryonic kidney cells and found to be safer with lesser cytotoxicity. The results revealed that compound 5 significantly increased cell population in the G2/M-phase which is modulated by a p53 independent mechanism. Compound 5 caused an increase in the percentage of late apoptotic cells in all tested cancer cells in a concentration-dependent manner. Among all synthesized derivatives, compound 5 the bromo-derivative, showed the highest cytotoxic potential, induced G2/M cell cycle arrest and apoptotic cell death in genotypically different human cancer cells. These results suggest that compound 5 might be a promising agent for cancer therapy and further structural modifications of benzimidazole derivatives may create promising anticancer agents. © 2020 Elsevier B.V.
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    Induction of autophagic cell death by thymoquinone in docetaxel resistant prostate cancer cells; [Dosetaksel dirençli prostat kanseri hücrelerinde timokinon tarafından otofajik hücre ölümünün indüklenmesi]
    (Duzce University Medical School, 2021) İlhan S.; Oğuz F.
    Aim: Acquired docetaxel (DOC) resistance of prostate cancer (PCa) is still a clinical problem. In addition to failure in chemotherapy treatment, it causes tumor recurrence. Therefore, novel and more effective compounds are needed in DOC-resistant PCa treatment. This study aimed to investigate the possible cytotoxic and cell death-inducing activities of thymoquinone (TQ), one of the main active components of Nigella sativa L., on DOC-resistant prostate cancer cells. Material and Methods: DOC-resistant PC3 cells (DOC-R/PC3) were developed by the continuous culture with increment concentrations of DOC (1-10 nM) until they improved their growth and division abilities. The cell viability was determined by MTT assay. The Muse™ Annexin V & Dead Cell kit was performed to detect apoptotic cell death. Autophagic vacuoles were observed by staining autophagic vacuoles. The levels of LC3I, LC3II and Beclin-1 proteins were investigated via western blot analysis. Results: TQ inhibited the viability of DOC-R/PC3 cells in a dose-and time-dependent manner (p=0.014). The IC50 value of TQ for DOC-R/PC3 cells was calculated as 60 µM at 72 h. Treatment of TQ did not induce apoptotic cell death in DOC-resistant prostate cancer cells but induced the formation of autophagic vacuoles. Moreover, Beclin-1 and LC3-II protein levels were increased in TQ-treated DOC-R/PC3 cells, however, LC3-I levels were decreased in DOC-R/PC3 cells. Conclusion: All these results show that TQ may become a new therapeutic target for DOC-resistant prostate cancer in the future. © 2021, Duzce University Medical School. All rights reserved.
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    GC-MS Analysis and Apoptotic Effect of Paliurus spina-christi Mill. Leaf and Flower Extracts against Breast Cancer Cells
    (Sakarya University, 2022) Oguz F.; Çamli Pulat Ç.; İlhan S.; Atmaca H.
    In recent years, herbal medicines have become a significant novel source of treatment for various types of cancer, including breast cancer. Various investigations have declared that Paliurus spina-christi Mill. (PSC) shows antioxidant, antifungal, antimicrobial, and antibacterial properties, but its effect on cancer cells is unknown. This study purposed to evaluate the possible anti-cancer effects of the ethanolic extract of the PSC in human MCF-7 and MDA-MB-231 breast cancer cells. The leaf and flower extracts of PSC were prepared in ethanol and volatile compounds were determined by GC-MS analysis. The possible cytotoxic effects of extracts were evaluated via MTT assay. Apoptotic effect was examined using the PI Annexin V Apoptosis Detection Kit. Significant cytotoxic effects were detected after 72 h treatment of ethanolic leaf and flower extracts in MCF-7 cells but not in MDA-MB-231 cells. Both leaf and flower extracts of PSC induced apoptotic cell death in MCF-7 cells. On phytochemical screening, it was shown that the leaf extract of PSC contains pyrrolidine, 2-decenal, 2-undecanal, phytol, oleic acid, oleamide, squalane, vitamin E, and gamma-sitosterol and the flower extract contains pyrrolidine, 2-decenal, 2-undecenal, oleic acid, lupeol, and gamma-sitosterol. These data report that PSC leaf and flower extracts have cytotoxic and apoptotic effects in MCF-7 breast cancer cells. Moreover, this study can be considered an in vitro background for further in vivo cancer experiments. © 2022, Sakarya University. All rights reserved.
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    Potential Anti-SARS-CoV-2 Effects of Gossypol and AT-101: Molecular Docking Study Against Angiotensin Converting Enzyme 2
    (Sakarya University, 2024) İlhan S.; Atmaca H.
    This study explores the potential anti-SARS-CoV-2 effects of gossypol (GP) and its AT-101 derivative through in silico molecular docking simulations. GP and AT-101 are natural and modified compounds, respectively, with promising biological activities. Using Autodock Vina software, molecular docking simulations were performed to assess the binding interactions between GP, AT-101, and the receptor binding domain of angiotensin-converting enzyme 2 (ACE2) which plays a vital role in facilitating viral entry into host cells. The docking results revealed that GP and AT-101 exhibited favorable interactions with ACE2, suggesting their potential as anti-SARS-CoV-2 agents. GP formed seven hydrogen bonds with ACE2, while AT-101 formed eight, indicating more stable binding and superior interaction. However, it is important to acknowledge that these findings are based on in silico modeling and further research is required to validate the antiviral properties of l and AT-101 in vitro and in vivo. Moreover, the long-term safety and efficacy of these compounds for COVID-19 treatment warrant further investigation through clinical trials. In conclusion, this in silico study provides preliminary evidence of the potential anti-SARS-CoV-2 effects of GP and AT-101 by demonstrating their ability to interact with ACE2. However, it is important to acknowledge that these findings are based on in silico modeling and further research is required to validate the antiviral properties of GP and AT-101 in vitro and in vivo. © 2024, Sakarya University. All rights reserved.