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An In Vitro Enzymatic Assay to Measure Transcription Inhibition by GalliumIII and H3 5,10,15-trispentafluorophenylcorroles
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Gallic Acid: A Natural Phenolic Compound Exerting Antitumoral Activities in Colorectal Cancer via Interaction with

Victoria Sanchez-Martin1,2,3, María Del Carmen Plaza-Calonge1, Ana Soriano-Lerma1,4

  • 1GENYO, Centre for Genomics and Oncological Research, Pfizer/University of Granada/Andalusian Regional Government, 18016 Granada, Spain.

Cancers
|June 10, 2022
PubMed

Insights

Gallic acid, a natural compound, shows anti-cancer effects by targeting DNA G-quadruplexes (G4s). This interaction inhibits key genes, leading to cancer cell death and offering a potential new therapy for colorectal cancer (CRC).

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Cancer Research

Background:

  • Natural phenolic compounds are investigated for cancer prevention and treatment.
  • The precise antitumoral mechanisms of these compounds, including their interaction with DNA structures, require further elucidation.

Purpose of the Study:

  • To screen phenolic compounds for antitumoral potential in colorectal cancer (CRC).
  • To investigate the mechanism of action of gallic acid (GA) as a DNA G-quadruplex (G4) ligand.
  • To evaluate GA's therapeutic potential in preclinical models of CRC.

Main Methods:

  • Screening of phenolic compounds in a cellular CRC model.
  • In vitro and in vivo evaluation of gallic acid's biological activity.
  • Assessment of GA's interaction with DNA G-quadruplexes and its effects on gene transcription, cell cycle, and DNA damage.
  • Xenograft model studies in CRC.

Main Results:

  • Gallic acid (GA) was identified as a potent and selective antitumoral agent.
  • GA acts as a DNA G-quadruplex (G4) ligand, inhibiting ribosomal and CMYC gene transcription.
  • GA induced cell cycle arrest, nucleolar stress, and DNA damage, similar to known G4 ligands.
  • GA demonstrated antitumoral and G4-stabilizing properties in vivo.

Conclusions:

  • Gallic acid (GA) exhibits significant antitumoral effects in colorectal cancer (CRC) models.
  • GA's mechanism involves targeting DNA G-quadruplexes (G4s), modulating gene expression, and inducing cellular stress.
  • GA represents a promising natural therapeutic candidate for CRC, warranting further clinical investigation.
Keywords:
G-quadruplexcancercolorectal cancergallic acidphenol

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