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PreprintCC BYChemRxiv

Pt(II)-Flavin Complexes As Anticancer And Antibacterial Agents

8 affiliations
  1. 1Euskal Herriko Unibertsitatea UPV/EHU, Paseo Manuel de Lardizabal 3, Donostia, Spain, 20018
  2. 2Donostia International Physics Center, Paseo Manuel de Lardizabal 4, Donostia, Spain, 20018
  3. 3Institute of Medicinal and Pharmaceutical Chemistry
  4. 4Technische Universität Braunschweig
  5. 5Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche, Università degli Studi di Palermo, Viale delle Scienze, Edificio 17, Palermo, Italy, 90128
  6. 6CNRS, IPREM UMR, 2 Av. du Président Pierre Angot, Pau cedex, France, 64053
  7. 7Ikerbasque
  8. 8Basque Foundation for Science

Abstract

We report a new chelating pyridyl–imine ligand bearing a riboflavin-derived pendant group and its Pt(II) complexes 1 and 2, designed as cisplatin- and oxaliplatin-like derivatives. Both complexes reacted with DNA and a histone-derived peptide, with 1 showing markedly higher covalent reactivity. However, this trend was not reflected in biological activity. Complex 2 displayed micromolar antiproliferative effects and pronounced antibacterial activity, particularly against Bacillus subtilis, whereas 1 was inactive in the tested models. Cellular accumulation studies excluded enhanced Pt uptake as the origin of this difference. Fluorescence microscopy performed on Escherichia Coli and Bacillus subtilis indicated that 2 affects bacterial DNA and membrane potential, consistent with a dual antibacterial mechanism. Comparison with oxaliplatin and the free flavin ligands showed that both the Pt–oxalate fragment and the riboflavin-containing ligand are required for activity.

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BibTeX
@misc{plata2026ptiiflavin,
  title = {{Pt(II)-Flavin Complexes As Anticancer And Antibacterial Agents}},
  author = {Maria Jesus Moran Plata and Igor V. Esarev and Nitin Kumar and Laura Marretta and Leo Pontfort and Ana Cristina Carrasco and Beatrice Bernadette Mascitti and Alessio Terenzi and Luisa Ronga and Ingo Ott and Luca Salassa},
  howpublished = {ChemRxiv},
  year = {2026},
  month = sep,
  doi = {10.26434/chemrxiv.15009344/v1},
  url = {https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009344/v1},
  note = {CC BY},
}
RIS
TY  - UNPB
TI  - Pt(II)-Flavin Complexes As Anticancer And Antibacterial Agents
AU  - Maria Jesus Moran Plata
AU  - Igor V. Esarev
AU  - Nitin Kumar
AU  - Laura Marretta
AU  - Leo Pontfort
AU  - Ana Cristina Carrasco
AU  - Beatrice Bernadette Mascitti
AU  - Alessio Terenzi
AU  - Luisa Ronga
AU  - Ingo Ott
AU  - Luca Salassa
PY  - 2026
DA  - 2026/09/23
PB  - ChemRxiv
DO  - 10.26434/chemrxiv.15009344/v1
UR  - https://chemrxiv.org/doi/full/10.26434/chemrxiv.15009344/v1
AB  - We report a new chelating pyridyl–imine ligand bearing a riboflavin-derived pendant group and its Pt(II) complexes 1 and 2, designed as cisplatin- and oxaliplatin-like derivatives. Both complexes reacted with DNA and a histone-derived peptide, with 1 showing markedly higher covalent reactivity. However, this trend was not reflected in biological activity. Complex 2 displayed micromolar antiproliferative effects and pronounced antibacterial activity, particularly against Bacillus subtilis, whereas 1 was inactive in the tested models. Cellular accumulation studies excluded enhanced Pt uptake as the origin of this difference. Fluorescence microscopy performed on Escherichia Coli and Bacillus subtilis indicated that 2 affects bacterial DNA and membrane potential, consistent with a dual antibacterial mechanism. Comparison with oxaliplatin and the free flavin ligands showed that both the Pt–oxalate fragment and the riboflavin-containing ligand are required for activity.
ER  -