Synthetic hispidin, a PKC inhibitor, is more cytotoxic toward cancer cells than normal cells in vitro
C Gonindard, C Bergonzi, C Denier… - Cell biology and …, 1997 - Springer
C Gonindard, C Bergonzi, C Denier, C Sergheraert, A Klaebe, L Chavant, E Hollande
Cell biology and toxicology, 1997•SpringerThe 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) 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 …
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.
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