Bioengineering Functional Copolymers. XVII. Interaction of Organoboron Amide-Ester Branched Derivatives of Poly(Acrylic Acid) with Cancer Cells

Mustafa Türk, Gülten Kahraman, Sevda A. Khalilova, Zakir M. O. Rzayev, Serpil Oguztüzün

.
Institute of Science & Engineering, Division of Nanoscience and Nanomedicine, Hacettepe University, Ankara, Turkey..

DOI: 10.4236/jct.2011.22034                

Abstract

Novel bioengineering functional organoboron polymers were synthesized by 1) amidolysis of poly(acrcylic acid) (PAA) with 2-aminoethyldiphenyl borinate (2-AEPB), 2) esterification of organoboron PAA polymer (PAA-B) with a-hydroxy-methoxypoly(ethylene oxide) (PEO) as a compatibilizer and 3) conjugation of organoboron PEO branches (PAA-B-PEO) with folic acid (FA) as a targeting agent. Structure and composition of the synthesized polymers were characterized by FTIR-ATR and 1H (13C) NMR spectroscopy, chemical and physical analysis methods. Anti-tumor activity of organoboron functional polymer and its complex with FA (PAA-B-PEO-F) against cancer and normal cells were evaluated by using different biochemical methods such as cytotoxicity, statistical, apoptotic and necrotic cell indexes, double staining and caspase-3 immune staining, light and fluorescence inverted microscope analyses. It was found that citotoxicity and apoptotic/necrotic effects of polymers significantly depend on the structure and composition of studied polymers, and increase the following raw: PAA << PAA-B < PAA-B-PEO < PAA-B-PEO-F. Among them, PAA-B-PEO-F complex at 400 mg mL–1 concentration as a therapeutic drug exhibits minimal toxicity toward the nor-mal cells, but influential for HeLa cancer cells.

Keywords

Synthesis, Amidolysis, Organoboron Polymers, Conjugation, Citotoxicity, Apoptotic and Necrotic Effects

Conflicts of Interest

The authors declare no conflicts of interest.

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