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Antimicrobial and Anticancer Application of Silver(I) Dipeptide Complexes.

Gabriela Kuzderová1, Michaela Rendošová1, Róbert Gyepes2

  • 1Department of Inorganic Chemistry, P. J. Šafárik University, Moyzesova 11, 041 54 Kosice, Slovakia.

Molecules (Basel, Switzerland)
|November 13, 2021
PubMed
Summary

New silver(I) dipeptide complexes show promising antimicrobial and anticancer activities. These compounds bind to DNA and inhibit topoisomerase I, suggesting potential therapeutic applications.

Keywords:
DNA interactionanticancer activityantimicrobial activitycell cycle arrestcrystal structuredipeptidesilver(I) complexesstabilitytopoisomerase I inhibition

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Area of Science:

  • Coordination Chemistry
  • Medicinal Chemistry
  • Biochemistry

Background:

  • Silver(I) complexes with dipeptides are explored for biological applications.
  • Understanding their interaction with biological targets is crucial for therapeutic development.

Purpose of the Study:

  • To synthesize and characterize novel silver(I) dipeptide complexes.
  • To evaluate their antimicrobial, cytotoxic, and DNA-binding properties.
  • To elucidate their mechanism of action, including topoisomerase I inhibition.

Main Methods:

  • Synthesis and characterization using spectroscopy (mid-IR, NMR, mass spectrometry), elemental analysis, thermogravimetric analysis, and X-ray crystallography.
  • In vitro antimicrobial activity assays against pathogenic microorganisms.
  • Cytotoxicity assays (MTS) against various cancer cell lines and fibroblasts.
  • DNA binding affinity, DNA cleavage assays, cell cycle analysis, and topoisomerase I inhibition studies.

Main Results:

  • Three silver(I) dipeptide complexes (AgGlyGly, AgGlyAla, AgGlyAsp) were successfully prepared and characterized.
  • The complexes exhibited in vitro antimicrobial activity and influenced microbial biofilm formation.
  • Cytotoxicity was observed against cancer cell lines with varying selectivity indices.
  • Complexes bind to DNA via noncovalent interactions and inhibit topoisomerase I activity at 15 μM.

Conclusions:

  • The synthesized silver(I) dipeptide complexes possess significant antimicrobial and anticancer potential.
  • Their mechanism of action involves DNA binding and topoisomerase I inhibition.
  • These findings highlight the therapeutic promise of these novel silver(I) complexes.