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TOPÇU, GÜLAÇTI

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GÜLAÇTI
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Now showing 1 - 10 of 13
  • PublicationMetadata only
    Synthesis of New Oleanane Triterpenoids Including Fatty Acids Esters and Investigation of Their in vitro Cytotoxic Effects on 3T3 Fibroblast and PC3 Prostate Cancer Cell Lines
    (2019-12-19) Dağ, Aydan; Topçu, Gülaçtı; Atasoy, Sezen; Aktaş, Asude Sena; Şenol, Halil; ŞENOL, HALIL; DAĞ, AYDAN; ATASOY, SEZEN; TOPÇU, GÜLAÇTI
  • PublicationMetadata only
    Computer Aided Design and Synthesis of New Ursane Triterpenoids with Nuclear Factor Kappa B Inhibition Effect
    (2019-12-19) Şenol, Halil; Akdemir, Atilla; Topçu, Gülaçtı; ŞENOL, HALIL; AKDEMİR, ATİLLA; TOPÇU, GÜLAÇTI
  • PublicationMetadata only
    Simultaneous Determination of Phenol and p-Cresol in Human Urine by an HPLC Method
    (2016-06-01) Tekkeli, S. E. Kepekci; Kiziltas, M. V.; Dincel, DEMET; ERKOC, R.; Topcu, GÜLAÇTI; TEKKELİ, ŞERİFE EVRİM; DİNCEL, DEMET; TOPÇU, GÜLAÇTI
    Introduction: In patients with chronic kidney disease (CKD), uremic toxins accumulate in blood and cannot be excreted with urine. Accumulation of these toxins has negative effects on many body functions. Because of the importance of these toxins, we developed and validated a simple, sensitive, accurate, and precise method for the determination of two main uremic toxins:phenol and p-cresol in human urine. Materials and methods:Separation of these analytes in urine samples was achieved by reverse-phase high-performance liquid chromatography (RP-HPLC) with a C18 column at 35 degrees C using the mobile phase of methanol-water (65:35) at a flow rate of 1.4 mL min(-1). Fluorimetric detection was used at 284 nm for excitation and 310 nm for emission. Results:The method is linear over the range of 1.5-35 ng mL(-1) and 1-45 ng mL(-1) for phenol and p-cresol, respectively. The method was applied to urine samples from 10 healthy subjects and 10 chronic kidney disease patients. Conclusions:This assay appears to be useful in routine analysis of clinical samples for simultaneous determination of phenol and p-cresol levels in urine.
  • 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.
  • PublicationMetadata only
    Synthesis of Oleanolic Acid Analogues and Their Cytotoxic Effects on 3T3 Cell Line
    (2018-01-01) Tuncay, Salih; Kocyigit, ABDÜRRAHİM; SEÇEN, Hasan; Ocal, Nuket; Topcu, GÜLAÇTI; Guler, ERAY METİN; ŞENOL, HALIL; GÜLER, ERAY METİN; KOÇYİĞİT, ABDÜRRAHİM; TOPÇU, GÜLAÇTI
    Background: Oleanolic acid (OA) is a known natural compound with many important biological activities. Thirteen oleanolic acid derivatives linked at C-3 and C-28 were synthesized and their structures were confirmed by H-1- and C-13 NMR and mass spectral analyses. Among them, compounds 4, 6, 8-10, 12, 13 were synthesized for the first time. They were evaluated for their cytotoxic activity. They showed proliferative effect at low concentrations while cytotoxic effect was observed at high concentrations in a dose dependent manner.
  • PublicationMetadata only
    Synthesis and initial evaluation of efficacy of olean-12-en-28-ol, 3 beta-pentacosanoate for the symptomatic treatment of multiple sclerosis
    (2019-07-01) DAĞ, AYDAN; Sen, A.; ŞENOL, HALİL; Kale, E.; TOPÇU, GÜLAÇTI; ŞENOL, HALIL; DAĞ, AYDAN; TOPÇU, GÜLAÇTI
  • PublicationMetadata only
    Synthesis of New Ursane Triterpenoids Including Fatty Acids Esters and Investigation of Their in vitro Cytotoxic Effects on 3T3 Fibroblast and PC3 Prostate Cancer Cell Lines
    (2019-12-19) Dağ, Aydan; Topçu, Gülaçtı; Atasoy, Sezen; Çokuludağ, Kübra; Şenol, Halil; ŞENOL, HALIL; DAĞ, AYDAN; ATASOY, SEZEN; TOPÇU, GÜLAÇTI
  • PublicationMetadata only
    Chemical Characterization of 64 Propolis Samples from Hakkari, Turkey
    (2018-11-01) Bayram, Nesrin Ecem; SORKUN, KADRİYE; Oz, Gul Cevahir; SALİH, BEKİR; Topcu, GÜLAÇTI; TOPÇU, GÜLAÇTI
    Propolis is a resinous substance produced by honey bees from various plants they visit. Sixty-four propolis samples were collected from different localities of four districts (Merkez, Yiiksekova, Semdinli, and Qukurca) in Hakkari territory. Ethanol extracts of the propolis samples were prepared, and their chemical contents were determined by gas chromatography-mass spectroscopy (GC-MS). Flavonoids were generally found in a high concentration in Semdinli samples of Turkey. Twenty-seven coumarins were identified in the 28 propolis samples among studied 64 ones. Except suberosin, the coumarins were never reported before in any propolis sample with Turkish origin. The propolis samples belonging to Yuksekova were found to be richer in coumarins than the others, and the most richest one among the Yfiksekova apiaries, was found to be Akocak sample (Y2) with 41.99% total yield, followed by Akcall sample (Y5) (30.86%). This is a first comprehensive and original report about the chemical profile of propolis samples from Hakkari. The propolis samples from Hakkari exhibited a chemical content rich in flavonoids including coumarins and furocoumarins.
  • PublicationOpen Access
    SAR Evaluation of Disubstituted Tacrine Analogues as Promising Cholinesterase and Carbonic Anhydrase Inhibitors
    (2019-04-01) ÖKTEN, S; EKIZ, M; TUTAR, A; BÜTÜN, BURCU; Gülçin, İlhami; TOPÇU, GÜLAÇTI; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI
    Background: The inhibition of both hydrolysis products of acetylcholine (ACh), Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE), is essential for successful treatment of Alzhemier patients. Objectives: This study was investigated inhibition potentials of recently synthesized disubstituted tacrines derivatives on going our research against AChE, BChE and carbonic anhydrase cyctosolic (hCA I and H) enzymes to explore the Structure activity relationship (SAR). Methods: Inhibitory activities of tested compounds against AChE and BChE were measured by spectrophotometric method, developed by Ellman et al. Furthermore, the disubstituted tacrines were determined as inhibitors of two physiologically relevant CA isoforms, the cytosolic hCA I and H by an esterase assay method. Results: The silyl, thiomethyl and cyano substituted seven membered hydrocycle tacrines (9, 11 and 14) significantly inhibited AChE, compared with starting compound 3 (6,8-dibromo-2,3,4,5-teytrahydro-1H-cyclohepta[1,2-b] quinoline) and reference compounds, galantamine and tacrine, while methoxy substituted seven membered hydrocycle tacrine derivative 10 showed selective inhibition against BChE (IC50 = 563 nM). Interestingly, disubstituted tacrines displayed higher or parallel inhibition to galantamine. Additionally, all these tacrine analogues were recorded to be powerful inhibitor compounds of the cytosolic isoenzyme hCA I with K-i in the range of 43.81-471.67 nM, as well as a moderate selectivity toward hCA II isoenzyme with K-i in the range from 87.14 to 614.68 nM compared with AZA, as standard. Conclusion: The disubstituted seven membered hydrocycle tacrine analogues 9-12 and 14 may have promising anti Alzhemier drug candidate and dibromo six membered hydrocycle 2 and dibromo seven membered hydrocycle 3 derivatives may be novel hCA I and II enzyme inhibitors.
  • PublicationOpen Access
    Phytochemical screening and evaluation of the antimicrobial and antioxidant activities of Ferula caspica M. Bieb. extracts
    (2019-05-01) Kahraman, Çiğdem; TOPÇU, GÜLAÇTI; Bedir, Erdal; Tatlı, İrem; Ekizoğlu, M; Akdemir, Zeliha Ş; TOPÇU, GÜLAÇTI
    Chloroform, ethyl acetate and methanol extracts from the aerial parts of Ferula caspica M. Bieb. were tested for their antioxidant capacities by CUPRAC, ABTS, FRAP, Folin–Ciocalteu and aluminum chloride methods and for antimicrobial activities by the broth microdilution method. Chloroform and ethyl acetate extracts showed the highest antioxidant capacity and antimicrobial activity. Three known sesquiterpene derivatives; 1-(20 ,40 -dihydroxyphenyl)-3,7,11-trimethyl-3-vinyl-6(E),10-dodecadien-1-on e (1), 2,3-dihydro-7-hydroxy-2,3-dimethyl-2-[40 ,80 -dimethyl-30 ,70 -nonadienyl]-furo[3,2,c]coumarin (2), 2,3-dihydro-7-hydroxy-2,3-dimethyl-3-[40 ,80 -dimethyl-30 ,70 -nonadienyl]-furo[3,2,c]coumarin(3); phenylpropanoid; laserine/2-epilaserine (4/5) and steroid mixtures; stigmasterol and b-sitosterol (6/7) were isolated from chloroform extract; three known flavonoids; kaempferol-3-O-b-glucopyranoside (8), kaempferol-3-O-a-rhamnopyranoside (9), quercetin-3-O-b-glucopyranoside (10), and one benzoic acid derivative; 2,4-dihydroxybenzoic acid (11) were isolated from the ethyl acetate extract. The structures were elucidated by spectroscopic methods. 2019 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).