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DAĞ, AYDAN

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AYDAN
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DAĞ
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    PublicationOpen Access
    Synthesis and Characterization of Biodegradable Amphiphilic Star and Y-Shaped Block Copolymers as Potential Carriers for Vinorelbine
    (2014-01-01T00:00:00Z) Bahadori, Fatemeh; Dag, Aydan; Durmaz, Hakan; Cakir, Nese; ONYUKSEL, Hayat; Tunca, Ümit; Topcu, Gulacti; Hızal, Gürkan; BAHADORİ, FATEMEH; DAĞ, AYDAN; TOPÇU, GÜLAÇTI
    Two amphiphilic block copolymers using hydrophobic poly(e-caprolactone) (PCL) and hydrophilic poly(ethylene glycol) (PEG) were successfully synthesized. One of them is an (A-b-B)(4) type star polymer [(PCL-b-PEG)(4)] and the other one is a Y-shaped PEG-(PCL)(2). A star-shaped polymer (PCL-b-PEG)(4) was prepared by ring-opening polymerization (ROP) of epsilon-caprolactone continued by click reaction of (PCL-azide)(4) and PEG-alkyne. The synthesis of Y-shaped PEG-(PCL)(2) block copolymer was carried out via Diels-Alder click reaction of a furan protected maleimide end-functionalized PEG (PEG-MI) with an anthracene end-functionalized PCL following the ROP of epsilon-caprolactone. The characterization of micelles is carried out using both materials in aqueous media as drug delivery vehicles, which showed satisfying results and enhanced the cytotoxic effect of the anti-cancer drug vinorelbine (VLB). However, micelles consisted of Y-shaped unimers were found to be more convenient for delivery of hydrophobic drugs such as VLB because they formed in lower concentration, carrying a higher amount of drugs and owing a monomodal distribution. We concluded that the free tails of hydrophobic chains in Y-shaped block copolymer facilitate the assembly of amphiphilic material in water to form micelles.
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    PublicationOpen Access
    Design, synthesis and docking study of novel coumarin ligands as potential selective acetylcholinesterase inhibitors
    (2017-01-01) Sonmez, Fatih; KURT, Belma Zengin; Gazioglu, IŞIL; BASILE, Livia; Dag, AYDAN; CAPPELLO, Valentina; GINEX, Tiziana; Kucukislamoglu, Mustafa; GUCCIONE, Salvatore; ZENGİN KURT, BELMA; GAZİOĞLU, IŞIL; DAĞ, AYDAN
    New coumaryl-thiazole derivatives with the acetamide moiety as a linker between the alkyl chains and/or the heterocycle nucleus were synthesized and in vitro tested as acetylcholinesterase (AChE) inhibitors. 2-(diethylamino)-N-(4-(2-oxo-2H-chromen-3-yl)thiazol-2-yl)acetamide (6c, IC50 value of 43 nM) was the best AChE inhibitor with a selectivity index of 4151.16 over BuChE. Kinetic study of AChE inhibition revealed that 6c was a mixed-type inhibitor. Moreover, the result of H4IIE hepatoma cell toxicity assay for 6c showed negligible cell death. Molecular docking studies were also carried out to clarify the inhibition mode of the more active compounds. Best pose of compound 6c is positioned into the active site with the coumarin ring wedged between the residues of the CAS and catalytic triad of AChE. In addition, the coumarin ring is anchored into the gorge of the enzyme by H-bond with Tyr130.
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    PublicationOpen Access
    Assessment of in vitro cytotoxic and genotoxic activities of some trimethoprim conjugates
    (2018-06-01) Bayulken, Devrim Guzel; Bostancioglu, R. Beklem; Koparal, A. Tansu; Tuylu, Berrin Ayaz; Dag, AYDAN; Benkli, KADRİYE; DAĞ, AYDAN; BENKLİ, KADRIYE
    Trimethoprim, a commonly used antibacterial agent, is widely applied in the treatment of variety of infections in human. A few studies have demonstrated an extensive exposure of man to antibiotics, but there is still a lack of data for cytotoxic effects including nephrotoxicity, gastrointestinal toxicity, hematotoxicity, neurotoxicity and ototoxicity. The main purpose behind this study was to determine cytotoxic and genotoxic activities of trimethoprim (1), trimethoprim with maleic acid (2) and trimethoprim in conjugation with oxalic acid dihydrate (3). The cytotoxic effects of these three conjugates were elucidated by employing 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoium bromide (MTT) assay using embryonic rat fibroblast-like cell line (F2408) and H-ras oncogene activated embryonic rat fibroblast-like cancer cell line (5RP7). Additionally, determination of genotoxic activity of these three compounds were studied by using cytokinesis blocked micronucleus assay (CBMN) in human lymphocytes. The results demonstrated that trimethoprim alone and its combination with other compounds are able to induce both cytotoxic and genotoxic damage on cultured cells (F2408, 5RP7, human lymphocytes).
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    PublicationOpen Access
    Cytotoxic, Apoptotic and Genotoxic Effects of Lipid-Based and Polymeric Nano Micelles, an In Vitro Evaluation
    (2017-11-01) BAHADORİ, FATEMEH; KOÇYİĞİT, ABDÜRRAHİM; DAĞ, AYDAN; TOPÇU, GÜLAÇTI; BAHADORİ, FATEMEH; KOÇYİĞİT, ABDÜRRAHİM; DAĞ, AYDAN; TOPÇU, GÜLAÇTI
    Self-assembly systems (SAS) mainly consist of micelles, and liposomes are the classes of Nano Drug Delivery Systems with superior properties compared to traditional therapeutics in targeting cancer tumors. All commercially available nano-formulations of chemotherapeutics currently consist of SAS. According to our knowledge, a specific toxicity comparison based on material differences has not yet been performed. The purpose of this study was to evaluate and compare the toxicity of two SAS consisting of Sterically Stabilized Micelles (SSM) made of a lipid-based amphiphilic distearoyl-sn-glycero-phosphatidylethanolamine-polyethylene glycol (PEG)-2000 and a polymeric micelle (PM) consisting of Y-shape amphiphilic block copolymer, synthesized using poly ε-caprolactone and PEG. The mechanism of cytotoxicity and genotoxicity of micelles on L-929 healthy mouse fibroblast cells was assessed using Sulforhodamine-B, WST-1, Acridine Orange/Ethidium Bromide and alkaline single-cell gel electrophoresis assays. Results showed that SSM in conc. of 40 mg/mL shows very low cytotoxicity at the end of 24, 48 and 72 h. The DNA damage caused by SSM was much lower than PM while the latter one showed significant toxicity by causing apoptosis with the ED50 value of 3 mg/mL. While the DNA damage caused by SSM was ignorable, some DNA chain breaks were detected on cells treated with PM.
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    PublicationOpen Access
    Synthesis and biological evaluation of novel coumarin-chalcone derivatives containing urea moiety as potential anticancer agents
    (2020-01-01T00:00:00Z) Kurt, BELMA; Kandas, Nur Ozten; DAĞ, AYDAN; Sonmez, Fatih; Kucukislamoglu, Mustafa; ZENGİN KURT, BELMA; DAĞ, AYDAN
    The increasing interest on new drug discovery is constantly up to date as drugs do not increase survival adequately against increasing cancer cases worldwide. Based on the reported anticancer activity of coumarin, chalcone and urea derivatives, the present investigation dealt with the design and synthesis of coumarin derivatives bearing diversely substituted chalcone-urea moieties 5a-k. Through a structure-based molecular hybridization approach, a series of novel coumarin-chalcone derivatives containing urea moiety was synthesized and screened for their in vitro antiproliferative activities against the cancer cell lines (H4IIE and HepG2). In addition, the synthesized compounds were tested on a cell line that was not cancerous (CHO) and the damage, it could give to normal cells was determined. Among the synthesized compounds, 5k exhibited better inhibition of H4IIE compared to Sorafenib. 5j also showed better inhibition against HepG2 than Sorafenib. In particular, 5k induced H4IIE apoptosis, arrested cell cycle at the S phase. Therefore, 5k and 5j may be potent antitumor agents, representing a promising lead for further optimization. (C) 2017 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University.
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    PublicationOpen Access
    GLUT-Targeting Phototherapeutic Nanoparticles for Synergistic Triple Combination Cancer Therapy.
    (2023-02-12T21:00:00Z) Cetin Ersen, Busra; Goncu, Beyza; Dag, Aydan; Birlik Demirel, Gokcen; DAĞ, AYDAN; GÖNCÜ, BEYZA SERVET
    The combination of multimodal therapies into one nanocarrier system is promising for its potential to enhance treatment performance by overcoming the efficacy problems encountered in conventional monomodal therapy. In this study, targeted and multimodal therapeutic hybrid nanocarriers are fabricated for breast cancer treatments. In this context, the synthesized gold nanorods (AuNRd), photothermal therapy (PTT) agent, are coated with doxorubicin (DOX) conjugated, targeted, and biocompatible tetrablock glycopeptide (P(DMAEMA--HMBAMA--FrucMA)--P(Lys)/DOX, P-DOX) polymer. Here, fructose-based (Fruc) glycopeptide polymer enhances cellular uptake into breast cancer through GLUT5. A photosensitizer molecule, indocyanine green (ICG), was loaded into the particles to provide photodynamic therapy (PDT) upon NIR light at 808 nm. In the final step of the fabrication, the polymer-coated nanoparticles are integrated with antisense ISIS5132 oligonucleotides to prevent apoptotic resistance of cells against drug molecules. The biocompatibility and therapeutic efficacy of the nanoparticles are evaluated on both human normal skin fibroblast cell (CCD-1079Sk) and human breast cancer cell (MCF7) lines. These multimodal therapeutic AuNRd@P-DOX/ICG/ISIS5132 nanoparticles demonstrate an efficient triple synergistic effect of chemo-/PTT/PDT, which is desired for breast cancer treatment. We believe that this promising multimodal therapeutic nanoparticle system can promote the further clinical application in the treatment of breast cancer and can also be adapted to other types of cancer.