Editor-in-Chief Hatice Kübra Elçioğlu Vice Editors Levent Kabasakal Esra Tatar Online ISSN 2630-6344 Publisher Marmara University Frequency Bimonthly (Six issues / year) Abbreviation J.Res.Pharm. Former Name Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal 2015 , Vol 19 , Issue 1
Synthesis, characterization and antiproliferative activities of novel modified poly (maleic anhydride-co-vinyl acetate)/cytosine β-Darabinofuranoside hydrochloride conjugate
1Cumhuriyet University Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Sivas, Turkey
2Çankırı Karatekin University Faculty of Science, Department of Chemistry, Çankırı, Turkey
3Cumhuriyet University Faculty of Science, Department of Chemistry, Sivas, Turkey
DOI : 10.12991/mpj.2015198613 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).
Marmara University