Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5137918 | Journal of Pharmaceutical and Biomedical Analysis | 2017 | 8 Pages |
â¢The intestinal permeability of 42 compounds in GQD was investigated using Caco-2 model.â¢A fully validated LC/MS/MS quantitative analytical method was developed.â¢GQD remarkably changed the transport of many compounds.
Caco-2 cell monolayer model was used to evaluate the intestinal permeability of 42 bioactive compounds in the famous traditional Chinese medicine (TCM) formula Gegen-Qinlian Decoction (GQD). These compounds include alkaloids, flavonoids and glycosides, triterpenoid saponins, and coumarins. Their transportations across the cell monolayers in the forms of herb extract and formula extract were monitored by liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) analysis. Most alkaloids from Huang-Lian; flavonoid C-glycosides from Ge-Gen and Huang-Qin; O-glycosides from Ge-Gen, Huang-Qin and Gan-Cao; O-glucuronides from Huang-Qin; and coumarins from Gan-Cao exhibited favorable permeability. Their PAB values were > 1.05 Ã 10â5 cm/s, and efflux ratios (ER, PBA/PAB) were â¤Â 1.0. In contrast, triterpenoid saponins showed poor permeability (PAB â¤Â 1.50 Ã 10â6 cm/s, ER â¤Â 1.5), indicating a paracellular diffusion mechanism. Furthermore, GQD could remarkably improve the intestinal transport of alkaloids in Huang-Lian, flavonoid C-glycosides in Ge-Gen, as well as coumarins and flavonoid O-glycosides in Gan-Cao. These results indicate herb-herb interactions in GQD.
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