Detail
Article
Online article
FT
Medvik - BMC
  • Something wrong with this record ?

Ring-Substituted 1-Hydroxynaphthalene-2-Carboxanilides Inhibit Proliferation and Trigger Mitochondria-Mediated Apoptosis

T. Kauerová, T. Goněc, J. Jampílek, S. Hafner, AK. Gaiser, T. Syrovets, R. Fedr, K. Souček, P. Kollar

. 2020 ; 21 (10) : . [pub] 20200512

Language English Country Switzerland

Document type Journal Article

Persistent link   https://www.medvik.cz/link/bmc21012594

Grant support
grant ITA by the University of Veterinary and Pharmaceutical Sciences Brno, No: FaF/Suchý/ITA 2019 Veterinární a Farmaceutická Univerzita Brno

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.

References provided by Crossref.org

000      
00000naa a2200000 a 4500
001      
bmc21012594
003      
CZ-PrNML
005      
20210507102555.0
007      
ta
008      
210420s2020 sz f 000 0|eng||
009      
AR
024    7_
$a 10.3390/ijms21103416 $2 doi
035    __
$a (PubMed)32408543
040    __
$a ABA008 $b cze $d ABA008 $e AACR2
041    0_
$a eng
044    __
$a sz
100    1_
$a Kauerová, Tereza $u Department of Pharmacology and Toxicology, Faculty of Pharmacy, Masaryk University, Palackeho tr. 1946/1, 612 42 Brno, Czech Republic
245    10
$a Ring-Substituted 1-Hydroxynaphthalene-2-Carboxanilides Inhibit Proliferation and Trigger Mitochondria-Mediated Apoptosis / $c T. Kauerová, T. Goněc, J. Jampílek, S. Hafner, AK. Gaiser, T. Syrovets, R. Fedr, K. Souček, P. Kollar
520    9_
$a 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.
650    _2
$a anilidy $x chemie $x farmakologie $7 D000813
650    _2
$a protinádorové látky $x chemie $x farmakologie $7 D000970
650    _2
$a apoptóza $x účinky léků $7 D017209
650    _2
$a buněčný cyklus $x účinky léků $7 D002453
650    _2
$a proliferace buněk $x účinky léků $7 D049109
650    _2
$a viabilita buněk $x účinky léků $7 D002470
650    _2
$a lidé $7 D006801
650    _2
$a MFC-7 buňky $7 D061986
650    _2
$a membránový potenciál mitochondrií $x účinky léků $7 D053078
650    _2
$a mitochondrie $x účinky léků $x metabolismus $7 D008928
650    _2
$a molekulární struktura $7 D015394
650    _2
$a naftoly $x chemie $7 D009284
650    _2
$a reaktivní formy kyslíku $x metabolismus $7 D017382
650    _2
$a salicylanilidy $x chemie $x farmakologie $7 D012458
650    _2
$a vztahy mezi strukturou a aktivitou $7 D013329
650    _2
$a superoxidy $x metabolismus $7 D013481
650    _2
$a THP-1 buňky $7 D000074084
655    _2
$a časopisecké články $7 D016428
700    1_
$a Goněc, Tomáš $u Department of Chemical Drugs, Faculty of Pharmacy, Masaryk University, Palackeho tr. 1946/1, 612 42 Brno, Czech Republic
700    1_
$a Jampílek, Josef $u Institute of Neuroimmunology, Slovak Academy of Sciences, Dubravska cesta 9, 845 10 Bratislava, Slovakia
700    1_
$a Hafner, Susanne $u Institute of Pharmacology of Natural Products and Clinical Pharmacology, Ulm University, Helmholtzstraße 20, 89081 Ulm, Germany
700    1_
$a Gaiser, Ann-Kathrin $u Institute of Pharmacology of Natural Products and Clinical Pharmacology, Ulm University, Helmholtzstraße 20, 89081 Ulm, Germany
700    1_
$a Syrovets, Tatiana $u Institute of Pharmacology of Natural Products and Clinical Pharmacology, Ulm University, Helmholtzstraße 20, 89081 Ulm, Germany
700    1_
$a Fedr, Radek $u Department of Cytokinetics, Institute of Biophysics of the Czech Academy of Sciences, Kralovopolska 135, 612 65 Brno, Czech Republic
700    1_
$a Souček, Karel $u Department of Cytokinetics, Institute of Biophysics of the Czech Academy of Sciences, Kralovopolska 135, 612 65 Brno, Czech Republic
700    1_
$a Kollar, Peter $u Department of Pharmacology and Toxicology, Faculty of Pharmacy, Masaryk University, Palackeho tr. 1946/1, 612 42 Brno, Czech Republic $u Department of Human Pharmacology and Toxicology, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences Brno, Palackeho tr. 1946/1, 612 42 Brno, Czech Republic
773    0_
$w MED00176142 $t International journal of molecular sciences $x 1422-0067 $g Roč. 21, č. 10 (2020)
856    41
$u https://pubmed.ncbi.nlm.nih.gov/32408543 $y Pubmed
910    __
$a ABA008 $b sig $c sign $y p $z 0
990    __
$a 20210420 $b ABA008
991    __
$a 20210507102555 $b ABA008
999    __
$a ok $b bmc $g 1650873 $s 1132973
BAS    __
$a 3
BAS    __
$a PreBMC
BMC    __
$a 2020 $b 21 $c 10 $e 20200512 $i 1422-0067 $m International journal of molecular sciences $n Int J Mol Sci $x MED00176142
GRA    __
$a grant ITA by the University of Veterinary and Pharmaceutical Sciences Brno, No: FaF/Suchý/ITA 2019 $p Veterinární a Farmaceutická Univerzita Brno
LZP    __
$a Pubmed-20210420

Find record

Citation metrics

Archiving options