Strong in vitro anticancer activity of copper(ii) and zinc(ii) complexes containing naturally occurring lapachol: cellular effects in ovarian A2780 cells

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F24%3A73626127" target="_blank" >RIV/61989592:15640/24:73626127 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/61989592:15310/24:73626127

Výsledek na webu

<a href="https://pubs.rsc.org/en/content/articlelanding/2024/md/d4md00543k" target="_blank" >https://pubs.rsc.org/en/content/articlelanding/2024/md/d4md00543k</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1039/d4md00543k" target="_blank" >10.1039/d4md00543k</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Strong in vitro anticancer activity of copper(ii) and zinc(ii) complexes containing naturally occurring lapachol: cellular effects in ovarian A2780 cells

Popis výsledku v původním jazyce

Copper(II) and zinc(II) complexes with lapachol (HLap) of the composition [M(Lap)(2)(N-N)] and [Cu(Lap)(H2O)(terpy)]NO3 (4), where M = Cu (1-3) or Zn (for 5-7), and N-N stands for bathophenanthroline (1 and 5), 5-methyl-1,10-phenanthroline (2 and 6), 2,2 &apos;-bipyridine (3), 2,2 &apos;;6 &apos;,2 &apos;&apos;-terpyridine (terpy, 4) and 1,10-phenanthroline (7), were synthesised and characterised. Complexes 1-5 revealed strong in vitro antiproliferative effects against A2780, A2780R, MCF-7, PC-3, A549 and HOS human cancer lines and MRC-5 normal cells, with IC50 values above 0.5 mu M, and reasonable selectivity index (SI), with SI &gt; 3.8 for IC50(MRC-5)/IC50(A2780). Considerable time-dependent cytotoxicity in A2780 cells was observed for complexes 6 and 7, with IC50 &gt; 50 mu M (24 h) to ca. 4 mu M (48 h). Cellular effects of complexes 1, 5 and 7 in A2780 cells were investigated by flow cytometry revealing that the most cytotoxic complexes (1 and 5) significantly perturbed the mitochondrial membrane potential and the interaction with mitochondrial metabolism followed by the triggering of the intracellular pathway of apoptosis.

Název v anglickém jazyce

Strong in vitro anticancer activity of copper(ii) and zinc(ii) complexes containing naturally occurring lapachol: cellular effects in ovarian A2780 cells

Popis výsledku anglicky

Copper(II) and zinc(II) complexes with lapachol (HLap) of the composition [M(Lap)(2)(N-N)] and [Cu(Lap)(H2O)(terpy)]NO3 (4), where M = Cu (1-3) or Zn (for 5-7), and N-N stands for bathophenanthroline (1 and 5), 5-methyl-1,10-phenanthroline (2 and 6), 2,2 &apos;-bipyridine (3), 2,2 &apos;;6 &apos;,2 &apos;&apos;-terpyridine (terpy, 4) and 1,10-phenanthroline (7), were synthesised and characterised. Complexes 1-5 revealed strong in vitro antiproliferative effects against A2780, A2780R, MCF-7, PC-3, A549 and HOS human cancer lines and MRC-5 normal cells, with IC50 values above 0.5 mu M, and reasonable selectivity index (SI), with SI &gt; 3.8 for IC50(MRC-5)/IC50(A2780). Considerable time-dependent cytotoxicity in A2780 cells was observed for complexes 6 and 7, with IC50 &gt; 50 mu M (24 h) to ca. 4 mu M (48 h). Cellular effects of complexes 1, 5 and 7 in A2780 cells were investigated by flow cytometry revealing that the most cytotoxic complexes (1 and 5) significantly perturbed the mitochondrial membrane potential and the interaction with mitochondrial metabolism followed by the triggering of the intracellular pathway of apoptosis.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

10402 - Inorganic and nuclear chemistry

Projekt

<a href="/cs/project/GA21-19060S" target="_blank" >GA21-19060S: Protinádorově aktivní koordinační sloučeniny s multimodálním účinkem</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2024

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

RSC MEDICINAL CHEMISTRY

ISSN

2632-8682

e-ISSN

2632-8682

Svazek periodika

15

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

GB - Spojené království Velké Británie a Severního Irska

Počet stran výsledku

13

Strana od-do

4180-4192

Kód UT WoS článku

001328548000001

EID výsledku v databázi Scopus

2-s2.0-85205910133