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Impact of local anesthetics on epigenetics in cancer

Lucillia Bezu1,2,3, Oliver Kepp1,2, Guido Kroemer1,2,4

  • 1Equipe Labellisée Par La Ligue Contre Le Cancer, Université de Paris, Sorbonne Université, INSERM UMR1138, Centre de Recherche des Cordeliers, Institut Universitaire de France, Paris, France.

Frontiers in Oncology
|September 16, 2022
PubMed

Insights

Local anesthetics show potential as novel anticancer agents by reversing epigenetic alterations like DNA hypermethylation. These non-nucleoside drugs offer a less toxic alternative to current treatments, targeting cancer cells through epigenetic modifications.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Epigenetic alterations, including DNA hypermethylation, silence tumor suppressor genes, promoting cancer development.
  • Current DNA methyltransferase (DNMT) inhibitors (5-azacytidine, decitabine) are nucleoside derivatives with significant side effects and genotoxicity.
  • There is a need for less toxic epigenetic modifiers for cancer therapy.

Purpose of the Study:

  • To explore the anticancer potential of local anesthetics as epigenetic modifiers.
  • To investigate the mechanisms by which local anesthetics exert cytotoxic effects on cancer cells.

Main Methods:

  • Review of preclinical studies on local anesthetics' epigenetic effects.
  • Analysis of DNMT inhibition, micro-RNA expression, and histone acetylation modulation by local anesthetics.

Main Results:

  • Local anesthetics act as non-nucleoside DNMT inhibitors.
  • These agents modulate micro-RNA expression and repress histone acetylation.
  • Local anesthetics demonstrate cytotoxic effects on malignant cells through epigenetic mechanisms.

Conclusions:

  • Local anesthetics possess potent epigenetic activities relevant to cancer therapy.
  • Understanding these mechanisms could establish local anesthetics as viable anticancer drugs.
  • Non-nucleoside epigenetic modifiers like local anesthetics offer a promising, less toxic therapeutic avenue.
Keywords:
cancerdemethylationepigeneticlocal anestheticsmiRNA

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