The in vitro structure-related anti-cancer activity of ginsenosides and their derivatives

Hang Dong, Li Ping Bai, Vincent Kam Wai Wong, Hua Zhou, Jing Rong Wang, Yan Liu, Zhi Hong Jiang*, Liang Liu

*Corresponding author for this work

Research output: Contribution to journalJournal articlepeer-review

82 Citations (Scopus)


Panax ginseng has long been used in Asia as a herbal medicine for the prevention and treatment of various diseases, including cancer. The current study evaluated the cytotoxic potency against a variety of cancer cells by using ginseng ethanol extracts (RSE), protopanaxadiol (PPD)-type, protopanaxatriol (PPT)-type ginsenosides fractions, and their hydrolysates, which were prepared by stepwise hydrolysis of the sugar moieties of the ginsenosides. The results showed that the cytotoxic potency of the hydrolysates of RSE and total PPD-type or PPT-type ginsenoside fractions was much stronger than the original RSE and ginsenosides; especially the hydrolysate of PPD-type ginsenoside fractions. Subsequently, two derivatives of protopanaxadiol (1), compounds 2 and 3, were synthesized via hydrogenation and dehydration reactions of compound 1. Using those two derivatives and the original ginsenosides, a comparative study on various cancer cell lines was conducted; the results demonstrated that the cytotoxic potency was generally in the descending order of compound 3 > 20(S)-dihydroprotopanaxadiol (2) > PPD (1) > 20(S)- Rh2 > 20(R)-Rh2 ≅ 20(R)-Rg3 ≅ 20(S)-Rg3. The results clearly indicate the structurerelated activities in which the compound with less polar chemical structures possesses higher cytotoxic activity towards cancer cells.

Original languageEnglish
Pages (from-to)10619-10630
Number of pages12
Issue number12
Publication statusPublished - Dec 2011

Scopus Subject Areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

User-Defined Keywords

  • Anti-cancer
  • Cytotoxicity
  • Ginsenosides
  • Protopanaxadiol
  • Structure-related activity


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