Kato Toyonori, Hayashi Yayoi, Inoue Katsuhisa, Yuasa Hiroaki
Graduate School of Pharmaceutical Sciences, Nagoya City University, Tanabe-dori, Nagoya, Japan.
Biol Pharm Bull. 2005 Mar;28(3):553-5. doi: 10.1248/bpb.28.553.
The absorption of glycerol was examined using the closed loop of the rat small intestine in situ to clarify the transport mechanism. The absorption of glycerol, evaluated by its disappearance from the intestinal lumen, was saturable and reduced under the Na(+)-free conditions, suggesting the involvement of an Na(+)-dependent carrier-mediated transport system. Furthermore, glycerol absorption was selectively inhibited by several alcohols, among which 1,3-propanediol caused the greatest inhibition, and also by glycerol-3-phosphate and voglibose, which are alcohol-related compounds analogous to glycerol. Several other compounds that did not inhibit glycerol absorption included D-glucose and L-ascorbate, which are known to be transported by specific carriers. Therefore, the carriers for these two compounds do not seem to be involved in glycerol absorption. It is likely that the carrier-mediated transport system involved in glycerol absorption is specific to glycerol and, possibly, some analogous compounds with hydroxyl groups. Thus, the present study has provided in situ evidence for the presence of an Na(+)-dependent carrier-mediated transport system for glycerol in the rat small intestine. It would be interesting to examine the possibility that the carrier-mediated glycerol transport system could be involved in drug absorption and also that it could be used for oral drug delivery.
为阐明甘油的转运机制,利用大鼠小肠原位闭环对甘油的吸收进行了研究。通过肠腔内甘油的消失来评估其吸收情况,结果显示甘油的吸收具有饱和性,且在无钠条件下吸收减少,这表明存在一种依赖钠离子的载体介导转运系统。此外,几种醇类可选择性抑制甘油的吸收,其中1,3 - 丙二醇的抑制作用最强,甘油 - 3 - 磷酸和伏格列波糖(与甘油类似的醇类相关化合物)也有抑制作用。其他几种不抑制甘油吸收的化合物包括已知通过特定载体转运的D - 葡萄糖和L - 抗坏血酸。因此,这两种化合物的载体似乎不参与甘油的吸收。参与甘油吸收的载体介导转运系统可能对甘油以及一些可能带有羟基的类似化合物具有特异性。因此,本研究为大鼠小肠中存在依赖钠离子的甘油载体介导转运系统提供了原位证据。研究载体介导的甘油转运系统是否可能参与药物吸收以及是否可用于口服药物递送将是很有趣的。