Uptake and Metabolism of Ginsenoside Rh2 and Its Aglycon Protopanaxadiol by Caco-2 Cells

Hai-Tang Xie; Guang-Ji Wang; Miao Chen; Xi-ling Jiang; Hao Li; Hua Lv; Chen-Rong Huang; Rui Wang; Michael Roberts

doi:10.1248/bpb.28.383

Notes

Uptake and Metabolism of Ginsenoside Rh2 and Its Aglycon Protopanaxadiol by Caco-2 Cells

Hai-Tang Xie, Guang-Ji Wang, Miao Chen, Xi-ling Jiang, Hao Li, Hua Lv, Chen-Rong Huang, Rui Wang, Michael Roberts

Author information

Hai-Tang Xie
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Guang-Ji Wang
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Miao Chen
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Xi-ling Jiang
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Hao Li
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Hua Lv
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Chen-Rong Huang
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Rui Wang
Key Laboratory of Pharmacokinetics, China Pharmaceutical University
Michael Roberts
School of Medicine, Princess Alexandra Hospital, University of Queensland

Keywords: Caco-2 cell, ginsenoside Rh2, protopanaxadiol, uptake, metabolism, high-performance liquid chromatography-mass spectrometry (HPLC-MS)

JOURNAL FREE ACCESS

2005 Volume 28 Issue 2 Pages 383-386

DOI https://doi.org/10.1248/bpb.28.383

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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 μmol·l⁻¹ and a V_max of 4.78 nmol·h⁻¹·mg⁻¹protein 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.

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