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In vitro and in vivo investigation of cardiotoxicity associated with anticancer proteasome inhibitors and their combination with anthracycline

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    SYSNO ASEP0517578
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleIn vitro and in vivo investigation of cardiotoxicity associated with anticancer proteasome inhibitors and their combination with anthracycline
    Author(s) Pokorná, Z. (CZ)
    Jirkovský, E. (CZ)
    Hlaváčková, Markéta (FGU-C) RID, ORCID
    Jansová, H. (CZ)
    Jirkovská, A. (CZ)
    Lencová-Popelová, O. (CZ)
    Brázdová, P. (CZ)
    Kubeš, J. (CZ)
    Sotáková-Kašparová, Dita (FGU-C) RID, ORCID, SAI
    Mazurová, Y. (CZ)
    Adamcová, M. (CZ)
    Vostatková, L. (CZ)
    Holzerová, Kristýna (FGU-C) ORCID, RID
    Kolář, František (FGU-C) RID, ORCID, SAI
    Šimůnek, T. (CZ)
    Štěrba, M. (CZ)
    Source TitleClinical science. - : Portland Press - ISSN 0143-5221
    Roč. 133, č. 16 (2019), s. 1827-1844
    Number of pages18 s.
    Languageeng - English
    CountryGB - United Kingdom
    Keywordsanthracyclines ; bortezomib ; carfilzomib ; cardiotoxicity ; proteasome inhibitors
    Subject RIVFR - Pharmacology ; Medidal Chemistry
    OECD categoryPharmacology and pharmacy
    R&D ProjectsGA13-15008S GA ČR - Czech Science Foundation (CSF)
    Method of publishingLimited access
    Institutional supportFGU-C - RVO:67985823
    UT WOS000511195100001
    EID SCOPUS85071685471
    DOI https://doi.org/10.1042/CS20190139
    AnnotationAlthough proteasome inhibitors (PIs) are modern targeted anticancer drugs, they have been associated with a certain risk of cardiotoxicity and heart failure (HF). Recently, PIs have been combined with anthracyclines (ANTs) to further boost their anticancer efficacy. However, this raised concerns regarding cardiac safety, which were further supported by several in vitro studies on immature cardiomyocytes. In the present study, we investigated the toxicity of clinically used PIs alone (bortezomib (BTZ), carfilzomib (CFZ)) as well as their combinations with an ANT (daunorubicin (DAU)) in both neonatal and adult ventricular cardiomyocytes (NVCMs and AVCMs) and in a chronic rabbit model of DAU-induced HF. Using NVCMs, we found significant cytotoxicity of both PIs around their maximum plasma concentration (cmax) as well as significant augmentation of DAU cytotoxicity. In AVCMs, BTZ did not induce significant cytotoxicity in therapeutic concentrations, whereas the toxicity of CFZ was significant and more profound. Importantly, neither PI significantly augmented the cardiotoxicity of DAU despite even more profound proteasome-inhibitory activity in AVCMs compared with NVCMs. Furthermore, in young adult rabbits, no significant augmentation of chronic ANT cardiotoxicity was noted with respect to any functional, morphological, biochemical or molecular parameter under study, despite significant inhibition of myocardial proteasome activity. Our experimental data show that combination of PIs with ANTs is not accompanied by an exaggerated risk of cardiotoxicity and HF in young adult animal cardiomyocytes and hearts.
    WorkplaceInstitute of Physiology
    ContactLucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400
    Year of Publishing2020
    Electronic addresshttps://doi.org/10.1042/CS20190139
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