Kawada J, Okita M, Nukatsuka M, Toyooka K, Naito S, Nabeshima A, Tsujihara K, Yoshimura Y, Nishida M
Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
Mol Cell Endocrinol. 1989 Apr;62(2):153-9. doi: 10.1016/0303-7207(89)90001-4.
4,6-O-Ethylidene glucose (ethylidene glucose), a specific inhibitor at the outer surface of a glucose transporter in the cell membranes, substituted analogue of streptozotocin was newly synthesized. This compound did not induce diabetes in rats and also did not show cytotoxic effect on pancreatic beta cells of neonatal rats in a monolayer culture system. The reasons why such a molecule was designed and why it showed no biological effects are discussed on the basis of a structure-activity relationship. Our results afford positive evidence for the presence of a glucose transport system or a glucose transporter on pancreatic beta cells and its involvement in the action of streptozotocin on beta cells.
4,6-O-亚乙基葡萄糖（亚乙基葡萄糖），一种细胞膜中葡萄糖转运蛋白外表面的特异性抑制剂，是新合成的链脲佐菌素取代类似物。该化合物不会诱导大鼠患糖尿病，在单层培养系统中对新生大鼠的胰腺β细胞也未显示出细胞毒性作用。基于构效关系讨论了设计这样一种分子的原因以及它为何没有生物学效应。我们的结果为胰腺β细胞上存在葡萄糖转运系统或葡萄糖转运蛋白及其参与链脲佐菌素对β细胞的作用提供了确凿证据。
