Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F18%3A10374332" target="_blank" >RIV/00179906:_____/18:10374332 - isvavai.cz</a>

Výsledek na webu

<a href="https://doi.org/10.1016/j.jorganchem.2018.01.031" target="_blank" >https://doi.org/10.1016/j.jorganchem.2018.01.031</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.jorganchem.2018.01.031" target="_blank" >10.1016/j.jorganchem.2018.01.031</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity

Popis výsledku v původním jazyce

A series of four ferrocenyl chalcone derivatives (1-4) and one ferrocenyl non- chalcone derivative (5) were investigated with regards to their interactions with calf thymus DNA and bovine serum albumin (BSA). Study on the DNA/BSA interactive properties of complexes is one of the active subjects of bioorganic chemistry. It could provide fundamental data for developing potential therapeutic applications and understanding mechanism of action for drug. The interactions and binding characteristics of complexes with ctDNA and BSA were investigated using UV-Vis, CD and fluorescence spectroscopy. Moreover, topoisomerase inhibition assays were used to evaluate the ability of compounds to inhibit the activity of topoisomerases I/II. No interaction was detected between ctDNA and ferrocene derivatives. However, human topoisomerase I (hTOPI) was inhibited in a concentration-depend manner in the presence of compounds 1, 3, 4, although no inhibition was observed with compounds 2 and 5. In the case of human topoisomerase II alpha, inhibitionwas observed and results indicate that these compounds can be classified as topoisomerase II suppressors, not poisons. The interaction between BSA and the four selected ligands (1-4) were studied by fluorescence quenching spectra. In addition, this method was used for the calculation of characteristic binding parameters. These results and results obtained by synchronous fluorescence spectra and 3D fluorescence spectra of the ferrocenyl chalcones with BSA determined that compounds create complexes with BSA and induce conformation changes.

Název v anglickém jazyce

Selected ferrocenyl chalcones as DNA/BSA-interacting agents and inhibitors of DNA topoisomerase I and II activity

Popis výsledku anglicky

A series of four ferrocenyl chalcone derivatives (1-4) and one ferrocenyl non- chalcone derivative (5) were investigated with regards to their interactions with calf thymus DNA and bovine serum albumin (BSA). Study on the DNA/BSA interactive properties of complexes is one of the active subjects of bioorganic chemistry. It could provide fundamental data for developing potential therapeutic applications and understanding mechanism of action for drug. The interactions and binding characteristics of complexes with ctDNA and BSA were investigated using UV-Vis, CD and fluorescence spectroscopy. Moreover, topoisomerase inhibition assays were used to evaluate the ability of compounds to inhibit the activity of topoisomerases I/II. No interaction was detected between ctDNA and ferrocene derivatives. However, human topoisomerase I (hTOPI) was inhibited in a concentration-depend manner in the presence of compounds 1, 3, 4, although no inhibition was observed with compounds 2 and 5. In the case of human topoisomerase II alpha, inhibitionwas observed and results indicate that these compounds can be classified as topoisomerase II suppressors, not poisons. The interaction between BSA and the four selected ligands (1-4) were studied by fluorescence quenching spectra. In addition, this method was used for the calculation of characteristic binding parameters. These results and results obtained by synchronous fluorescence spectra and 3D fluorescence spectra of the ferrocenyl chalcones with BSA determined that compounds create complexes with BSA and induce conformation changes.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

—

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2018

Kód důvěrnosti údajů

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

Název periodika

Journal of Organometallic Chemistry

ISSN

0022-328X

e-ISSN

—

Svazek periodika

861

Číslo periodika v rámci svazku

April

Stát vydavatele periodika

CH - Švýcarská konfederace

Počet stran výsledku

9

Strana od-do

1-9

Kód UT WoS článku

000428289400001

EID výsledku v databázi Scopus

2-s2.0-85042632202