Absorption of euphobiasteroid across Caco-2 cell monolayer model / 中草药

ABSTRACT

Objective: To study the absorption and transportation of euphobiasteroid in Caco-2 cell monolayer model. Methods: Caco-2 cell monolayer model was used to study the process of bi-direction transport of euphobiasteroid, and the effects of time, drug concentration, and inhibitors on the process were investigated. The concentration of euphobiasteroid was detected by UPLC-MS/MS, and the apparent permeability coefficient (Papp) and apparent permeability (PDR) were calculated. Results: During the transport process of euphobiasteroid in Caco-2 cells, the Papp values of variety concentration were from 1 × 10-6 to 1 × 10-5. The cumulative transshipment volume was increased with time and concentration, which presented concentration-dependent manner. The PDR values of 10, 30, and 50 μmol/L euphobiasteroid were 1.35, 0.83, and 0.65, respectively. Verapamil hydrochloride could promote the transportation of euphobiasteroid from AP side to BL side. Conclusion: The absorption of euphobiasteroid in intestine is moderate and mainly through passive transport. There may be excretion mechanism of intestinal transport protein in the intestine absorption of euphobiasteroid.