Synthesis, characterization and antitumoral activity of new cobalt(II)complexes: Effect of the ligand isomerism on the biological activity of the complexes
| Autor: | Érika S. Bull, Samila R. Morcelli, João Carlos de Aquino Almeida, Adolfo Horn Junior, Adailton J. Bortoluzzi, Leide Laura Figueiredo Maciel, Rafaela Oliveira Moreira, Milton M. Kanashiro, Wagner da Silva Terra, Christiane Fernandes, Franz Viana Borges |
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| Rok vydání: | 2016 |
| Předmět: |
Stereochemistry
chemistry.chemical_element Antineoplastic Agents Apoptosis Propylamine 010402 general chemistry 01 natural sciences Biochemistry Peripheral blood mononuclear cell Coordination complex Inorganic Chemistry chemistry.chemical_compound Neoplasms Humans Cytotoxicity Membrane Potential Mitochondrial chemistry.chemical_classification 010405 organic chemistry Biological activity Cobalt U937 Cells 0104 chemical sciences chemistry Cell culture Leukocytes Mononuclear Drug Screening Assays Antitumor |
| Zdroj: | Journal of Inorganic Biochemistry. 161:73-82 |
| ISSN: | 0162-0134 |
| DOI: | 10.1016/j.jinorgbio.2016.05.003 |
| Popis: | The synthesis, physico-chemical characterization and cytotoxicity against five human tumoral cell lines (THP-1, U937, Molt-4, Colo205 and H460) of three new cobalt(II) coordination compounds are reported (i.e. Co(HL1)Cl (1), Co(HL2)Cl (2) and [Co(HL3)Cl]0.0.5 (CH3)2CHOH (3)). H2L2 (2-{[[2-hydroxy-3-(1-naphthyloxy)propyl](pyridin-2-ylmethyl)amino]methyl}phenol) and H2L3 (2-{[[2-hydroxy-3-(2-naphthyloxy)propyl](pyridin-2-ylmethyl)amino]methyl}phenol) present α and β-naphthyl groups respectively, which is absent in H2L1 (N-(2-hydroxybenzyl)-N-(2-pyridylmethyl)[(3-chloro)(2-hydroxy)]propylamine. These compounds were characterized by a range of physico-chemical methods. X-ray diffraction studies were performed for complex (3), indicating the formation of a mononuclear complex. Complexes (2) and (3), which contain α and β-naphthyl groups respectively, have presented lower IC50 values than those exhibited by complex (1). Complex (3) presents IC50 values lower than cisplatin against Colo205 (90 and 196μmolL(-1), respectively) and H460 (147 and 197μmolL(-1), respectively). These human neoplastic cells under investigation were also more susceptible toward complex (3) than peripheral blood mononuclear cells. Transmission electron microscopy investigations are in agreement with the loss of mitochondrial membrane potential (ΔΨm) observed by JC-1 mitochondrial potential sensor and indicate that the activity of complex (3) against leukemic cell line (U937) is mediated by an apoptotic mechanism associated with mitochondrial dysfunction (intrinsic pathway). |
| Databáze: | OpenAIRE |
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