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Synthesis and biological evaluation of echinomycin analogues as potential colon cancer agent

Keita Kojima1, Hiroaki Konishi2, Kyoka Momosaki1

  • 1Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo, 060-0812, Japan.

Scientific Reports
|April 1, 2024
PubMed

Insights

Novel echinomycin analogues show promise for colon cancer treatment. Analogue 3 effectively inhibits cancer growth in vivo with low toxicity, suggesting its potential as a new chemotherapeutic agent.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Molecular Biology

Background:

  • Colorectal cancer is a leading cause of cancer death, necessitating new therapeutic strategies.
  • Echinomycin, a natural cyclic peptide, exhibits potent anticancer activity against various cell lines.

Purpose of the Study:

  • To synthesize and evaluate novel echinomycin analogues for colon cancer therapy.
  • To investigate the mechanism of action and in vivo efficacy of these analogues.

Main Methods:

  • Synthesis of echinomycin analogues.
  • In vitro assessment of inhibition of HIF-1α-mediated transcription.
  • Transcriptome analysis to identify cellular effects.
  • In vivo evaluation using a mouse xenograft model.

Main Results:

  • Analogue 3 and Analogue 1 inhibited HIF-1α-mediated transcription.
  • Transcriptome analysis revealed cell cycle regulation as a key target of Analogue 3.
  • Analogue 3 demonstrated superior in vivo efficacy compared to echinomycin with no significant toxicity.

Conclusions:

  • Analogue 3 is a promising novel agent for colon cancer treatment.
  • Its efficacy at low doses and favorable safety profile warrant further investigation.

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