Apoptosis-inducing activity of the actin-depolymerizing agent aplyronine A and its side-chain derivatives

Osamu Ohno, Maho Morita, Kazuhiro Kitamura, Toshiaki Teruya, Kozo Yoneda, Masaki Kita, Hideo Kigoshi, Kiyotake Suenaga

Research output: Contribution to journalArticlepeer-review

25 Citations (Scopus)


Aplyronine A (1) and mycalolide B (2), which are cytotoxic actin-depolymerizing marine macrolides, were revealed to induce apoptosis in human leukemia HL60 cells and human epithelial carcinoma HeLa S3 cells. Based on these results, actin-depolymerizing compounds were expected to exhibit apoptosis-inducing activity in cancer cells. Compounds 3-6, which were synthesized based on the side-chain structure of aplyronine A, were evaluated for their actin-depolymerizing activities in vitro and cytotoxicities against HL60 cells. The growth-inhibitory activities of 3-6 were well correlated with their actin-depolymerizing activities, and derivative 6 was shown to induce the disruption of actin filaments and apoptosis in HL60 cells. These results suggested that actin-depolymerizing agents 1, 2, and 6-induced apoptosis in HL60 cells may have been due to their actin-depolymerizing activity.

Original languageEnglish
Pages (from-to)1467-1471
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 2013 Mar 1


  • Actin
  • Actin-depolymerizing activity
  • Aplyronine A
  • Apoptosis
  • Mycalolide B

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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