Oral absorption mechanism of the polysaccharides from Gastrodia elata Blume base on fluorescence labeling

The mechanisms of action of polysaccharides in vivo have been widely elucidated. However, the systematic research of its absorption and transport mechanisms remains unclear. Herein, we extracted a polysaccharide fraction (GEP) from Gastrodia elata by water extraction and alcohol precipitation and aimed to reveal its oral absorption processes through animal models and Caco-2 cells monolayer models. Our research data showed that GEP-Cy5.5 could be absorbed through the small intestine and the main absorption intestinal segment was the ileum (the absorption rate constant [Ka]: (3.64 ± 0.70) × 10−4 cm/s; the effective apparent permeability [Papp value]: (4.88 ± 1.02) × 10−5 cm/s). The ligated intestinal loops also revealed that GEP-Cy5.5 could pass through the villi of the small intestine and the mucosal barrier into the submucosa. Furthermore, GEP-Cy5.5 was readily absorbed into the blood through the gastrointestinal tract, then distributed in the liver and the kidney. The Papp value of in vitro transport study was (1.29 ± 0.08) × 10−6 cm/s, which was a time-dependent process. Notably, GEP-Cy5.5 was transported through the endocytosis process mediated by clathrin and macropinocytosis. The underlying absorptive mechanisms of GEP in vivo and in vitro were clarified, which provided the guidance for clinical medicine administration and could deepen the biological understanding of oral polysaccharides.