TZT-1027 elucidates antitumor activity through direct cytotoxicity and selective blockade of blood supply

Naoko Hashiguchi, Tetsuro Kubota, Jun Ichi Koh, Yoshinori Yamada, Yoshiro Saikawa, Yoshihide Otani, Masahiko Watanabe, Koichiro Kumai, Masaki Kitajima, Jun Ichi Watanabe, Motohiro Kobayashi

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Abstract

Background: TZT-1027 is a newly developed antitumor agent derived from dolastatin 10. Materials and Methods: The in vitro activity of TZT-1027 on MCF-7 and R-27 cells was evaluated by MTT assay. TZT-10271 mg/kg/week was administered i.v. for 4 weeks into nude mice bearing MCF-7 and R-27. Subsequently, primary cultured cells from xenografts were also used for CD-DST. Two mg of TZT-1027 or 40 mg docetaxel per kg were injected i.v. into nude mice bearing R-27. 0.2% Evans blue was injected to assess the blood flow. Results: TZT-1027 suppressed the in vitro growth of MCF-7 cells, while R-27 cells were resistant to TZT-1027, although its in vivo antitumor activity was remarkable. TZT-1027 blockaded R-27 tumor blood flow immediately after injection; blood flow was not affected by docetaxel. Conclusion: TZT-1027 exerts its antitumor activity through direct cytotoxicity against MCF-7 cells and through selective blockade of tumor blood flow against R-27 cells.

Original languageEnglish
Pages (from-to)2201-2208
Number of pages8
JournalAnticancer research
Volume24
Issue number4
Publication statusPublished - 2004 Jul 1

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Keywords

  • Breast cancer
  • Nude mouse
  • TZT-1027
  • Vascular flow

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

Cite this

Hashiguchi, N., Kubota, T., Koh, J. I., Yamada, Y., Saikawa, Y., Otani, Y., Watanabe, M., Kumai, K., Kitajima, M., Watanabe, J. I., & Kobayashi, M. (2004). TZT-1027 elucidates antitumor activity through direct cytotoxicity and selective blockade of blood supply. Anticancer research, 24(4), 2201-2208.