ABSTRACT
Objective: To evaluate the transport property of water extract from Magnoliae Officinalis Cortex (WEMOC) across Caco-2 monolayer model by bioactivity method and observe the influence on the activity of P-glycoprotein (P-gp) in cell membrane. Methods: The validated Caco-2 cell monolayer model was used to observe the bidirection transportation of WEMOC; The amount of WEMOC in the receiver compartment, apparent permeability coefficient (P'app), and efflux ratio (ER) value could be determined according to the standard curve of total anti-oxidant capacity. The accumulation and efflux of rhodamine123 (Rh123), which is the substrate of P-gp, were determined to evaluate the influence of WEMOC on P-gp. Results: P'app(AP→BL) of WEMOC was around 1 × 10-5 cm/s, and positively related to concentration; ER was far less than 2; It had no impact on the accumulation and efflux of Rh123. Conclusion: The active ingredient groups of WEMOC with anti-oxidant activity can be well absorbed by passive diffusion down a concentration gradient. Neither is it the substrate of P-gp, nor does it have influence on P-gp activity. Our research establishes a novel method to evaluate the transport characteristics of WEMOC, which provides the pharmacokinetic basis for the clinical application of Magnoliae Officinalis Cortex.