Intestinal Absorption of Stemona Alkaloids in a Caco-2 Cell Model

Abstract

The intestinal absorption of neotuberostemonine and neostenine, two major bioactive alkaloids of the commonly used antitussive traditional Chinese medicine Stemona tuberosa Lour, was investigated using a Caco-2 monolayer model. Both alkaloids exhibited a high absorptive permeability which was higher for neostenine [P_app(AB) = 12.03 ± 1.14 × 10 ^{- 6} cm/s] than for neotuberostemonine [P_app(AB) = 9.27 ± 0.79 × 10 ^{- 6} cm/s], indicating that they are likely to be well absorbed and orally active. Furthermore, both alkaloids were identified to be the substrates of P-glycoprotein and have a transport preference from the basolateral to apical direction with efflux ratios between 2 and 3. Cyclosporin A dose-dependently inhibited the secretory permeability of these alkaloids and abolished their active efflux transport.

Key words

Neotuberostemonine - neostenine - Stemona alkaloids - Stemona tuberosa - Caco-2 cell model

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