Počet záznamů: 1  

N-Indolyl diiron vinyliminium complexes exhibit antiproliferative effects in cancer cells associated with disruption of mitochondrial homeostasis, ROS scavenging, and antioxidant activity

  1. 1.
    SYSNO ASEP0583469
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevN-Indolyl diiron vinyliminium complexes exhibit antiproliferative effects in cancer cells associated with disruption of mitochondrial homeostasis, ROS scavenging, and antioxidant activity
    Tvůrce(i) Bresciani, G. (IT)
    Červinka, Jakub (BFU-R)
    Kostrhunová, Hana (BFU-R) RID, ORCID
    Biancalana, L. (IT)
    Bortoluzzi, M. (IT)
    Pampaloni, G. (IT)
    Novohradský, Vojtěch (BFU-R) ORCID
    Brabec, Viktor (BFU-R) RID, ORCID
    Marchetti, F. (IT)
    Kašpárková, Jana (BFU-R) RID, ORCID
    Celkový počet autorů10
    Číslo článku110742
    Zdroj.dok.Chemico-Biological Interactions. - : Elsevier - ISSN 0009-2797
    Roč. 385, NOV 1 2023 (2023)
    Poč.str.15 s.
    Jazyk dok.eng - angličtina
    Země vyd.IE - Irsko
    Klíč. slovabasis-sets ; mechanisms ; cisplatin ; molecules ; drugs ; oxaliplatin ; insertion ; energies
    Vědní obor RIVCE - Biochemie
    Obor OECDBiochemistry and molecular biology
    CEPGA23-06316S GA ČR - Grantová agentura ČR
    Způsob publikováníOpen access
    Institucionální podporaBFU-R - RVO:68081707
    UT WOS001094243700001
    EID SCOPUS85173242183
    DOI10.1016/j.cbi.2023.110742
    AnotaceThe indole scaffold has been established as a key organic moiety for developing new drugs, on the other hand, a range of diiron bis-cyclopentadienyl complexes have recently emerged for their promising anticancer potential. Here, we report the synthesis of novel diiron complexes with an indole-functionalized vinyliminium ligand (2-5) and an indole-lacking analogue for comparative purposes (6), which were characterized by analytical and spectroscopic techniques. Complexes 2-6 are substantially stable in DMSO-d6 and DMEM-d solutions at 37 degrees C (8% average degradation after 48 h) and display a balanced hydrophilic/lipophilic behaviour (LogPow values in the range0.32 to 0.47), associated with appreciable water solubility. The complexes display selective antiproliferative potency towards several cancer cells in monolayer cultures, mainly in the low micromolar range, with reduced toxicity towards noncancerous epithelial cells. Thus, the cytotoxicity of the complexes is comparable to or better than clinically used metallopharmaceutical cisplatin. Comparing the antiproliferative activity obtained for complexes containing different ligands, we confirmed the importance of the indolyl group in the mechanism of antiproliferative activity of these complexes. Cell-based mechanistic studies suggest that the investigated diiron vinyliminium complexes (DVCs) show cytostatic rather than cytotoxic effects and subsequently induce a population of cells to undergo apoptosis. Furthermore, the molecular mechanism of action involves interactions with mitochondrial DNA and proteins, the reactive oxygen species (ROS)-scavenging properties and antioxidant activity of these complexes in cancer cells. This study highlights the importance of DVCs to their cancer cell activity and reinforces their prospective therapeutic potential as anticancer agents.
    PracovištěBiofyzikální ústav
    KontaktJana Poláková, polakova@ibp.cz, Tel.: 541 517 244
    Rok sběru2024
    Elektronická adresahttps://www.sciencedirect.com/science/article/pii/S000927972300409X?via%3Dihub
Počet záznamů: 1  

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