Cytotoxic activity of hydrolyzable tannins against human oral tumor cell lines - A possible mechanism

H. Sakagami, Y. Jiang, K. Kusama, T. Atsumi, T. Ueha, M. Toguchi, I. Iwakura, K. Satoh, H. Ito, T. Hatano, T. Yoshida

Research output: Contribution to journalArticlepeer-review

132 Citations (Scopus)


Hydrolyzable tannins showed higher cytotoxic activity against human oral squamous cell carcinoma and salivary gland tumor cell lines than against normal human gingival fibroblasts, whereas gallic acid, a component unit of tannins, showed much weaker selective cytotoxicity. The cytotoxic activity of dimeric compounds was generally higher than that of monomeric compounds. Macrocyclic ellagitannin oligomers, such as oenothein B, woodfordin C and woodfordin D showed the greatest cytotoxic activity, and their activity (per given number of molecules) was one order higher than those of gallic acid and epigallocatechin gallate, a major component of green tea. These compounds induced apoptotic cell death characterized by DNA fragmentation (as demonstrated by the TUNEL method) and cleavage of cytokeratin 18 by activated caspase(s) (as demonstrated by M30 monoclonal antibody). ESR spectroscopy revealed that these macrocyclic compounds at higher concentrations produced their own radicals and significantly enhanced the radical intensity of sodium ascorbate, possibly by their prooxidant actions. Catalase failed to eliminate their apoptosis-inducing activity, reducing the possibility of the involvement of hydrogen peroxide production in the extracellular fraction. These observations suggested that the antitumor activity of macrocyclic ellagitannin oligomers reported previously might be explained by their apoptosis-inducing activity.

Original languageEnglish
Pages (from-to)39-47
Number of pages9
Issue number1
Publication statusPublished - Mar 2000


  • Apoptosis
  • Caspase
  • DNA fragmentation
  • Macrocyclic ellagitannins
  • Oral tumor cells

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Drug Discovery
  • Complementary and alternative medicine


Dive into the research topics of 'Cytotoxic activity of hydrolyzable tannins against human oral tumor cell lines - A possible mechanism'. Together they form a unique fingerprint.

Cite this