Person:
BİNGÖL ÖZAKPINAR, ÖZLEM

Organizational Units

Organizational Unit

Eczacılık Fakültesi

Last Name

BİNGÖL ÖZAKPINAR

First Name

ÖZLEM

Full item page

Search Results

Now showing 1 - 10 of 29

Open Access
Synthesis and Characterization of Celecoxib Derivatives as Possible Anti-Inflammatory, Analgesic, Antioxidant, Anticancer and Anti-HCV Agents
(MDPI, 2013-03-21) ŞENER, AZİZE; Kucukguzel, S. Guniz; Coskun, Inci; Aydin, Sevil; Aktay, Goknur; Gursoy, Sule; Cevik, Ozge; Ozakpinar, Ozlem Bingol; Ozsavci, Derya; Sener, Azize; Kaushik-Basu, Neerja; Basu, Amartya; Talele, Tanaji T.
A series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamides 2a-e were synthesized by the addition of ethyl alpha-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)- 1H-pyrazol-1-yl] benzene sulfonamides 1a-e, which were synthesized by the reaction of alkyl/aryl isothiocyanates with celecoxib. The structures of the isolated products were determined by spectral methods and their anti-inflammatory, analgesic, antioxidant, anticancer and anti-HCV NS5B RNA-dependent RNA polymerase (RdRp) activities evaluated. The compounds were also tested for gastric toxicity and selected compound 1a was screened for its anticancer activity against 60 human tumor cell lines. These investigations revealed that compound 1a exhibited anti-inflammatory and analgesic activities and further did not cause tissue damage in liver, kidney, colon and brain compared to untreated controls or celecoxib. Compounds 1c and 1d displayed modest inhibition of HCV NS5B RdRp activity. In conclusion, N-(ethylcarbamothioyl)-4-[5-(4-methylphenyl)- 3-(trifluoromethyl)-1H-pyrazol-1-yl] benzenesulfonamide (1a) may have the potential to be developed into a therapeutic agent.
Open Access
Apocynin reduces cytotoxic effects of monosodium glutamate in the brain: A spectroscopic, oxidative load, and machine learning study
(2022-10-15) BİNGÖL ÖZAKPINAR, ÖZLEM; Depciuch J., Jakubczyk P., Paja W., Sarzyński J., Pancerz K., AÇIKEL ELMAS M., Keskinöz E., BİNGÖL ÖZAKPINAR Ö., ARBAK S., Özgün G., et al.
© 2022 Elsevier B.V.Herein, we examined the modulatory effects of Apocynum (APO) on Monosodium Glutamate (MSG)-induced oxidative damage on the brain tissue of rats after long-term consumption of blood serum components by biochemical assays, Fourier transform infrared spectroscopy (FTIR), and machine learning methods. Sprague-Dawley male rats were randomly divided into the Control, Control + APO, MSG, and MSG + APO groups (n = 8 per group). All administrations were made by oral gavage saline, MSG, or APO and they were repeated for 28 days of the experiments. Brain tissue and blood serum samples were collected and analyzed for measurement levels of malondialdehyde (MDA), glutathione (GSH), myeloperoxidase (MPO), superoxide dismutase (SOD) activity, and Spectroscopic analysis. After 29 days, the results were evaluated using machine learning (ML). The levels of MDA and MPO showed changes in the MSG and MSG + APO groups, respectively. Changes in the proteins and lipids were observed in the FTIR spectra of the MSG groups. Additionally, APO in these animals improved the FTIR spectra to be similar to those in the Control group. The accuracy of the FTIR results calculated by ML was 100%. The findings of this study demonstrate that Apocynin treatment protects against MSG-induced oxidative damage by inhibiting reactive oxygen species and upregulating antioxidant capacity, indicating its potential in alleviating the toxic effects of MSG.
Open Access
Investigation of 3D-printed chitosan-xanthan gum patches
(2022-07-01) ALTAN, ERAY; GÜNDÜZ, OĞUZHAN; BİNGÖL ÖZAKPINAR, ÖZLEM; ALTAN E., Turker N., Hindy O. A., Dirican Z., Ozakpinar Ö., Demir A. U., Kalaskar D., Thakur S., GÜNDÜZ O.
In this study, using a new polymer combination of Chitosan(CH)/Xanthan Gum(XG) has been exhibited for wound dressing implementation by the 3D-Printing method, which was fabricated due to its biocompatible, biodegradable, improved mechanical strength, low degradation rate, and hydrophilic nature to develop cell-mimicking, cell adhesion, proliferation, and differentiation. Different concentrations of XG were added to the CH solution as 0.25, 0.50, 0.75, 1, and 2 wt% respectively in the formic acid/distilled water (1.5:8.5) solution and rheologically characterized to evaluate their printability. The results demonstrated that high mechanical strength, hydrophilic properties, and slow degradation rate were observed with the presence and increment of XG concentration within the 3D-Printed patches. Moreover, in vitro cell culture research was conducted by seeding NIH 3T3 fibroblast cells on the patches, proving the cell proliferation rate, viability, and adhesion. Finally, 1% XG and 4% CH containing 3D-Printed patches were great potential for wound dressing applications.
Open Access
Growth Arrest-Specific 6 (Gas6) and TAM Receptors in Mouse Platelets
(GALENOS YAYINCILIK, 2015-03-05) BİNGÖL ÖZAKPINAR, ÖZLEM; Uras, Fikriye; Kucuk, Burhanettin; Ozakpinar, Ozlem Bingol; Demir, Ahmet Muzaffer
Objective: Growth arrest-specific 6 (Gas6) is a newly discovered vitamin K-dependent protein, which is a ligand for TAM receptors [Tyro3 (Sky), Axl, and Mer] from the tyrosine kinase family. Gas6 knockout mice were resistant to venous and arterial thrombosis. There are contradictory reports on the presence of Gas6 and its receptors in mouse platelets. The objective of this study was to investigate whether Gas6 and its receptors were present in mouse platelets or not. Materials and Methods: Specific pathogen-free BALB/c male and female mice of 8-10 weeks old and 25-30 g in weight were anesthetized under light ether anesthesia and blood samples were taken from their hearts. RNAs were isolated from isolated platelets, and then mRNAs encoding Gas6 and TAM receptors were detected by reverse transcription-polymerase chain reaction (RT-PCR). Protein concentrations of Gas6 and TAM receptors in platelets were measured by ELISA, but not those of Mer, because of the absence of any commercial ELISA kit for mouse specimens. Results: RT-PCR results indicated the presence of mRNAs encoding Gas6 and Mer in mouse platelets. However, although RTPCR reactions were performed at various temperatures and cycles, we could not detect the presence of mRNAs encoding Axl and Tyro3 (Sky). Receptor protein levels of Axl and Tyro3 were below the detection limits of the ELISA method. Conclusion: We found the presence of mRNAs encoding Gas6 and the receptor Mer in mouse platelets, but not Axl and Tyro3. Gas6, Axl, and Tyro3 protein levels were below the detection limits of the ELISA. The presence of mRNA is not obvious evidence of protein expression in platelets that have no nucleus or DNA. Further studies are required to clarify the presence of Gas6/TAM receptors in platelets using real-time PCR and more sensitive immunological methods, and future studies on mechanisms will indicate whether the Gas6/TAM pathway is a strategy for treatment of disorders.
Open Access
Novel 1,2,4-triazoles derived from Ibuprofen: synthesis and in vitro evaluation of their mPGES-1 inhibitory and antiproliferative activity
(2022-11-01) BİNGÖL ÖZAKPINAR, ÖZLEM; KULABAŞ, NECLA; TATAR, ESRA; KÜÇÜKGÜZEL, İLKAY; Bulbul B., Ding K., Zhan C., Ciftci G., YELEKÇİ K., Gurboga M., BİNGÖL ÖZAKPINAR Ö., Aydemir E., Baybag D., ŞAHİN F., et al.
Some novel triazole-bearing ketone and oxime derivatives were synthesized from Ibuprofen. In vitro cytotoxic activities of all synthesized molecules against five cancer lines (human breast cancer MCF-7, human lung cancer A549, human prostate cancer PC-3, human cervix cancer HeLa, and human chronic myelogenous leukemia K562 cell lines) were evaluated by MTT assay. In addition, mouse embryonic fibroblast cells (NIH/3T3) were also evaluated to determine the selectivity. Compounds 18, 36, and 45 were found to be the most cytotoxic, and their IC50 values were in the range of 17.46-68.76 mu M, against the tested cancer cells. According to the results, compounds 7 and 13 demonstrated good anti-inflammatory activity against the microsomal enzyme prostaglandin E2 synthase-1 (mPGES-1) enzyme at IC50 values of 13.6 and 4.95 mu M. The low cytotoxicity and non-mutagenity of these compounds were found interesting. Also, these compounds significantly prevented tube formation in angiogenesis studies. In conclusion, the anti-inflammatory and angiogenesis inhibitory activities of these compounds without toxicity suggested that they may be promising agents in anti-inflammatory treatment and they may be supportive agents for the cancer treatment.
Open Access
Synthesis and anticancer activity of novel hydrazone linkage-based aryl sulfonate derivatives as apoptosis inducers
(SPRINGER BIRKHAUSER, 2022-02) BİNGÖL ÖZAKPINAR, ÖZLEM; Senkardes, Sevil; Han, M. Ihsan; Gurboga, Merve; Ozakpinar, Ozlem Bingol; Kucukguzel, S. Guniz
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] .
Open Access
Applying quality by design approach for the determination of potent paclitaxel loaded poly(lactic acid) based implants for localized tumor drug delivery
(2022-04-01) BİNGÖL ÖZAKPINAR, ÖZLEM; Ozcan Bulbul E., Ustundag Okur N., Misirli D., Cevher E., Tsanaktsis V., BİNGÖL ÖZAKPINAR Ö., Siafaka P. I.
In the present study, poly(lactic acid) (PLA) and poly(ethylene succinate) (PESu) or poly(ethylene glycol) (PEG) under the framework of quality by design, were blended to produce effective sustained-release matrices for Paclitaxel delivery. A complete physicochemical characterization including weight variation, thickness, water uptake, moisture absorption, moisture loss, and hydrolytic degradation under physiological conditions, was performed. Quality by design approach was applied to study the critical parameters. In vitro cancer toxicity was studied in human cancer cell lines including lung and breast adenocarcinoma. The developed Paclitaxel-loaded films can act as a promising alternative topical matrix as an implant for breast and lung cancer treatment.
Open Access
The Effect of Algan Hemostatic Agent (AHA) on Wound Healing
(MARMARA UNIV, INST HEALTH SCIENCES, 2020-09-04) ŞEN, ALİ; Aksoy, Halil; Sener, Azize; Akakin, Dilek; Sen, Ali; Ozakpinar, Ozlem Bingol; Ozcan, Sinemcan; Simsek, Ahmet Kaan; Sekerler, Turgut; Guzel, Sevket Ergun; Midi, Ahmet
Objective: The Algan Hemostatic Agent (AHA) is a novel herbal originated blood stopper. The aim of this study is to investigate the effect of AHA on wound healing on excisional wound model in rats. Methods: In this study, 54 adult Wistar albino rats were used. Rats were divided into 3 groups (saline, Madecassol (R) and AHA). Each group was then divided into 3 subgroups as the 3rd, 7th and 14th days. Two wounds were created in the dorsal thoracic region of the rats. One of the lesions was used for histopathological examinations and the other for hydroxyproline measurement. In order to evaluate the wound healing, wound area were measured during the whole treatment period and animals were sacrificed at the end of the 3rd, 7th and 14th days and tissue samples were taken for the determination of hydroxyproline levels. Results: AHA treatment did not cause significant difference in hydroxyproline level on days 3, 7, 14. The contraction percentage of wound area was higher in the AHA group on day 7 than that of the control group. However, the difference was not statistically significant (p>0.05). On days 3 and 14, no significant difference was detected in the contraction percentage of wound area between the control and the AHA groups. AHA and Madecassol (R) results of epidermis regeneration on the 14th day, neutrophil infiltration on the 7th day and edema on the 3rd, 7th and 14th days were different in terms of histopathological parameters compared to the control group. Conclusion: Despite good histological findings, AHA did not significantly accelerate wound healing, but did not adversely affect wound healing as well.
Open Access
In vitro antiproliferative, antioxidant, anti-inflammatory activities and phenolic profile of Centaurea saligna ( K.Koch) Wagenitz
(MARMARA UNIV, 2022) ŞEN, ALİ; Yildirim, Aybeniz; Sen, Ali; Goger, Fatih; Ozakpinar, Ozlem Bingol; Bitis, Leyla
Open Access
Determinants of the tumor suppressor INPP4B protein and lipid phosphatase activities
(ACADEMIC PRESS INC ELSEVIER SCIENCE, 2013-10) BİNGÖL ÖZAKPINAR, ÖZLEM; Lopez, Sandra M.; Hodgson, Myles C.; Packianathan, Charles; Bingol-Ozakpinar, Ozlem; Uras, Fikriye; Rosen, Barry P.; Agoulnik, Irina U.
The tumor suppressor INPP4B is an important regulator of phosphatidyl-inositol signaling in the cell. Reduced INPP4B expression is associated with poor outcomes for breast, prostate, and ovarian cancer patients. INPP4B contains a CX5R catalytic motif characteristic of dual-specificity phosphatases, such as PTEN. Lipid phosphatase activity of INPP4B has previously been described. In this report we show that INPP4B can dephosphorylate para-nitrophenyl phosphate (pNPP) and 6,8-difluoro-4-methylumbelliferyl (DiFMUP), synthetic phosphotyrosine analogs, suggesting that INPP4B has protein tyrosine phosphatase (PTP) activity. Using mutagenesis, we examined the functional role of specific amino acids within the INPP4B C(842)KSAKDR catalytic site. The K843M mutant displayed increased pNPP hydrolysis, the K846M mutant lost lipid phosphatase activity with no effect on PTP activity, and the D847E substitution ablated PTP activity and significantly reduced lipid phosphatase activity. Further, we show that INPP4B but not PTEN is able to reduce tyrosine phosphorylation of Akt1 and both the lipid and PTP activity of INPP4B likely contribute to the reduction of Akt1 phosphorylation. Taken together our data identified key residues in the INPP4B catalytic domain associated with lipid and protein phosphatase activities and found a robust downstream target regulated by INPP4B but not PTEN. (C) 2013 Elsevier Inc. All rights reserved.