Synthesis, characterization and antiproliferative activities of novel modified poly (maleic anhydride-co-vinyl acetate)/cytosine ?-Darabinofuranoside hydrochloride conjugate

Autor: Haci Bayram Zengin, Nihat Karakuş, Gulderen Karakus, Ayşe Şahin Yağlioğlu
Rok vydání: 2015
Předmět:
Zdroj: MARMARA PHARMACEUTCAL JOURNAL. 1:73-73
ISSN: 1309-0801
DOI: 10.12991/mpj.2015198613
Popis: Poly (maleic anhydride-co-vinyl acetate) (MAVA) copolymer was synthesized by free-radical- polymerization reaction in methyl ethyl ketone (MEK) at 80 oC using benzoyl-peroxide (BPO) as the radical-initiator. MAVA was then modified with anti-leukemic chemotherapy-agent cytosine β-Darabinofuranoside hydrochloride (CF). Modification was performed at 70 oC in dimethylformamide (DMF) containing triethylamine (Et3N) as the catalyst. Structural characterization of the copolymer and copolymer/drug couple (MAVA/CF) was carried out by Fourier Transform Infrared (FTIR) and Nuclear Magnetic Resonance (1H-NMR). FTIR and 1H-NMR spectra confirmed the modification reaction. UV-Spectrophotometric measurements indicated that MAVA/CF kept its molecular integrity in physiological-body-fluid, PBS, for first four days. Antiproliferative activities of MAVA/CF were also determined by BrdU-cell-proliferation-ELISA assays using C6 and HeLa cell lines (cisplatin and 5-fluorouracil used as positive control). MAVA/CF appeared to have little antiproliferative activity against C6 cell line while samples didn’t have antiproliferative activity against HeLa cell line at low concentrations (< 100 μg/ml). Reaction mechanism was also recommended for modification product MAVA/CF. Keywords: Antiproliferative activity, copolymer modification, cytosine β-D-arabinofuranoside hydrochloride, physiological body fluid PBS, poly(maleic anhydride-co-vinyl acetate).
Databáze: OpenAIRE