WoS İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6
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Article Citation - WoS: 7Citation - Scopus: 5Synthesis and Evaluation of Novel Metacetamol Derivatives With Hydrazone Moiety as Anticancer and Antimicrobial Agents(Wiley-v C H verlag Gmbh, 2023) Senkardes, Sevil; Atlihan, Irem; Cayir, Elif; Tiber, Pinar Mega; Orun, Oya; Nigiz, Seyma; Kucukguzel, S. Guniz; Mega Tiber, PınarBy exploiting the wide biological potential of the hydrazone scaffold, a series of hydrazone derivatives were synthesized, starting from N-(3-hydroxyphenyl)acetamide (metacetamol). The structures of the compounds were determined using IR, H-1 and C-13-NMR, and mass spectroscopic methods. The obtained molecules (3 a-j) were evaluated for their anticancer potential against MDA-MB-231 and MCF-7 breast cancer cell lines. According to the CCK-8 assay, all tested compounds showed moderate to potent anticancer activity. Among them, N-(3-(2-(2-(4-nitrobenzylidene)hydrazinyl)-2-oxoethoxy)phenyl)acetamide (3 e) was found to be the most effective derivative with an IC50 value of 9.89 & mu;M against MDA-MB-231 cell lines. This compound was further tested for its potential effects on the apoptotic pathway. Molecular docking studies was also carried out for 3 e in the colchicine binding pocket of tubulin. Additionally, compound 3 e also demonstrated effective antifungal activity, particularly against Candida krusei (MIC=8 & mu;g/ml), indicating that nitro group at the 4(th) position of the phenyl ring was the most preferable substituent for both cytotoxic and antimicrobial activity. Our preliminary findings suggest that compound 3 e could be exploited as a leading structure for further anticancer and antifungal drug development.Article Citation - WoS: 2Citation - Scopus: 3Petroselinum Crispum Extract Prevents Scopolamine-Induced Lens Damage in Rats(Wiley-v C H verlag Gmbh, 2023) Ertik, Onur; Pazarbasi, Seren Ede; Sener, Goksel; Sacan, Ozlem; Yanardag, RefiyeAlzheimer's disease (AD) is a neurodegenerative disease that occurs especially in advanced ages. It reduces the quality of life of both the patient and their relatives. In addition to its primary effects, AD causes metabolic defects and tissues are damaged due to these effects. Oxidative stress damages cells by disrupting antioxidant/oxidant balance in many tissues, especially due to AD. In individuals with AD and the elderly, lens tissue is damaged due to oxidative stress and may cause vision loss. Therefore, it is very important to investigate herbal products that both prevent/cure AD and reduce AD-related oxidative stress, as they may have fewer side effects. In this study, the protective effects of parsley (Petroselinum crispum) extract on lens tissues of an experimental AD model induced by scopolamine were examined and evaluated through biochemical parameters. The result of biochemical experiments and principal component analysis, was observed that parsley extract had a therapeutic effect by reducing oxidative stress in lens tissues of experimentally induced AD rats. It can be suggested that the phenolic and flavonoid-rich content of parsley extract may have caused the reduction of oxidative damage in lens tissues and can be used to protect lens tissue against oxidative stress due to AD disease.Article Citation - WoS: 3Citation - Scopus: 3A Novel Petox-Based Nanogel Targeting Prostate Cancer Cells for Drug Delivery(Wiley-v C H verlag Gmbh, 2024) Gulyuz, Sevgi; Sessevmez, Melike; Ukuser, Gokcen; Khalily, Melek Parlak; Tiryaki, Selen; Sipahioglu, Tarik; Yilmaz, OzgurThis study focuses on creating a specialized nanogel for targeted drug delivery in cancer treatment, specifically targeting prostate cancer. This nanogel (referred to as SGK 636/Peptide 563/PEtOx nanogel) is created using hydrophilic poly(2-ethyl-2-oxazoline) (PEtOx) through a combination of living/cationic ring-opening polymerization (CROP) and alkyne-azide cycloaddition (CuAAC) "click" chemical reactions. A fluorescent probe (BODIPY) is also conjugated with the nanogel to monitor drug delivery. The characterizations through 1H-NMR, and FT-IR, SEM, TEM, and DLS confirm the successful production of uniform, and spherical nanogels with controllable sizes (100 to 296 nm) and stability in physiological conditions. The biocompatibility of nanogels is evaluated using MTT cytotoxicity assays, revealing dose-dependent cytotoxicity. Drug-loaded nanogels exhibited significantly higher cytotoxicity against cancer cells in vitro compared to drug-free nanogels. Targeting efficiency is examined using both peptide-conjugated and peptide-free nanogels, with the intracellular uptake of peptide 563-conjugated nanogels by tumor cells being 60-fold higher than that of nanogels without the peptide. The findings suggest that the prepared nanogel holds great potential for various drug delivery applications due to its ease of synthesis, tunable functionality, non-toxicity, and enhanced intracellular uptake in the tumor region. This study emphisizes an innovative PEtOx-based nanogel tailored for targeted drug delivery in prostate cancer. Developed using click chemistry, a valuable technique for chemical synthesis, it exhibits consistent nanogel formation with customizable sizes. In vitro, drug-loaded nanogel exhibits potent cytotoxicity against cancer cells. Notably, peptide-conjugated nanogels significantly boost tumor cell uptake, showcasing promising promising potential for effective cancer drug delivey.image