Autophagy Promotes Survival of CHP-212 Neuroblastoma Cells Treated With Casiopeínas®.

Background: Neuroblastoma is the main solid extracranial tumor of childhood. The amplification of N-myc oncogene (MYCN) and 1p deletion are the main molecular alterations. These features are what make treatment impossible, especially in high-risk patients with metastases.

The mitochondrial apoptotic pathway is induced by Cu(II) antineoplastic compounds (Casiopeínas) in SK-N-SH neuroblastoma cells after short exposure times.

The family of Copper(II) coordination compounds Casiopeínas (Cas) has shown antiproliferative activity in several tumour lines by oxidative cellular damage and mitochondrial dysfunction that lead to cell death through apoptotic pathways. The goal of this work is looking for the functional mechanism of CasIIgly, CasIIIia and CasIIIEa in neuroblastoma metastatic cell line SK-N-SH, a paediatric extra-cranial tumour which is refractory to several anti-carcinogenic agents. All Cas have shown higher antiproliferative activity than cisplatin (IC = 123 μM) with IC values of 18, 22 and 63 µM for CasIIgly, CasIIIEa and CasIIIia, respectively.

Copper(II) mixed chelate compounds induce apoptosis through reactive oxygen species in neuroblastoma cell line CHP-212.

In the present work we report the antiproliferative activity of Cu(II) coordination compounds, CasIIgly ([Cu(4,7-dimethyl-1,10-phenanthroline) (glycinato) (H2O)]NO3), CasIIIia ([Cu(4,4'-dimethyl-2,2'-bipyridine) (glycinato) (H2O)]NO3), and CasIIIEa ([Cu(4,7-dimethyl-1,10-phenanthroline) (acetylacetonato) (H2O)]NO3), against human tumoral cell line CHP-212 (estromal neuroblastoma). Additionally, the molecular structure of CasIIIEa was reported. The IC50 values obtained for the evaluated compounds are in the range 18 to 47 μM, representing an inhibition potency increase of 5 to 12 times compared with cisplatin (IC50=226.

Whole genome gene expression analysis reveals casiopeína-induced apoptosis pathways.

Copper-based chemotherapeutic compounds Casiopeínas, have been presented as able to promote selective programmed cell death in cancer cells, thus being proper candidates for targeted cancer therapy. DNA fragmentation and apoptosis-in a process mediated by reactive oxygen species-for a number of tumor cells, have been argued to be the main mechanisms. However, a detailed functional mechanism (a model) is still to be defined and interrogated for a wide variety of cellular conditions before establishing settings and parameters needed for their wide clinical application.

Potential cytotoxic and amoebicide activity of first row transition metal compounds with 2,9-bis-(2',5'-diazahexanyl)-1,1-phenanthroline (L1).

A new synthetic pathway was reported to obtain N6 donor ligand 2,9-bis-(2',5'-diazahexanyl)-1,10-phenanthroline (L1) and its coordination compounds of essential divalent metal ions Mn, Fe, Co, Ni, Cu and Zn. Complete characterization of all compounds was done with the conventional techniques. Crystal structures of [NiL1](PF(6))(2) and [ZnL1](PF(6))(2)·H(2)O were also reported.