Effect of Tannic Acid on Transport of Diaco-Aconitine in Caco-2 Cell Model / 中国药学杂志

ABSTRACT

OBJECTIVE: To study the effects of three aconitine transporters in Caco-2 cells and tannin (tannic acid) in Terminalia on the transport of three di-ester aconitine (aconitine, meoaconitine and hypaconitine) in Aconitum chinensis. METHODS: The components were detected by UPLC/Q exactive MS in terms of the cumulative transshipment volume of three aconitine and the apparent permeability coefficient Papp as indicators to investigate the two-way transport behaviors of three aconitine in the Caco-2 cell model, as well as the proportion of tannic acid, and the changes of the transport behaviors of three aconitine. RESULTS: There was a positive correlation between the cumulative transshipment volume of aconitine and the incubation time. There was no statistical difference in Papp values of the three aconitine, and the efflux effect was significantly stronger than the absorption, with an external ratio close to 1.5.When the compatibility ratio of three aconitine with tannic acid was 1∶1 and 1∶0.5, the absorption of aconitine was significantly inhibited (P was 0.05), but the transport behavior with effluent was not significantly affected. CONCLUSION: Aconitine, meoaconitine, and hypaconitine in P. aeruginosa are mainly passive transporters, and may involve in efferent proteins, which are a kind of drug with good absorption.When mixed with tannic acid, the absorption and transshipment of three kinds of alkali were significantly reduced, which proves that Terminalia chebula could detoxify aconitum by inhibiting its absorption.