Cancer Letters
Volume 208, Issue 1 , Pages 59-64, 10 May 2004

G2-M arrest and antimitotic activity mediated by casticin, a flavonoid isolated from Viticis Fructus (Vitex rotundifolia Linne fil.)

  • Junko Kobayakawa

      Affiliations

    • Hyogo Institute for Oriental Medicine, Higashidaimotsu-cho, Hyogo 660-0828, Japan
    • Department of Natural Medicinal Chemistry, Kobe Pharmaceutical University, Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan
    • Corresponding Author InformationCorresponding author. Address: Hyogo Institute for Oriental Medicine, Higashidaimotsu-cho, Hyogo 660-0828, Japan. Tel.: +81-6-6482-5250; fax: +81-6-6482-7430
    • ,
  • Fumiko Sato-Nishimori

      Affiliations

    • Hyogo Institute for Oriental Medicine, Higashidaimotsu-cho, Hyogo 660-0828, Japan
    • ,
  • Masataka Moriyasu

      Affiliations

    • Department of Natural Medicinal Chemistry, Kobe Pharmaceutical University, Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan
    • ,
  • Yoshizumi Matsukawa

      Affiliations

    • Hyogo Institute for Oriental Medicine, Higashidaimotsu-cho, Hyogo 660-0828, Japan

Received 20 November 2003; accepted 9 January 2004.

Abstract 

Flavonoids are distributed in many plants. We studied the antitumor effects of flavonoids isolated from Viticis Fructus, casticin, artemetin, quercetagetin and 5,3′-dihydroxy-6,7,4′ -trimethoxyflavanone. Casticin inhibited the growth of KB cells markedly (IC50=0.23 μM), compared with the other flavonoids tested (IC50=15.3–18.6 μM). In contrast, casticin did not inhibit the proliferation of A431 cells similar to normal cell lines, 3T3 Swiss Albino and TIG-103. Flow cytometric analyses revealed that the exposure of KB cells to casticin led to significant arrest at G2-M. In immunostaining of KB cells, casticin disrupted mitotic spindles.

These results suggest that G2-M arrest by casticin may be relevant to its antimitotic activity, although the mechanism of selective growth inhibition has been unknown. Further examinations are required to confirm that casticin is an antitumor drug for specific cancers with low toxicity.

Keywords: Flavonoid, Casticin, KB cells, G2-M arrest, Normal cells, Antimitosis

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PII: S0304-3835(04)00044-8

doi:10.1016/j.canlet.2004.01.012

Cancer Letters
Volume 208, Issue 1 , Pages 59-64, 10 May 2004

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