Uptake and metabolism of ginsenoside Rh2 and its aglycon protopanaxadiol by Caco-2 cells

Xie, H. T., Wang, G.J., Chen, M, Jiang, X. L., Li, H, Lv, H, Huang, C. R., Wang, R and Roberts, M (2005) Uptake and metabolism of ginsenoside Rh2 and its aglycon protopanaxadiol by Caco-2 cells. Biological & Pharmaceutical Bulletin, 28 2: 383-386. doi:10.1248/bpb.28.383

Author Xie, H. T.
Wang, G.J.
Chen, M
Jiang, X. L.
Li, H
Lv, H
Huang, C. R.
Wang, R
Roberts, M
Title Uptake and metabolism of ginsenoside Rh2 and its aglycon protopanaxadiol by Caco-2 cells
Journal name Biological & Pharmaceutical Bulletin   Check publisher's open access policy
ISSN 0918-6158
Publication date 2005
Sub-type Article (original research)
DOI 10.1248/bpb.28.383
Volume 28
Issue 2
Start page 383
End page 386
Total pages 4
Editor Y. Nomura
Place of publication Japan
Publisher Pharmaceutical Society of Japan
Collection year 2005
Language eng
Subject C1
320501 Pharmaceutical Sciences and Pharmacy
730118 Organs, diseases and abnormal conditions not elsewhere classified
Abstract The uptake and metabolism profiles of ginsenoside Rh2 and its aglycon protopanaxadiol (ppd) were studied in the human epithelial Caco-2 cell line. High-performance liquid chromatography-mass spectrometry was applied to determine Rh2 and its aglycon ppd concentration in the cells at different pH, temperature, concentration levels and in the presence or absence of inhibitors. Rh2 uptake was time and concentration dependent, and its uptake rates were reduced by metabolic inhibitors and influenced by low temperature, thus indicating that the absorption process was energy-dependent. Drug uptake was maximal when the extracellular pH was 7.0 for Rh2 and 8.0 for ppd. Rh2 kinetic analysis showed that a non-saturable component (K-d 0.17 nmol (.) h(-1) (.) mg(-1) protein) and an active transport system with a K-m of 3.95 mumol (.) l(-1) and a V-max of 4.78 nmol(.)h(-1) (.)mg(-1) protein were responsible for the drug uptake. Kinetic analysis of ppd showed a non-saturable component (K-d 0.78 nmol (.) h(-1) (.) mg(-1) protein). It was suggested that active extrusion of P-glycoprotein and drug degradation in the intestine may influence Rh2 bioavailability.
Keyword Pharmacology & Pharmacy
Caco-2 Cell
Ginsenoside Rh2
High-performance Liquid Chromatography-mass Spectrometry (hplc-ms)
Line Caco-2
Q-Index Code C1

Document type: Journal Article
Sub-type: Article (original research)
Collections: Excellence in Research Australia (ERA) - Collection
2006 Higher Education Research Data Collection
School of Medicine Publications
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Created: Wed, 15 Aug 2007, 06:29:46 EST