J 2020

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

KAUEROVÁ, Tereza, Tomáš GONĚC, Josef JAMPÍLEK, Susanne HAFNER, Ann-Kathrin GAISER et. al.

Basic information

Original name

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

Authors

KAUEROVÁ, Tereza (203 Czech Republic, belonging to the institution), Tomáš GONĚC (203 Czech Republic, belonging to the institution), Josef JAMPÍLEK (703 Slovakia), Susanne HAFNER (276 Germany), Ann-Kathrin GAISER (276 Germany), Tatiana SYROVETS (276 Germany), Radek FEDR (203 Czech Republic), Karel SOUČEK (203 Czech Republic) and Peter KOLLÁR (203 Czech Republic, guarantor, belonging to the institution)

Edition

International Journal of Molecular Sciences, Basel, Multidisciplinary Digital Publishing Institute, 2020, 1422-0067

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

Switzerland

Confidentiality degree

není předmětem státního či obchodního tajemství

Impact factor

Impact factor: 5.923

RIV identification code

RIV/00216224:14160/20:00116289

Organization unit

Faculty of Pharmacy

UT WoS

000539312100012

Keywords (in Czech)

salicylanilidy; hydroxynaftalenkarboxamidy; apoptóza; buněčný cyklus; antiproliferativní účinek

Keywords in English

salicylanilides; hydroxynaphthalene carboxamides; apoptosis; cell cycle; antiproliferative effect

Tags

Tags

International impact, Reviewed
Změněno: 22/3/2021 12:59, Mgr. Hana Hurtová

Abstract

V originále

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.