Archives of Pharmacal Research

, Volume 27, Issue 1, pp 61–67 | Cite as

Transformation of ginseng saponins to ginsenoside rh2 by acids and human intestinal bacteria and biological activities of their transformants

  • Eun-Ah Bae
  • Myung Joo Han
  • Eun-Jin Kim
  • Dong-Hyun KimEmail author
Research Articles Articles


When ginseng water extract was incubated at 60°C in acidic conditions, its protopanaxadiol ginsenosides were transformed to ginsenoside Rg3 and ▵20-ginsenoside Rg3. However, protopanaxadiol glycoside ginsenosides Rb1, Rb2 and Rc isolated from ginseng were mostly not transformed to ginsenoside Rg3 by the incubation in neutral condition. The transformation of these ginsenosides to ginsenoside Rg3 and ▵20-ginsenoside Rg3 was increased by increasing incubation temperature and time in acidic condition: the optimal incubation time and temperature for this transformation was 5 h and 60°C resepectively. The transformed ginsenoside Rg3 and ▵20-ginsenoside Rg3 were metabolized to ginsenoside Rh2 and ▵20-ginsenoside Rh2, respectively, by human fecal microflora. Among the bacteria isolated from human fecal microflora,Bacteroides sp.,Bifidobacterium sp. andFusobacterium sp. potently transformed ginsenoside Rg3 to ginsenoside Rh2. Acid-treated ginseng (AG) extract, fermented AG extract, ginsenoside Rh2 and protopanaxadiol showed potent cytotoxicity against tumor cell lines. AG extract, fermented AG extract and protopanaxadiol potently inhibited the growth ofHelicobacter pylori.

Key words

Ginseng Ginsenoside Rg3 Intestinal bacteria Ginsenoside Rh2 Helicobacter pylori Cytotoxicity 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. Akao, T., Kanaoka, M., and Kobashi, K., Appearance of compound K, a major metabolite of ginsenoside Rb1 by intestinal bacteria, in rat plasma after oral administrationmeasurement of compound K by enzyme immunoassay.Biol. Pharm. Bull., 21, 245–249 (1998).PubMedGoogle Scholar
  2. Akao, T., Kida, H., Kanaoka, M., Hattori, M., and 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.J. Pharm. Pharmacol., 50, 1155–1160 (1998).PubMedGoogle Scholar
  3. Bae, E.-A., Park, S.-Y., and Kim, D.-H., Constitutive β-glucosidases hydrolyzing ginsenoside Rb1 and Rb2 from human intestinal bacteria.Biol. Pharm. Bull., 23, 1481–1485 (2000).PubMedGoogle Scholar
  4. Bae, E. A., Han, M. J., Choo, M. K., Park, S. Y., and Kim, D. H., Metabolism of 20(S)- and 20(R)-ginsenoside Rg3 by human intestinal bacteria and its relation toin vitro biological activities.Biol. Pharm. Bull., 25, 58–63 (2002).PubMedCrossRefGoogle Scholar
  5. Carmichael, J., DeGreff, W. G., Gazdar, A. F., Minna, J. D., and Mitchell, J. B., Evaluation of a tetrazolium-based semiautomated colorimetric assay: Assessment of chemosensitivity testing.Cancer Res., 47, 936–940 (1987).PubMedGoogle Scholar
  6. Han, B. H., Park, M. H., Han, Y. N., Woo, L. K., Sankawa, U., Yahara, S., and Tanaka, O., Degradation of ginseng saponins under mild acidic conditions.Planta Med., 44, 146–149 (1982).PubMedCrossRefGoogle Scholar
  7. Hasegawa, H., Sung, J.-H., and Benno, Y., Role of human intestinalPrevotella oris in hydrolyzing Ginseng saponins.Planta Med., 63, 436–440 (1997).PubMedCrossRefGoogle Scholar
  8. Kanaoka, M., Kato, H., Shimada, F., and Yano, S., Studies on the enzyme immunoassay of bioactive constituents contained in oriental medicinal drugs. VI. Enzyme immunoassay of ginsenoside Rb1 formPanax ginseng.Chem. Pharm. Bull., 40, 314–317 (1992).PubMedGoogle Scholar
  9. Kanaoka, M., Akao, T., and Kobashi, K., Metabolism of ginseng saponins, ginsenosides, by human intestinal bacteria.J. Tradit. Med., 11, 241–245 (1994).Google Scholar
  10. Karikura M., Miyaze T., Tanizawa H., Taniyzma T., and Takino Y., Studies on absorption, distribution, excretion and metabolism of ginseng saponins. VII. Comparison of the decomposition modes of ginsenoside Rb1 and Rb2 in the digestive tract of rats.Chem. Pharm. Bull., 39, 2357–2361 (1991).PubMedGoogle Scholar
  11. Kitagawa, I., Yoshikawa, M., Yoshihara, M., Hayashi, T., and Taniyama, T., Chemical studies on crude drug precession. I. On the constituents of ginseng radix rubura (I).Yakugaku Zasshi, 103, 612–622 (1983).PubMedGoogle Scholar
  12. Kown, S. W., Han, S. B., Park, I. H., Kim, J. M., Park, M. K., and Park, J. H., Liquid chromatographic determination of less polar ginsenosides in processed ginseng.J. Chromatogr. A, 921, 335–339 (2001)CrossRefGoogle Scholar
  13. Lee, S. J., Sung, J. H., Lee, S. J., Moon, C. K., and Lee, B. H., Antitumor activity of a novel ginseng saponin metabolite in human pulmonary adenocarcinoma cells resistant to cisplatin.Cancer Lett., 144, 39–43 (1999).PubMedCrossRefGoogle Scholar
  14. Mochizuki, M., Yoo, C. Y., Matsuzawa, K., Sato, K., Saiki, I., Tono-oka, S., Samukawa, K., and Azuma, I., Inhibitory effect of tumor metastasis in mice by saponins, ginsenoside Rb2, 20(R)- and 20(S)-ginsenoside Rg3, of Red ginseng.Biol. Pharm. Bull., 18, 1197–1202 (1995).PubMedGoogle Scholar
  15. Sato, K., Mochizuki, M., Saiki, I., Yoo, Y. C., Samukawa K., and Azuma, I., Inhibition of tumor angiogenesis and metastasis by a saponin of Panax ginseng-ginsenoside Rb2.Biol. Pharm. Bull., 17, 635–639 (1994).PubMedGoogle Scholar
  16. Shibata, S., Fujita, M., Itokawa, H., Tanaka, O., and Ishii, T., Panaxadiol, a sapogenin of ginseng roots (1).Chem. Pharm. Bull., 11, 759–764 (1963).PubMedGoogle Scholar
  17. Tanaka, N., Tanaka, O., and Shibata, S., Chemical studies on the oriental plant drugs. XXVIII. Saponins and sapogenins of ginseng; Stereochemistry of sapogenin of ginsenoside Rb1, Rb2 and Rc.Chem. Pharm. Bull., 20, 1212–1216 (1972).Google Scholar
  18. 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.Oncol. Res., 9, 411–417 (1998).Google Scholar
  19. Wu, J. Y., Gardner, B. H., Murphy, C. I., Seals, J. R., Kensil, C. R., Recchia, J., Beltz, G. A., Newman, G. W., and Newman, M. J., Saponin adjuvant enhancement of antigen-specific immune responses to an experimental HIV-1 vaccine.J. Immunol., 148, 1519–1525 (1992).PubMedGoogle Scholar

Copyright information

© The Pharmaceutical Society of Korea 2004

Authors and Affiliations

  • Eun-Ah Bae
    • 1
  • Myung Joo Han
    • 1
  • Eun-Jin Kim
    • 2
  • Dong-Hyun Kim
    • 2
    Email author
  1. 1.Department of Food and NutritionKyung Hee UniversityKorea
  2. 2.College of Pharmacy, Kyung Hee UniversityDongdaemun-Ku, SeoulKorea

Personalised recommendations