Antiproliferative and antibacterial properties of biocompatible copper(II) complexes bearing chelating N,N-heterocycle ligands and potential mechanisms of action

Biometals. 2021 Oct;34(5):1155-1172. doi: 10.1007/s10534-021-00334-9. Epub 2021 Aug 5.

Abstract

In an attempt to propose new applications for the biomedical field, complexes with mixed ligands {[Cu(bpy)22OClO3)]ClO4}n (1) and [Cu(phen)2(OH2)](ClO4)2 (2) (bpy: 2,2'-biyridine; phen and 1,10-phenantroline) were evaluated for their antibacterial and cytotoxicicity features and for the elucidation of some of the mechanisms involved. Complex (2) proved to be a very potent antibacterial agent, exhibing MIC and MBEC values 2 to 54 times lower than those obtained for complex (1) against both susceptible or resistant Gram-positive and Gram-negative strains, in planktonic or biofilm growth state. In exchange, complex (1) exhibited selective cytotoxicity against melanoma tumor cells (B16), proving a promising potential for developing novel anticancer drugs. The possible mechanisms of both antimicrobial and antitumor activity of the copper(II) complexes is their DNA intercalative ability coupled with ROS generation. The obtained results recommend the two complexes for further development as multipurpose copper-containing drugs.

Keywords: 1,10-Phenantroline; 2,2′-biyridine; Biofilm; Copper(ii) complex; DNA intercalation; Melanoma cells; Saccharomyces cerevisiae.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Chelating Agents / pharmacology
  • Coordination Complexes* / chemistry
  • Coordination Complexes* / pharmacology
  • Copper / chemistry
  • Copper / pharmacology
  • Crystallography, X-Ray
  • Ligands

Substances

  • Anti-Bacterial Agents
  • Antineoplastic Agents
  • Chelating Agents
  • Coordination Complexes
  • Ligands
  • Copper