4.5 Article

Anti-tumor effects of valproate zinc complexes on a lung cancer cell line

Journal

POLYHEDRON
Volume 208, Issue -, Pages -

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.poly.2021.115415

Keywords

Cytotoxicity; Coordination compounds; Cell viability; Cell cycle; Apoptosis; SCFAs

Funding

  1. CAPES
  2. FAPERGS [16/2551-0000523-0]

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Valproate-Zn+2 complexes exhibit potential anti-tumoral activity in lung cancer cells, with complex 2 showing higher selectivity. The results suggest these complexes could serve as prototypes for new drugs.
Lung cancer is one of the most common types of cancer worldwide and the development of new treatment strategies is needed. Valproate exhibits anti-cancer properties and has been studied as a candidate for cancer therapy. Novel treatments with synthesized coordination complexes with valproate bioisosteres are promising, as they are often more effective and selective than organic molecules. We evaluated the anti-tumoral effects of two ternary complexes containing Zn+2, valproate, and 2,2 '-bipyridine (complex 1) or nicotinamide (complex 2) in a lung cancer cell line. Both complexes 1 and 2 exerted a 50% reduction in the viability of human epithelial lung cells (A549), indicating that coordination with Zn+2 improves the cytotoxic effects of valproate. Complex 1 increased the frequency of apoptotic cells 6-fold compared to vehicle, but it was less selective to tumor cells than complex 2. Complex 2 reduced the frequency of cells in S phase at rates similar to valproate (from 10.2% in the control to 0% in both complex 2 and valproate). Our data highlighted the potential anti-tumoral activity of valproate-Zn+2 complexes and their viability as proptotypes for new drugs.

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