Structure-activity relationship of 9-methylstreptimidone, a compound that induces apoptosis selectively in adult T-cell leukemia cells

Masatoshi Takeiri, Eisuke Ota, Shigeru Nishiyama, Hiromasa Kiyota, Kazuo Umezawa

Research output: Contribution to journalArticle

5 Citations (Scopus)

Abstract

We previously reported that 9-methylstreptimidone, a piperidine compound isolated from a culture filtrate of Streptomyces, induces apoptosis selectively in adult T-cell leukemia cells. It was screened for a compound that inhibits LPS-induced NF-κB and NO production in mouse macrophages. However, 9-methystreptimidone is poorly obtained from the producing microorganism and difficult to synthesize. Therefore, in the present research, we studied the structure-activity relationship to look for new selective inhibitors. We found that the structure of the unsaturated hydrophobic portion of 9-methylstreptimidone was essential for the inhibition of LPS-induced NO production. Among the 9-methylstreptimidone-related compounds tested, (±)-4,α-diepi-streptovitacin A inhibited NO production in macrophage-like cells as potently as 9-methylstreptimidone and without cellular toxicity. Moreover, this compound selectively induced apoptosis in adult T-cell leukemia MT-1 cells.

Original languageEnglish
Pages (from-to)7-14
Number of pages8
JournalOncology Research
Volume20
Issue number1
DOIs
Publication statusPublished - 2012

Keywords

  • 9-Methylstreptimidone
  • Adult T-cell leukemia
  • Apoptosis
  • Macrophage
  • Streptovitacin

ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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