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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts
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Preclinical Assessment of the Bioactivity of the Anticancer Coumarin OT48 by Spheroids, Colony Formation Assays, and Zebrafish Xenografts

Published on: June 26, 2018

Antitumor-promoting activity of coumarins from citrus plants

Chihiro Ito1, Masataka Itoigawa, Motoharu Ju-ichi

  • 1Faculty of Pharmacy, Meijo University, Tempaku, Nagoya, Japan.

Planta Medica
|January 29, 2005
PubMed

Insights

Citrus coumarins show potential as antitumor agents. Several 8-substituted coumarins significantly inhibited Epstein-Barr virus early antigen activation in vitro, with osthenol also demonstrating efficacy in vivo against skin tumor promotion.

Area of Science:

  • Natural Product Chemistry
  • Pharmacology
  • Oncology

Background:

  • The search for novel antitumor-promoting agents is crucial for cancer prevention and treatment.
  • Citrus plants (Rutaceae family) are a rich source of diverse phytochemicals, including coumarins, with known biological activities.
  • Epstein-Barr virus early antigen (EBV-EA) activation is a model system for studying tumor promotion.

Purpose of the Study:

  • To screen coumarins from Citrus species for their potential antitumor-promoting properties.
  • To evaluate the in vitro inhibitory effects of these coumarins on EBV-EA activation.
  • To assess the in vivo efficacy of promising compounds in a skin carcinogenesis model.

Main Methods:

  • In vitro screening of 31 coumarins from 11 Citrus species against TPA-induced EBV-EA activation in Raji cells.
  • Determination of IC50 values for inhibitory coumarins.
  • In vivo two-stage carcinogenesis test in mice to evaluate skin tumor promotion inhibition.

Main Results:

  • Five 8-substituted coumarins, including 8-formyl-7-hydroxycoumarin, osthenol, demethylauraptenol, osthenon, and dihydroosthenon, significantly inhibited EBV-EA activation.
  • Osthenol (7) demonstrated potent inhibition with IC50 values ranging from 129-207 mol ratio/32 pmol TPA.
  • Osthenol (7) showed a significant inhibitory effect on mouse skin tumor promotion in vivo.

Conclusions:

  • Certain 8-substituted coumarins isolated from Citrus species possess significant antitumor-promoting potential.
  • Osthenol is a promising candidate for further investigation as an anticancer agent due to its dual in vitro and in vivo activity.
  • This study highlights the therapeutic value of Citrus-derived coumarins in cancer chemoprevention.

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