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@article{1675888,
author = {Kauerová, Tereza and Goněc, Tomáš and Jampílek, Josef and Hafner, Susanne and Gaiser, AnnandKathrin and Syrovets, Tatiana and Fedr, Radek and Souček, Karel and Kollár, Peter},
article_location = {Basel},
article_number = {10},
doi = {http://dx.doi.org/10.3390/ijms21103416},
keywords = {salicylanilides; hydroxynaphthalene carboxamides; apoptosis; cell cycle; antiproliferative effect},
language = {eng},
issn = {1422-0067},
journal = {International Journal of Molecular Sciences},
title = {Ring-Substituted 1-Hydroxynaphthalene-2-Carboxanilides Inhibit Proliferation and Trigger Mitochondria-Mediated Apoptosis},
url = {https://www.mdpi.com/1422-0067/21/10/3416/htm},
volume = {21},
year = {2020}
}
TY - JOUR
ID - 1675888
AU - Kauerová, Tereza - Goněc, Tomáš - Jampílek, Josef - Hafner, Susanne - Gaiser, Ann-Kathrin - Syrovets, Tatiana - Fedr, Radek - Souček, Karel - Kollár, Peter
PY - 2020
TI - Ring-Substituted 1-Hydroxynaphthalene-2-Carboxanilides Inhibit Proliferation and Trigger Mitochondria-Mediated Apoptosis
JF - International Journal of Molecular Sciences
VL - 21
IS - 10
SP - 1-17
EP - 1-17
PB - Multidisciplinary Digital Publishing Institute
SN - 14220067
KW - salicylanilides
KW - hydroxynaphthalene carboxamides
KW - apoptosis
KW - cell cycle
KW - antiproliferative effect
UR - https://www.mdpi.com/1422-0067/21/10/3416/htm
L2 - https://www.mdpi.com/1422-0067/21/10/3416/htm
N2 - Ring-substituted 1-hydroxynaphthalene-2-carboxanilides were previously investigated for their antimycobacterial properties. In our study, we have shown their antiproliferative and cell death-inducing effects in cancer cell lines. Cell proliferation and viability were assessed by WST-1 assay and a dye exclusion test, respectively. Cell cycle distribution, phosphatidylserine externalization, levels of reactive oxygen or nitrogen species (RONS), mitochondrial membrane depolarization, and release of cytochrome c were estimated by flow cytometry. Levels of regulatory proteins were determined by Western blotting. Our data suggest that the ability to inhibit the proliferation of THP-1 or MCF-7 cells might be referred to meta- or para-substituted derivatives with electron-withdrawing groups -F, -Br, or -CF3 at anilide moiety. This effect was accompanied by accumulation of cells in G1 phase. Compound 10 also induced apoptosis in THP-1 cells in association with a loss of mitochondrial membrane potential and production of mitochondrial superoxide. Our study provides a new insight into the action of salicylanilide derivatives, hydroxynaphthalene carboxamides, in cancer cells. Thus, their structure merits further investigation as a model moiety of new small-molecule compounds with potential anticancer properties.
ER -
KAUEROVÁ, Tereza, Tomáš GONĚC, Josef JAMPÍLEK, Susanne HAFNER, Ann-Kathrin GAISER, Tatiana SYROVETS, Radek FEDR, Karel SOUČEK and Peter KOLLÁR. Ring-Substituted 1-Hydroxynaphthalene-2-Carboxanilides Inhibit Proliferation and Trigger Mitochondria-Mediated Apoptosis. \textit{International Journal of Molecular Sciences}. Basel: Multidisciplinary Digital Publishing Institute, 2020, vol.~21, No~10, p.~1-17. ISSN~1422-0067. Available from: https://dx.doi.org/10.3390/ijms21103416.
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