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Planta Med 2003; 69(6): 518-522
DOI: 10.1055/s-2003-40653
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

Antiallergic Activity of Ginseng and its Ginsenosides

Min-Kyung Choo1 , Eun-Kyung Park1 , Myung Joo Han2 , Dong-Hyun Kim1
  • 1College of Pharmacy, Kyung Hee University, Seoul, Korea
  • 2Department of Food and Nutrition, Kyung Hee University, Seoul, Korea
Further Information

Publication History

Received: November 19, 2002

Accepted: March 8, 2003

Publication Date:
16 July 2003 (online)

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Abstract

In this study, we measured the antiallergic activities of ginsenosides isolated from the root of Panax ginseng ( Araliaceae), and of their metabolites, as produced by human intestinal bacteria. Compound K, which was identified as a main metabolite, had the most potent inhibitory activity on β-hexosaminidase release from RBL-2H3 cells and on the PCA reaction. The inhibitory activity of compound K was more potent than that of disodium cromoglycate, one of the commercial anti-allergic drugs. This compound demonstrated a membrane stabilizing action on differential scanning calorimetry. However, compound K did not inhibit the activation of hyaluronidase and did not scavenge active oxygen. These results suggest that the antiallergic action of compound K originates from its cell membrane stabilizing activity and that the ginsenosides of ginseng are prodrugs with extensive antiallergic properties.

Abbreviations

compound K:20-O-β-D-glucopyranosyl-20(S)-protopanaxadiol

DNP:dinitrophenol

DSCG:disodium cromoglycate

DPPC:dipalmitoylphosphatidylcholine

DPPH:1,1-diphenyl-2-picrylhydrazyl

HSA:human serum albumin

IC50:50% inhibitory concentration

EC50:50% effective concentration

XOD:xanthine oxidase

ICR:Institute of Cancer Research

PBS:phosphate buffered saline

PCA:passive cutaneous anaphylaxis

RAW264.7:mouse monocyte leukemiaRBL-2H3: rat basophil leukemia

SD:Sprague-Dawley

Key words

Panax ginseng - Araliaceae - ginsenosides - compound K - antiallergic activity - intestinal bacteria

References

  • 1 Tanaka N, Tanaka O, Shibata S. Chemical studies on the oriental plant drugs. XXVIII. Saponins and sapogenins of ginseng; Stereochemistry of sapogenin of ginsenoside Rb1, Rb2 and Rc.  Chemical and Pharmaceutical Bulletin. 1972;  20 1212-6
    PubMedSearch in Google Scholar
  • 2 Shibata S, Fujita M, Itokawa H, Tanaka O, Ishii T. Panaxadiol, a sapongenin of ginseng roots (1).  Chemical and Pharmaceutical Bulletin. 1963;  11 759-64
    PubMedSearch in Google Scholar
  • 3 Wu J Y, Gardner B H, Murphy C I, Seals J R, Kensil C R, Recchia J, Beltz G A, Newman G W, Newman M J. Saponin adjuvant enhancement of antigen-specific immune responses to an experimental HIV-1 vaccine.  Journal of Immunology. 1992;  148 1519-25
    PubMedSearch in Google Scholar
  • 4 Mochizuki M, Yoo C Y, Matsuzawa K, Sato K, Saiki I, Tono-oka S, Samukawa K, Azuma I. Inhibitory effect of tumor metastasis in mice by saponins, ginsenoside Rb2, 20(R)- and 20(S)-ginsenoside Rg3, of red ginseng.  Biological and Pharmaceutical Bulletin. 1995;  18 1197-202
    PubMedSearch in Google Scholar
  • 5 Wakabayashi C, Hasegawa H, Murata J, and Saiki I. In vivo antimetastatic action of ginseng protopanaxadiol saponins is based on their intestinal bacterial metabolites after oral administration.  Oncology Research. 1998;  9 411-7
    PubMedSearch in Google Scholar
  • 6 Akao T, Kida H ., Kanaoka M, Hattori M, Kobashi K. Intestinal bacterial hydrolysis is required for the appearance of compound K in rat plasma after oral administration of ginsenoside Rb1 from Panax ginseng .  Journal of Pharmacy and Pharmacology. 1988;  50 1155-60
    PubMedSearch in Google Scholar
  • 7 Hasegawa H, Sung J H, Benno Y. Role of human intestinal Prevotella oris in hydrolyzing Ginseng saponins.  Planta Medica. 1997;  63 436-40
    Thieme ConnectPubMedSearch in Google Scholar
  • 8 Akao T, Kanaoka M, Kobashi K. Appearance of compound K, a major metabolite of ginsenoside Rb1 by intestinal bacteria, in rat plasma after oral administration - measurement of compound K by enzyme immunoassay.  Biological and Pharmaceutical Bulletin. 1988;  21 245-9
    PubMedSearch in Google Scholar
  • 9 Bae E A, Park S Y, Kim D H. Constitutive β-glucosidases hydrolyzing ginsenoside Rb1 and Rb2 from human intestinal bacteria.  Biological and Pharmaceutical Bulletin. 2000;  23 1481-5
    PubMedSearch in Google Scholar
  • 10 Bae E A, Han M J, Choo M K, Park S Y, Kim D H. Metabolism of 20(S)- and 20(R)-ginsenoside Rg3 by human intestinal bacteria and its relation to in vitro biological activities.  Biological and Pharmaceutical Bulletin. 2002;  25 58-63
    PubMedSearch in Google Scholar
  • 11 Lee S J, Sung J H, Lee S J, Moon C K, Lee B H. Antitumor activity of a novel ginseng saponin metabolite in human pulmonary adenocarcinoma cells resistant to cisplatin.  Cancer Letters. 1999;  144 39-43
    CrossrefPubMedSearch in Google Scholar
  • 12 Bae E A, Choo M K, Park E K, Park S Y, Shin H Y, Kim D H. Metabolism of ginsenoside Rc by human intestinal bacteria and its related antiallergic activity.  Biological and Pharmaceutical Bulletin. 2002;  25 743-7
    PubMedSearch in Google Scholar
  • 13 Choi O H, Kim J H, Kinet J P. Calcium mobilization via sphingosine kinase in signaling by the Fc epsilon.  Nature. 1996;  380 634-6
    CrossrefPubMedSearch in Google Scholar
  • 14 Ryu S Y, Oak M H, Kim K M. Yomogin inhibits the degranulation of mast cells and the production of nitric oxide in activated RAW264.7 cells.  Planta Medica. 2000;  66 171-3
    PubMedSearch in Google Scholar
  • 15 Kakegawa H, Matsumoto H, Satoh T. Inhibitory effects of some natural products on the activation of hyaluronidase.  Chemical and Pharmaceutical. Bulletin. 1992;  40 1439-42
    PubMedSearch in Google Scholar
  • 16 Xiong Q, Kadota S, Tani T, Namba T. Antioxidative effects of phenylethanoids from Cistanche deserticola .  Chemical and Pharmaceutical Bulletin. 1996;  19 1580-5
    PubMedSearch in Google Scholar
  • 17 Tasaka K, Mio M, Okamoto M. Intracellular calcium release induced by histamine releasers and its inhibition by some antiallergic drugs.  Annals of Allergy. 1986;  56 464-9
    PubMedSearch in Google Scholar
  • 18 Katayama S, Shionoya H, Ohtake S. A new method for extraction of extravasated dye in the skin and the influence of fasting stress on passive cutaneous anaphylaxis in guinea pigs and rats.  Microbiology and Immunology. 1978;  22 89-101
    PubMedSearch in Google Scholar
  • 19 Simons F ER. The antiallergic effects of antihistamines (H1-receptor antagonists).  Journal of Allergy and Clinical Immunology. 1992;  90 705-15
    CrossrefPubMedSearch in Google Scholar
  • 20 Cox J SG. Disodium cromglycate (FPL-670) (”Intar”): A specific inhibitor of reaginic antibody-antigen mechanism.  Nature. 1967;  216 1326-9
    PubMedSearch in Google Scholar
  • 21 Ito H, Miyazaki T, Ono M, Sakurai H. Antiallergic activities of rabdosiin and its related compounds: chemical and biochemical evaluations.  Bioorganic and Medical Chemistry. 1998;  6 1051-6
    PubMedSearch in Google Scholar
  • 22 Akagi M, Mio M, Tasaka K. Histamine release inhibition and prevention of the decrease in membrane fluidity induced by certain antiallergic drugs: analysis of the inhibitory mechanism of NCO-650.  Agents Actions. 1983;  13 149-56
    PubMedSearch in Google Scholar
  • 23 Shibata H, Mio M, Tasaka K. Analysis of the mechanism of histamine release induced by substance P.  Biochemical and Biophysical Acta. 1985;  846 1-7
    PubMedSearch in Google Scholar

Prof. Dr. Dong-Hyun Kim

College of Pharmacy

Kyung-Hee University

1 Hoegi

Dongdaemun-ku

Seoul 130-701

Korea

Email: dhkim@khu.ac.kr

Fax: +82-2-957-5030