Potential antiprostatic performance of novel lanthanide-complexes based on 5-nitropicolinic acid

J Biol Inorg Chem. 2024 Apr;29(3):331-338. doi: 10.1007/s00775-024-02054-0. Epub 2024 May 8.

Abstract

Two new lanthanide-complexes based on the 5-nitropicolinate ligand (5-npic) were obtained and fully characterized. Single-crystal X-ray diffraction revealed that these compounds are isostructural to a Dy-complex, previously published by us, based on dinuclear monomers link together with an extended hydrogen bond network, providing a final chemical formula of [Ln2(5-npic)6(H2O)4]·(H2O)2, where Ln = Dy (1), Gd (2), and Tb (3). Preliminary photoluminescent studies exhibited a ligand-centered emission for all complexes. The potential antitumoral activity of these materials was assayed in a prostatic cancer cell line (PC-3; the 2nd most common male cancerous disease), showing a significant anticancer activity (50-60% at 500 μg·mL-1). In turn, a high biocompatibility by both, the complexes and their precursors in human immunological HL-60 cells, was evidenced. In view of the strongest toxic effect in the tumoral cell line provided by the free 5-npic ligand (~ 40-50%), the overall anticancer complex performance seems to be triggered by the presence of this molecule.

Keywords: 5-Nitropicolinic acid; Coordination compounds; Lanthanide; Prostate cancer; Single-crystal X-ray diffraction.

MeSH terms

  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Cell Survival / drug effects
  • Coordination Complexes / chemical synthesis
  • Coordination Complexes / chemistry
  • Coordination Complexes / pharmacology
  • Crystallography, X-Ray
  • Drug Screening Assays, Antitumor
  • HL-60 Cells
  • Humans
  • Lanthanoid Series Elements* / chemistry
  • Lanthanoid Series Elements* / pharmacology
  • Male
  • Models, Molecular
  • Molecular Structure
  • PC-3 Cells
  • Picolinic Acids* / chemistry
  • Picolinic Acids* / pharmacology
  • Prostatic Neoplasms / drug therapy
  • Prostatic Neoplasms / pathology

Substances

  • Lanthanoid Series Elements
  • Picolinic Acids
  • Antineoplastic Agents
  • Coordination Complexes