Antineoplastic Evaluation of Two Mixed Chelate Copper Complexes (Casiopeínas®) in HCT-15 Xenograft Model

Authors

  • María Elena Bravo-Gómez Universidad Nacional Autónoma de México
  • Ana Laura Hernández de la Paz Universidad Nacional Autónoma de México
  • Isabel Gracia-Mora Universidad Nacional Autónoma de México

DOI:

https://doi.org/10.29356/jmcs.v57i3.208

Keywords:

Copper, mixed chelate, anticancer compounds, xenograft models, SAR relationships

Abstract

Casiopeínas® is a family of copper complexes with the general formulae [Cu(N-N)(N-O)]NO3 and [Cu(N-N)(O-O)]NO3; where N-N = substituted aromatic diimine (2,2’-bipyridine (bipy) or 1,10-phenanthroline (phen)); N-O = α-aminoacidate or a peptide; and O-O = acetylacetonate (acac) or salicylaldehydate. These compounds have shown antiproliferative activity in vitro and antitumor activity in several mouse models with promissory results. Efforts have been done in order to understand the role played by ligands in the biological activity. With the aim of finding out the effect of secondary ligand (N-O or O-O), two of the most active complexes in vitro assays were selected to perform in vivo study on HCT-15 colon adenocarcinoma xenograft model. Both complexes, [Cu(3,4,7,8-tetramethyl-1,10-phen anthroline)(glycinato)]NO3 (1) and [Cu(3,4,7,8-tetramethyl-1,10-phenanthroline)(acetylacetonato)]NO3 (2) share the same diimine ligand and the secondary ligand changes from glycinate (gly) to acac. Results show that 2 is effective to reduce tumor size but 1 does not achieve the values required according to protocols, revealing an important difference between compounds attributable to change of ligand from gly to acac.

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Author Biographies

María Elena Bravo-Gómez, Universidad Nacional Autónoma de México

Departamento de Química Inorgánica y Nuclear, Facultad de Química

Ana Laura Hernández de la Paz, Universidad Nacional Autónoma de México

Departamento de Química Inorgánica y Nuclear, Facultad de Química

Isabel Gracia-Mora, Universidad Nacional Autónoma de México

Unidad de Experimentación Animal (UNEXA), Facultad de Química

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Published

2017-10-12

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