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Cytotoxic and apoptotic effects of ternary silver(I) complexes bearing 2-formylpyridine thiosemicarbazones and 1,10-phenanthroline

Abstract

New silver(I) compounds containing 2-formylpyridine-N(4)-R-thiosemicarbazones and 1,10-phenanthroline (phen) were synthesized and characterized by spectroscopic techniques (IR and NMR), elemental analysis, ESI-MS and molar condutance measurements. In these complexes, both phen and thiosemicarbazone ligands are coordinated in a chelating bidentate fashion. The compounds 1-3 showed not only good in vitro antiproliferative activity against human lung (A549) and breast tumor cells (MDA-MB-231 and MCF-7), with IC50 values ranging from 1.49 to 20.90 μM, but also demonstrated to be less toxic towards human breast non-tumor cells (MCF-10A). Uptake cellular studies indicated that compounds 1-3 were taken up by MDA-MB-231 cells in 6 hours. Cell death assays in MDA-MB-231 cells were conducted with compound 1 aiming at to evaluate its effects in cell morphology, induction of apoptosis, cell cycle, reactive oxygen species (ROS) and mitochondrial membrane potential (ΔΨm). Compound 1 caused morphological changes, such as cell shrinkage and rounding, increased the sub-G1 phase population, induced apoptotic cell death, ROS formation and loss of mitochondrial membrane potential (ΔΨm). DNA binding results revealed that 1 interacted with ct-DNA minor groove. Complexes 1-3 also exhibited good in vitro activity against M. tuberculosis H37Rv, with MIC values varying from 3.37-4.65 μM.

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Article information


Submitted
22 Jan 2020
Accepted
20 Mar 2020
First published
23 Mar 2020

Dalton Trans., 2020, Accepted Manuscript
Article type
Paper

Cytotoxic and apoptotic effects of ternary silver(I) complexes bearing 2-formylpyridine thiosemicarbazones and 1,10-phenanthroline

D. E. S. Silva, A. B. Becceneri, M. C. Solcia, J. V. B. Santiago, M. B. Moreira, J. A. G. Neto, F. R. Pavan, M. R. Cominetti, J. C. M. Pereira and A. Vieira de Godoy Netto, Dalton Trans., 2020, Accepted Manuscript , DOI: 10.1039/D0DT00253D

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