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KARAKUŞ, SEVGİ

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KARAKUŞ

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    Synthesis, anticancer evaluation and in silico ADMET studies on urea/thiourea derivatives from gabapentin
    (TAYLOR & FRANCIS LTD, 2020) KAYMAKÇIOĞLU, BEDİA; Turk, Sevda; Tok, Fatih; Erdogan, Omer; Cevik, Ozge; Tok, Tugba Taskin; Kocyigit-Kaymakcioglu, Bedia; Karakus, Sevgi
    2-(1-((3-Substitutedureido/thioureido)methyl)cyclohexyl)acetic acid derivatives (1-9) were synthesized from gabapentin. All the synthesized compounds were characterized by using IR, H-1-NMR, C-13-NMR spectroscopy, mass spectrometry and elemental analysis. Urea and thiourea derivatives were investigated for their potential in vitro anticancer activities on PC3 and MCF7 cancer cell lines using MTT assay. Cell apoptosis was detected by with Annexin V Assay. Our results showed that compound 8 {2-(1-((3-(2,6-dichlorophenyl)ureido)methyl)cyclohexyl)acetic acid} significantly inhibited the proliferation and growing of PC3 and MCF7 cells. Both cell types showed dysfunction of cellular morphology which induced apoptosis 10 mu M concentration of compound 8 treated cells. Our results indicate that compound 8 might have significance as an anti-tumor agent against human prostate and breast cancer. The theoretical structure and activity estimation via in silico ADMET was also examined.
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    Therapeutic drug monitoring in pediatric patients treated with anti-tuberculosis medications by high performance liquid chromatography
    (2022-01-01) OKUYAN, BETÜL; TOK, FATİH; KARAKUŞ, SEVGİ; KAYMAKÇIOĞLU, BEDİA; SANCAR, MESUT; OKUYAN B., TOK F., KARAKUŞ S., Dalgiç N., ÇAKIR E., Midyat L., Koçyiğit-Kaymakçioğlu B., Berk U. E. , İZZETTİN F. V. , Rollas S., et al.
    © 2022 Marmara University Press.The aim of this study is to perform therapeutic drug monitoring for isoniazid (INH), rifampicin (RIF), and pyrazinamide (PZA) in pediatric tuberculosis patients. The study was carried out in 3 different training-research hospitals in Istanbul, Türkiye between 2011 and 2012. The pediatric patients (aged ≤14 years) who initiated the standard primary anti-tuberculosis therapy were included in this study. The serum samples were collected 3 hours after the first medication doses were given on the 5th day of treatment. Chromatographic experiments were performed on an Agilent 1100 High-Performance Liquid Chromatography (HPLC) system, and the separation was carried out on a Nova-Pak C18 (3.9x150 mm, 5 μm, Merck) analytical column. In this HPLC method, the gradient elusion delivered 3% to 40% (v/v) acetonitrile in phosphate buffer was used, and diode array detector. Twenty-three children (60.9% male) patients were included with a mean age of 111.70 ± 59.94 months. Plasma levels were measured sub-therapeutically for INH in 14, RIF in 10, and PZA in 5 patients, according to the normal range of adult patients. Maximum plasma concentrations after three hours were found between 0.53-14.02 mg/L for INH, 11.17-60.39 mg/L for PZA, 2.15-16.75 mg/L for RIF. In conclusion, this method has been successfully applied to simultaneously determine RIF, INH, and PZA plasma levels in pediatric tuberculosis patients. RIF and INH plasma levels were found to be lower in pediatric patients with tuberculosis compared to target range of adult patients.
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    Synthesis of new hydrazide-hydrazone derived from etophenamate and investigation of their antimicrobial activity
    (2023-10-22) GÜRBÜZ, BURÇAK; RAYAMAN, PERVİN; KARAKUŞ, SEVGİ; Saral Çakmak S., GÜRBÜZ B., RAYAMAN P., KARAKUŞ S.
    Recently since the emerging resistant strains to antimicrobial agents, the development of original antimicrobial agents in pharmaceutical chemistry has gained great importance. Antibiotic resistance is accepted as one of the greatest threatens against health worldwide. Since 1950s to now it is known that hydrazide-hydrazones have antimicrobial, anticancer, antitubercular, anticonvulsant etc., biological spectrum and biological activity (Polovic et al., 2019). Hydrazone derivatives are used in treatment and involved in the structure of many drugs such as nifuroxazide, nitrofurazone, bisanthren, budralazine, and levosimendan. Etophenamate was chosen as the starting compound to synthesis of 16 novel hydrazide-hydrazones. All of these derivatives were investigated in order to determine their antimicrobial activities. The structures of the synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, mass spectroscopy and elemental analysis. In this study, the antimicrobial activity of 16 hydrazide-hydrazone derivatives to 4 standard bacterial strains (Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalis ATCC 29212) and 4 standard yeast strains (Candida albicans ATCC 90028, Candida glabrata ATCC 90030, Candida parapsilosis ATCC 90018, Candida tropicalis KUEN 1021) was examined by the microdilution method in accordance with the Clinical and Laboratory Standards Institute (CLSI) standards, and the Minimal Inhibitory Concentration (MIC) values of these derivatives were determined. It was found that among these derivatives, 2c (725-0.35µg/ml) and 2p (1000-0.5µg/ml) possed antimicrobial activity against all of the 8 standard microorganism strains.