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A natural compound, aristoyagonine, is identified as a potent bromodomain inhibitor by mid-throughput screening

Young Hun Kim1, Minsung Kim2, Miyoun Yoo1

  • 1Bio & Drug Discovery Division, Korea Research Institute of Chemical Technology, Daejeon, 34114, Republic of Korea.

Biochemical and Biophysical Research Communications
|June 22, 2018
PubMed

Insights

A novel natural compound, aristoyagonine, acts as a Bromodomain-containing protein 4 (Brd4) inhibitor. It effectively reduced tumor growth in mice and showed cytotoxicity in gastric cancer cells, including resistant types.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Bromodomain-containing protein 4 (Brd4) is a key regulator of gene expression implicated in tumorigenesis.
  • Developing targeted therapies, such as Brd4 inhibitors, is crucial for cancer treatment.
  • Identifying novel scaffolds for Brd4 inhibitors can overcome existing resistance mechanisms.

Purpose of the Study:

  • To discover novel scaffolds for Bromodomain-containing protein 4 (Brd4) inhibitors.
  • To evaluate the therapeutic potential of a newly identified natural compound, aristoyagonine, as a Brd4 inhibitor.

Main Methods:

  • Mid-throughput screening using alpha-screen and ELISA enzyme assays to identify novel inhibitors.
  • In vitro biochemical assays to confirm inhibitory activity.
  • In vivo studies using a Ty82-xenograft mouse model to assess tumor growth inhibition.
  • Cytotoxicity assays in gastric cancer cell lines, including those resistant to known inhibitors.

Main Results:

  • A novel natural compound, aristoyagonine, was identified as a Brd4 bromodomain inhibitor with a unique scaffold.
  • Aristoyagonine demonstrated significant in vitro inhibitory activity and reduced tumor growth in a xenograft mouse model.
  • Aristoyagonine exhibited cytotoxicity against both I-BET-762-sensitive and I-BET-762-resistant gastric cancer cells.

Conclusions:

  • Aristoyagonine represents the first described natural compound with Brd4 bromodomain inhibitory activity.
  • This natural compound holds promise as a potential therapeutic agent for gastric cancer, including cases resistant to existing treatments.
  • The unique scaffold of aristoyagonine opens new avenues for the development of next-generation Brd4 inhibitors.
Keywords:
AristoyagonineBromodomain inhibitorCancerMid-throughput screeningNatural compound

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