Source:http://linkedlifedata.com/resource/pubmed/id/20608841
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
9
|
| pubmed:dateCreated |
2010-10-8
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| pubmed:abstractText |
This study investigated the absorption mechanism of ginsenoside Rh2 to clarify the reasons for its poor absorption. Transepithelial transport across Caco-2 cell monolayers, cellular uptake, and in situ rat intestinal perfusion were examined. Cellular uptake of Rh2 was linear from 1 to 50 ?M at 4°C, whereas it was saturated when the concentration exceeded 10 ?M at 37°C. At 37°C, the uptake at 10 ?M was linear in 60 min. Intracellular exposure in 240 min was 2173.70 and 979.38 ng·min/?g for S and R isomers, respectively. Transepithelial permeability of Rh2 was about 10?? to 10?? cm/s. Efflux ratios were above 1.5. Sodium dodecyl sulfate, sodium citrate, and sodium deoxycholate had no effect on Rh2 permeability. After intestinal perfusion for 3 h, 9.1% of 20(R)-Rh2 and 15.7% of 20(S)-Rh2 were absorbed. Cyclosporine, quercetin, and probenecid could improve the cellular uptake, absorptive permeability, and intestinal absorption. Carrier-mediated transport was the major absorption mechanism. Rh2 was a substrate of ABC transporters. The ABC-transporter-mediated efflux and the poor permeability were the major reasons for Rh2 poor absorption. The stereoselective absorption was significant. R isomer exhibited lower absorption profiles in all the experiments, possibly due to more potent efflux.
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| pubmed:language |
eng
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| pubmed:journal | |
| pubmed:citationSubset |
IM
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| pubmed:chemical | |
| pubmed:status |
MEDLINE
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| pubmed:month |
Sep
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| pubmed:issn |
1366-5928
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| pubmed:author | |
| pubmed:issnType |
Electronic
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| pubmed:volume |
40
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| pubmed:owner |
NLM
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| pubmed:authorsComplete |
Y
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| pubmed:pagination |
602-12
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| pubmed:meshHeading |
pubmed-meshheading:20608841-ATP-Binding Cassette Transporters,
pubmed-meshheading:20608841-Animals,
pubmed-meshheading:20608841-Biological Transport,
pubmed-meshheading:20608841-Caco-2 Cells,
pubmed-meshheading:20608841-Cell Survival,
pubmed-meshheading:20608841-Drug Stability,
pubmed-meshheading:20608841-Epithelial Cells,
pubmed-meshheading:20608841-Ginsenosides,
pubmed-meshheading:20608841-Humans,
pubmed-meshheading:20608841-Hydrogen-Ion Concentration,
pubmed-meshheading:20608841-Intestinal Absorption,
pubmed-meshheading:20608841-Perfusion,
pubmed-meshheading:20608841-Permeability,
pubmed-meshheading:20608841-Rats,
pubmed-meshheading:20608841-Rats, Sprague-Dawley,
pubmed-meshheading:20608841-Stereoisomerism,
pubmed-meshheading:20608841-Temperature,
pubmed-meshheading:20608841-Time Factors
|
| pubmed:year |
2010
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| pubmed:articleTitle |
Intestinal absorption mechanisms of ginsenoside Rh2: stereoselectivity and involvement of ABC transporters.
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| pubmed:affiliation |
Key Laboratory of Drug Metabolism & Pharmacokinetics, China Pharmaceutical University, Nanjing, China.
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| pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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