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Kettner, C.A. and Shenvi, A.B. (1984) Inhibition of the serine proteases leukocyte elastase, pancreatic elastase, cathepsin G, and chymotrypsin by peptide boronic acids. J Biol Chem, 259(24), 15106. Miyazaki, H., Kikuchi, A., Kitano, S., Koyama, Y., Okano, T., Sakurai, Y., Kataoka, K. (1993)

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• TITLE: Bioengineering functional copolymers. XII. Interaction of boron-containing and PEO branched derivatives of poly(MA-alt-MVE) with HeLa cells

  AUTHORS: Mustafa Türk, Zakir M. O. Rzayev, Gülcihan Kurucu

  KEYWORDS: Synthesis; Organoboron Copolymers; Structure-Property Relations; Cytotoxicity; Antitumor Activity; Apoptotic Effect

  JOURNAL NAME: Health, Vol.2 No.1, January 15, 2010

  ABSTRACT: Novel boron-containing bioengineering copoly- mer and its α-hydoxy-ω-methoxy-poly(ethy- lene oxide (PEO) macrobranched derivatives were synthesized by (1) partially amidolysis of poly(maleic anhydride-alt-methyl vinyl ether) w?th ethanolamine ester of diphenylboronic acid and (2) esterification of synthesized B-con- taining copolymers with PEO. They had a com- bination of hydrophilic/hydrophobic linkages, free carboxylic groups, positive charges and an ionized organoboron linkage as antitumor sites, along with an ability to interact with HeLa cells. The structure, composition and properties (cy- totoxicity and antitumor activity) of synthe- sized copolymers were investigated. In vitro cytotoxicity results, obtained by the fluore scence microscopy measurements indicate that unlike the virgin copolymer, boron-containing and PEO macrobranched derivatives exhibit higher antitumor activity. It was found that organoboron copolymer exhibits the most apo- ptotic and necrotic effects against HeLa cells whereas a minor effect relative to cancer cells was observed on L929 Fibroblast cells.