Transport properties of paeoniflorin and amygdalin across caco-2 cell monolayer model and their modulation of cytochrome p450 metabolism

Paeoniflorin and amygdalin are two major active saponins constituents in some Chinese herbal formulas used for cardio-cerebrovascular diseases. However, their intestinal absorption property and metabolic characteristics have not been clarified. The aim of this work was to study the absorption property of Paeoniflorin and Amygdalin across Caco-2 cell monolayer and their metabolic characteristics on the activity of cytochrome P450 (CYP450) enzyme. The results showed that the transport amount of Paeoniflorin and Amygdalin was positively correlated with the time and concentrations, and the transport amount from AP side to BL side was higher than that from BL to AP. The absorptions of Paeoniflorin and Amygdalin were reduced by P-glycoprotein, which provided the pharmacokinetic basis for their clinical application. Furthermore, we demonstrated that Paeoniflorin and Amygdalin had obvious inhibiting effects on CYP2C9 and CYP2E1. The transports of Paeoniflorin and Amygdalin across Caco-2 cell monolayer model were deduced as the passive transport, which indicated that the present bioassay system was appropriate and reliable for the evaluation of the transport characteristics and metabolic characteristics of active ingredient groups in Bu-yang-huan-wu decoction. Moreover, this research method may also be suitable for the appropriate bioactivity and metabolic characteristics analysis of other plant extracts.