1. Anticancer activity of two novel ruthenium compounds in gastric cancer cells.
- Author
-
Ramírez-Rivera S, Pizarro S, Gallardo M, Gajardo F, Delgadillo A, De La Fuente-Ortega E, MacDonnell FM, and Bernal G
- Subjects
- Antineoplastic Agents pharmacology, Apoptosis drug effects, Cell Line, Tumor drug effects, Cell Survival drug effects, Cisplatin pharmacology, Dose-Response Relationship, Drug, Humans, Ruthenium pharmacology, Ruthenium therapeutic use, Ruthenium Compounds therapeutic use, Stomach Neoplasms drug therapy, Structure-Activity Relationship, Ruthenium Compounds pharmacology, Stomach Neoplasms metabolism
- Abstract
Aims: Ruthenium (II) complexes are promising anticancer molecules due its pharmacological properties and selectivity to cells tumor. The aim of this work was to study the cytotoxic activity, and apoptosis induction of two new ruthenium complexes on a human gastric cancer cell line., Main Methods: Two ruthenium(II) complexes were synthesized: [(H
2 pbbzim)Ru(tpy-Ph-COOCH3 )](Cl)2 (Ru-UCN1), and [(tpy)Ru(tpy-Ph-bzH)](Cl)2 (Ru-UCN3), and their anticancer capacity determined by cytotoxic assays, gene expression analysis, caspase activation and confocal microscopy., Key Findings: Ru-UCN3 is more notably cytotoxic than cisplatin in human gastric cancer cells AGS at 24 h, while Ru-UCN1 is more active against gastric cancer cells than cisplatin at 48 h. The complexes induce apoptosis as shown by RT-qPCR, protease activity, and confocal microscopy. Ru-UCN1 induces the overexpression of pro-apoptotic genes at 3 and 6 h, whereas Ru-UCN3 induces overexpression of these genes at 12 and 24 h. Ru-UCN1 treatment shows a strong activation of caspases 3/7 at 24 h, which was not observed for Ru-UCN3 treatment in the same timeframe., Significance: Taken together, this data suggests that Ru-UCN1 and to a lesser extent, Ru-UCN3, may be interesting anticancer agents for gastric cancer., (Copyright © 2018 Elsevier Inc. All rights reserved.)- Published
- 2018
- Full Text
- View/download PDF