Development of Scientific Basics of New Polymer-Drugs Based on Sugar Balls

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The present study is concerned with synthesis of sugar/lipid-hybrid sugar balls and reading of a guest molecule into the host molecule. Galactose-bearing glycopeptide-type sugar ball capsule was designed, which was expected to interact with liver cell specifically. Polymer reaction of poly(amido amine) dendrimer with peracetylated sugar-substituted serine N carboxyanhydride (NCA) was carried out in the presence of 8-anilino-l-naphthalenesulfonate (ANS) in chloroform at -30 ゜C for 15 min. Acyl groups were introduced to the terminal amino groups to form a hydrophobic layer.Then, the product was deacetylated with hydrazine monohydrate in methanol. UV and fluorescence measurements indicated that the existence of ANS inside the sugar ball capsule.Synthesis of "sugar cylinders", novel graft copolymers [poly(L-lysine)-graft glycopeptide-persubstituted poly(amido amine) dendrimer] was also carried out by the polymer reaction of poly(L-lysine)-graft-poly(amido amine) dendrimer with peracetylated N-acetyl-D glucosamine-substituted L-serine N-carboxyanhydride in chloroform at -30 ゜C, Functionality of the terminal amino groups in the polymer reaction was 1.0, which was determined by NMR spectro scopy.Cell recognition ability of the sugar ball/plasmid DNA complexes was examined by erythrocyte agglutination inhibition assays using wheat germ agglutinin (WGA). The minimum inhibitory concentrations of the sugar ball/DNA complexes were well fitted with those of corresponding sugar balls. The nuclease digestion of the complex by restriction endonucleases was investigated at 37 ゜C. DNA dissociated by poly(aspartic acid) appeared resistant to the nucleases.