Cell Biology and Toxicology

, Volume 13, Issue 3, pp 141–153

Synthetic hispidin, a PKC inhibitor, is more cytotoxic toward cancer cells than normal cells in vitro

  • C. Gonindard
  • C. Bergonzi
  • C. Denier
  • C. Sergheraert
  • A. Klaebe
  • L. Chavant
  • E. Hollande
Article

Abstract

The trypanocidal activity of naturally occurring 6-(3,4-dihydroxystyryl)-4-hydroxy-2-pyrone (hispidin) prompted us to examine its cytotoxic activity toward normal and cancerous cells in culture. Hispidin synthesized in our laboratory to a high degree of purity (checked by 1H and 13C NMR spectroscopy) was shown to be cytotoxic (between 10-3 mol/L and 10-7 mol/L) toward normal human MRC-5 fibroblasts, human cancerous keratinocytes (SCL-1 cell line), and human cancerous pancreatic duct cells (Capan-1 cell line). Interestingly, addition of hispidin in three successive doses (between 10-5 mol/L and 10-7 mol/L) led to a 100-fold increase in activity with an enhanced activity on cancer cells compared to normal cells (50%). Synthetic hispidin was found to inhibit isoform β of protein kinase C (IC50 of 2 × 10-6 mol/L), but not E. coli and placental type XV alkaline phosphatases. The enhanced activity of hispidin toward the cancerous cell lines is discussed.

anti-neoplastic drug cancer hispidin keratinocyte protein kinase C 

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Copyright information

© Kluwer Academic Publishers 1997

Authors and Affiliations

  • C. Gonindard
    • 1
  • C. Bergonzi
    • 2
  • C. Denier
    • 2
  • C. Sergheraert
    • 3
  • A. Klaebe
    • 2
  • L. Chavant
    • 4
  • E. Hollande
    • 1
  1. 1.Laboratoire de Biologie Cellulaire, Équipe de Cytophysiologie des Cellules Eucaryotes HumainesUniversité Paul SabatierToulouseFrance
  2. 2.Laboratoire IMRCP, Groupe de Chimie Organique BiologiqueUniversité Paul SabatierToulouseFrance
  3. 3.Institut Pasteur de LilleLilleFrance
  4. 4.Mycologie (4R1), EA 822Université Paul SabatierToulouseFrance

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