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 [Papp(AB) = 12.03 ± 1.14 × 10 - 6 cm/s] than for neotuberostemonine [Papp(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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Ge Lin, Ph. D.
Department of Pharmacology
Faculty of Medicine
The Chinese University of Hong Kong
Shatin
N. T.
Hong Kong
SAR
Phone: +852-2609-6824
Fax: +852-2603-5139
Email: linge@cuhk.edu.hk