Visual evidence and quantification of interaction of polymeric sulfonylurea with pancreatic islet.
Visual evidence and quantification of interaction of polymeric sulfonylurea with pancreatic islet.
复制标题
聚合磺酰脲与胰岛相互作用的视觉证据和定量。
DOI：
10.1021/bm025713j
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发表时间：
2003
期刊：
影响因子：
--
通讯作者：
Bae,YouHan
中科院分区：
文献类型：
--
作者：
Kim,Sungwon;Bae,YouHan
使用从格列本脲设计的聚合磺酰脲 (PSU)，我们检查了磺酰脲与胰岛而不是基因改造的 β 细胞系的相互作用，以阐明磺酰脲结合的 ATP 敏感 K+ (KATP) 通道的生物学作用。 10 nM（SU 当量）处理后，PSU 增强胰岛的胰岛素分泌，尤其是在低葡萄糖浓度下，但其活性被 100 μM 二氮嗪抑制。共聚焦显微镜可视化 PSU 与胰岛的相互作用，并揭示细胞内 Ca2+ 的调节发生在 PSU 也结合的胰岛的同一区域。在共焦显微图像的定量方法中，证实了PSU与格列本脲在其结合位点上的竞争以及葡萄糖对PSU结合的抑制。在这项研究中，得出的结论是 PSU 是与格列本脲相当的药物，并提供了一种研究完整胰岛的新标准方法。
Using a polymeric sulfonylurea (PSU) designed from glibenclamide, we examined the interactions of sulfonylurea with pancreatic islets rather than genetically remodeled β-cell lines to clarify the biological roles of ATP-sensitive K+(KATP) channels to which sulfonylurea binds. PSU enhanced insulin secretion from the islets with 10 nM (SU equivalent) treatment, especially at low glucose concentration, but its activity was inhibited by 100 μM diazoxide. Confocal microscopy visualized PSU interactions with the islet and revealed that the modulation of intracellular Ca2+occurred in the same region of an islet where PSU was also bound. In quantification method of the confocal microscopic images, competition of PSU with glibenclamide on its binding sites and glucose inhibition against PSU binding were confirmed. In this study, it was concluded that the PSU was a comparable drug with glibenclamide and offered a new standard method to study intact islets.