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Methodology for Accurate Detection of Mitochondrial DNA Methylation
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Berberine C9-Derivatives Selective Cytotoxicity Depends on Balance Between Mitochondrial Damage and DNA Intercalation

Anastasiia Yu Kolchanova1, Konstantin G Lyamzaev1, Nicolae Valutsa2

  • 1Chemistry Department and AN Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, Moscow, Russian Federation.

Archiv Der Pharmazie
|February 11, 2026
PubMed

Insights

Berberine derivatives show selective cancer cell growth inhibition. The most effective compounds, C9-substituted berberines, work at nanomolar concentrations by intercalating into DNA.

Area of Science:

  • Natural Products Chemistry
  • Medicinal Chemistry
  • Cancer Biology

Background:

  • Berberine, a natural compound, exhibits anticancer properties in vitro.
  • Screening of novel compounds identified berberine derivatives with selective cytotoxicity.
  • C9-substituted berberines demonstrated potent activity in the nanomolar range.

Purpose of the Study:

  • To synthesize and evaluate novel berberine derivatives for anticancer activity.
  • To investigate the structure-activity relationships (SAR) of these derivatives.
  • To elucidate the mechanism of action of potent berberine derivatives.

Main Methods:

  • Fluorescent cells co-cultivation test (FCCT) for cytotoxicity screening.
  • Synthesis of various berberine derivatives.
  • Analysis of DNA intercalation and mitochondrial membrane potential disruption.

Main Results:

  • C9-substituted berberines showed selective cytotoxicity against A549 and MCF7 cancer cells.
  • Several derivatives exhibited potent anticancer activity at nanomolar concentrations.
  • DNA intercalation was identified as a significant mechanism of action.
  • Mitochondrial disruption was observed for charged berberine derivatives.

Conclusions:

  • Berberine derivatives, particularly C9-substituted ones, are promising anticancer agents.
  • DNA intercalation is a key mechanism for their cytotoxic effects.
  • Further research into these compounds could lead to novel cancer therapies.
Keywords:
berberine derivativescytotoxicityintercalationmechanism of actionselectivity

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