Uptaking characteristics of puerarin in Caco-2 model system / 中草药

ABSTRACT

Objective To study the uptaking characteristics of puerarin in Caco-2 model system. Methods The transepithelial transporting character of puerarin across Caco-2 cells was investigated by changing the concentration, temperature of drug and using appropriate inhibitors. Results The transport of puerarin across Caco-2 cell monolayers was directional. With the increase of the concentration of pue-rarin, the permeability direction ratio (PDR) was decreased from 2.1 to 1.4. With the increase of temperature, PDR was increased. When the metabolic inhibitors, KCN and 2,4-dinitrophenol, were added, the PDR was decreased from 1.7 to 1.0 and 1.2, respectively. When 100 mg/L Verapamil was added, the permeability coefficient of apical to basolateral was increased from (0.84?0.18)?10-7 cm/s to (1.01?0.17)?10-7 cm/s, and the permeability coefficient of basolateral to apical was decreased from (1.43?0.18)?10-7 cm/s to (1.11?0.24)?10-7 cm/s. Conclusion The evacuation by P-glycoprotein affects the puerarin transepithelial transport across Caco-2 cells.