Analysis of Carrier-Mediated Transport Systems in Drug Absorption from Oral Mucosa

口腔粘膜药物吸收中载体介导的转运系统分析

• 批准号: 10672041
• 负责人: KIMURA Toshikiro
• 金额: $ 2.05万
• 依托单位: OKAYAMA UNIVERSITY
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1998
• 资助国家: 日本
• 起止时间: 1998 至 1999
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-10672041/
• 关键词: human oral mucosal cells; D-glucose; dipeptide; cultured stratified cell layer; active transport; facilitated diffusion; transporter

The in vitro uptake study was performed using the isolated cells of human oral mucosa, buccal and the dorsum of tongue, to investigate the mechanisms of glucose and oligopeptide uptake. The uptake of D-glucose was much larger in cells of the dorsum of tongue than in buccal cells and was inhibited more extensively by 2-deoxy-D-glucose, a substrate of facilitative glucose transporters, than by α-methyl-D-glucoside, a specific substrate of SGLT1, suggesting the larger contribution of facilitative transporter than NaィイD1+ィエD1/glucose cotransporter. Furthermore, from the results of inhibition studies by the several sugar analogues including maltose and D-mannose, GLUT1 and/or GLUT3 were suggested to take part in the glucose uptake by oral mucosa. Therefore, we have attempted to confirm the expression of glucose transporters on the oral mucosa by employing Western blotting. As a result, it was suggested that SGLT1, GLUT1, GLUT2 and GLUT3 are expressed in the epithelial cells of human oral mucosa. The result of the uptake study of glycylsarcosine, a model dipeptide, by isolated oral cells showed the presence of carrier-mediated transport systems for oligopeptides in human oral mucosal cells. The transport of D-glucose and glycylsarcosine across stratified cell layer of cultured human oral mucosal cells was also examined, and the results showed that the transporters function not only for the uptake of these substrates by the mucosal cells but also for the transport across the stratified mucosal cell layers.

体外摄取研究是对人口服粘膜，颊和舌葡萄糖和寡肽摄取的背面进行的细胞。 2-脱氧-D-葡萄糖UCOSIDE，一种特定的SGLT1底物，表明促进转运蛋白的贡献大于NAI I D1+葡萄糖共转运蛋白。建议通过口服粘膜来参与葡萄糖的更新，我们试图通过使用蛋白质印迹，在人口服粘液的上皮细胞中表达葡萄糖转运蛋白的表达。糖基糖苷的摄取研究的结果是，模型细胞显示了载体介导的转运系统在人OO粘膜细胞中的寡肽中存在。转运蛋白的功能不是粘膜细胞对底物的摄取，而是转运分层的粘膜细胞层。

项目成果

Yujiro Oyama: "Carrier-Mediated Transport Systems for Glucose in Mucosal cells of the Human Oral Cavity"Journal of Pharmaceutical Science. 88・8. 830-834 (1999)

Yujiro Oyama：“人体口腔粘膜细胞中葡萄糖的载体介导的运输系统”《药物科学杂志》88・8（1999）。

Yujiro Oyama: "Carrier-Mediated Transport Systems for Glucose in Mucosal cells of the Human Oral Cavity"Journal of Pharmaceutical Sciences. 88・8. 830-834 (1999)

Yujiro Oyama：“人类口腔粘膜细胞中的载体介导的葡萄糖转运系统”《药物科学杂志》88・8（1999）。

Yujiro Oyama, Hitoshi Yamano, Akiko Ohkuma, Ken-ichi Ogawara, Kazutaka Higaki, and Toshikiro Kimura :: "Carrier-mediated Transport Systems for Glucose in Mucosal Cells of Human Oral Cavity"Journal of Pharmaceutical Sciences. 88・8. 830-834 (1999)

Yujiro Oyama、Hitoshi Yamano、Akiko Ohkuma、Ken-ichi Okawara、Kazutaka Higaki 和 Toshikiro Kimura ::“人体口腔粘膜细胞中葡萄糖的载体介导的运输系统”药物科学杂志 830-834。 (1999)