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

Abstract

ABSTRACT
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).

Keywords

• Antiproliferative activity, copolymer modification, cytosine β-D-arabinofuranoside hydrochloride, physiological body fluid PBS, poly(maleic anhydride-co-vinyl acetate)

ORIGINAL RESEARCH

Abstract

References

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