Park K, Goto M, Takei R, Maruyama A, Kobayashi K, Miyazaki J, Cho C, Akaike T
Faculty of Bioscience and Biotechnology, Tokyo Institute of Technology, Yokohama, Japan.
J Biomater Sci Polym Ed. 2000;11(9):903-13. doi: 10.1163/156856200744093.
Copolymers composed of sulfonylurea (SU) as an antagonist of ATP-sensitive K+ channel and sugar moieties as double ligands were synthesized. Insulin secretion from MIN6 cells (insulinoma cell line) in contact with the copolymers was evaluated. MIN6 cells attached to the poly(N-p-vinylbenzyl-D-maltonamide-co-SU) [P(VMA-co-SU)]-coated dishes were in the more aggregated form as compared to other polymer-coated surfaces. By introducing SU into the sugar bearing homopolymer, an enhanced effect on insulin secretion from MIN6 cells was observed due to the specific interaction between SU ligands and SU receptors on the beta-cell membrane. P(VMA-co-SU) composed of SU and non-reducing glucose moieties demonstrated enhanced insulin secretion from MIN6 cells and faster proliferation of MIN6 cells as compared to poly(N-p-vinylbenzyl-D-lactonamide-co-SU) [P(VLA-co-SU)] probably owing to the glucose transporters presence on the MIN6 cell membrane. Insulin secretion from MIN6 cells pretreated with diazoxide as an agonist of ATP-sensitive K+ channel was suppressed.
合成了由作为ATP敏感性钾通道拮抗剂的磺酰脲(SU)和作为双配体的糖部分组成的共聚物。评估了与共聚物接触的MIN6细胞(胰岛素瘤细胞系)的胰岛素分泌情况。与其他聚合物包被的表面相比,附着在聚(N - 对乙烯基苄基 - D - 麦芽酰胺 - 共 - SU)[P(VMA - 共 - SU)]包被培养皿上的MIN6细胞呈更聚集的形态。通过将SU引入含糖均聚物中,由于SU配体与β细胞膜上的SU受体之间的特异性相互作用,观察到对MIN6细胞胰岛素分泌的增强作用。与聚(N - 对乙烯基苄基 - D - 内酯酰胺 - 共 - SU)[P(VLA - 共 - SU)]相比,由SU和非还原性葡萄糖部分组成的P(VMA - 共 - SU)表现出增强的MIN6细胞胰岛素分泌和更快的MIN6细胞增殖,这可能是由于MIN6细胞膜上存在葡萄糖转运蛋白。用作为ATP敏感性钾通道激动剂的二氮嗪预处理的MIN6细胞的胰岛素分泌受到抑制。