| In vivo: |
| Planta Med. 2003 Oct;69(10):914-20. | | Antitussive activity of Stemona alkaloids from Stemona tuberosa.[Pubmed: 14648394] |
METHODS AND RESULTS:
Bioactivity-directed fractionation of the crude extract of Stemona tuberosa led to the isolation and characterization of four new stenine-type Stemona alkaloids, namely tuberostemonine J ( 2), tuberostemonine H ( 3), epi-bisdehydrotuberostemonine J ( 4) and Neostenine ( 5), together with the known neotuberostemonine ( 1). These five isolated alkaloids were examined for antitussive activity in guinea pig after cough induction by citric acid aerosol stimulation.
CONCLUSIONS:
In this report, we demonstrated, for the first time, that compounds 1 and 5 showed significant antitussive activities. Further study of the structure-activity relationship on these isolated alkaloids and two synthetic analogues revealed that the saturated tricyclic pyrrolo[3,2,1- jk] benzazepine nucleus is the primary key structure contributing to the antitussive activity and all cis configurations at the three ring junctions are the optimal structure for the antitussive activity of stenine-type Stemona alkaloids. | | Planta Med. 2006 Feb;72(3):211-6. | | Intestinal absorption of Stemona alkaloids in a Caco-2 cell model.[Pubmed: 16534724] |
METHODS AND RESULTS:
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 x 10 (-6) cm/s] than for neotuberostemonine [P(app(AB)) = 9.27 +/- 0.79 x 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.
CONCLUSIONS:
Cyclosporin A dose-dependently inhibited the secretory permeability of these alkaloids and abolished their active efflux transport. |
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