Anticancer activity of salinomycin quaternary phosphonium salts

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dc.contributor.authorJędrzejczyk, Marta
dc.contributor.authorSulik, Michał
dc.contributor.authorMielczarek-Puta, Magdalena
dc.contributor.authorLim, Gwan Yong
dc.contributor.authorPodsiad, Małgorzata
dc.contributor.authorHoser, Jakub
dc.contributor.authorBednarczyk, Piotr
dc.contributor.authorStruga, Marta
dc.contributor.authorHuczynski, Adam
dc.contributor.organizationZakład Chemii Medycznej, Wydział Chemii, Uniewersytet im. Adama Mickiewicza w Poznaniu
dc.contributor.organizationKatedra Fizyki i Biofizyki, Instytut Biologii, Szkoła Główna Gospodarstwa Wiejskiego w Warszawie
dc.contributor.organizationKatedra i Zakład Biochemii, Wydział Lekarski, Uniwersytet Medyczny w Warszawie
dc.date.accessioned2024-11-19T17:24:31Z
dc.date.available2024-11-19T17:24:31Z
dc.date.issued2015-01-15
dc.description.abstractIn recent years salinomycin has emerged as a promising anticancer drug. Many literature reports have proved its remarkable antiproliferative activity. Moreover, chemical modifications of salinomycin lead to analogues with even higher cytotoxicity against cancer cell lines and a better selectivity index for malignant cells than those of the unmodified compound or a standard anticancer drug such as doxorubicin. In this paper we report the syn thesis of a series of twelve novel salinomycin conjugates and their characterization by spectroscopic and spec trometric methods. Salinomycin was conjugated with different triphenylphosphonium cations in order to find out whether the conjugation with mitochondrial targeting vectors would have a beneficial impact on biological properties. Salinomycin and its novel conjugates were tested to determine their in vitro antiproliferative and antimicrobial activity. Taking into account the presence of triphenylphosphonium moiety, the impact of the obtained analogues on mitochondria activity was evaluated by MitoTrackers dyes, furthermore their apoptosis effect and cell cycle arrest were assessed. In addition, the changes in the mitochondrial membrane potential were measured and the ability to generate reactive oxygen species was assessed. Finally, we conducted biophysical studies to investigate the impact of the obtained salinomycin analogues on mitochondrial respiration rates and their electrophysiological properties. Results of this study have proved that conjugation of salinomycin with phosphonium cations leads to promising results in the search for promising anticancer agents.en
dc.description.sponsorshipProjekt pt.:”Koniugaty celujące w mitochondria jako nowe środki przeciwnowotworowe” finansowano z grantu Narodowego Centrum Nauki – OPUS 21 (2021/41/B/ST4/00088).
dc.identifier.citationEur. J. Med. Chem., Vol. 282, 2025, 117055
dc.identifier.doi10.1016/j.ejmech.2024.117055
dc.identifier.issn0223-5234
dc.identifier.urihttps://open.icm.edu.pl/handle/123456789/25117
dc.language.isoen
dc.publisherElsevier
dc.rightsUznanie autorstwa 4.0 Międzynarodoween
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.sourceEuropean Journal of Medicinal Chemistry
dc.subjectionophoresen
dc.subjectmitochondria-targetingen
dc.subjecttriphenylphosphineen
dc.subjectTPP cationen
dc.subjectanticanceren
dc.titleAnticancer activity of salinomycin quaternary phosphonium saltsen
dc.title.alternativeAktywność przeciwnowotworowa czwartorzędowych soli fosfoniowych salinomycynypl
dc.typearticle
dc.type.versionpublishedVersion
person.identifier.orcidJędrzejczyk, Marta [0000-0003-4214-569X]
person.identifier.orcidHuczyński, Adam [0000-0003-4770-215X]
person.identifier.orcidSulik, Michał [0000-0001-6127-9621]
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