Enhancement of intestinal absorption of macromolecules by spermine in rats

Summary. The aim of this study was to investigate the enhancing effect of polyamines on intestinal absorption of fluorescein isothiocyanate-labeled dextran (MW 4400, FD-4) in the in situ loop study and in vivo oral absorption study. Absorption of FD-4 from the jejunum was significantly enhanced by 5 mM spermine without serious membrane damage in the jejunum. An in vivo oral absorption study was also performed, and plasma FD-4 levels increased significantly after co-administration of 30 mM spermine. In the in vitro transport studies with Caco-2 cells, prolonged incubation with spermine resulted in a gradual decrease in transepithelial electrical resistance. This finding suggests that the absorption-enhancing mechanism of spermine partly includes opening the tight junctions of the epithelium via the paracellular route. These results indicate that excess oral ingestion of polyamines may have widespread health effects via the modulation of the intestinal epithelial barrier function.