Antiproliferative activities through accelerating autophagic flux by basidalin and its analogs in human cancer cells

Tomoe Matagawa, Yukiko Sasazawa, Koki Agui, Motoki Fujimaki, Sayaka Kawano, Akihiro Ogura, Ken ichi Takao, Masayuki Igarashi, Siro Simizu

Research output: Contribution to journalArticlepeer-review


Basidalin, isolated from the basidiomycete Leucoagaricus naucina, has previously demonstrated antibacterial and antitumor properties against murine cancer cells in vivo, but its effects on human cancer cells remain unknown. In this study, we found that basidalin possesses antiproliferative activity against human cancer cell lines. To elucidate the antiproliferative mechanism of basidalin, we focused on autophagy. Treatment with basidalin led to an increase in LC3-II expression level, and accelerated autophagic flux through an mTOR-independent pathway. Moreover, according to the structure–activity relationship analysis—including newly synthesized basidalin analogs—the formyl group, not the amino group, contributes to the antiproliferative activities of basidalin against human cancer cells. Additionally, the antiproliferative activity of basidalin analogs was strongly correlated with autophagy-inducing activity, indicating that basidalin exhibits antiproliferative activity through autophagy induction. These data suggest that basidalin, characterized by its ability to upregulate autophagic flux, emerges as a novel anticancer drug.

Original languageEnglish
Article number129713
JournalBioorganic and Medicinal Chemistry Letters
Publication statusPublished - 2024 May 15


  • Antibiotic
  • Antiproliferative activity
  • Autophagy inducer
  • Basidalin
  • Structure–activity relationship
  • mTOR signal

ASJC Scopus subject areas

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


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