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The effect of silymarin flavonolignans and their sulfated conjugates on platelet aggregation and blood vessels ex vivo

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    SYSNO ASEP0518345
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleThe effect of silymarin flavonolignans and their sulfated conjugates on platelet aggregation and blood vessels ex vivo
    Author(s) Pourová, J. (CZ)
    Applová, L. (CZ)
    Macáková, K. (CZ)
    Vopršalová, M. (CZ)
    Migkos, T. (CZ)
    Bentanachs, R. (CZ)
    Biedermann, David (MBU-M) RID, ORCID
    Petrásková, Lucie (MBU-M) ORCID
    Tvrdý, V. (CZ)
    Hrubša, M. (CZ)
    Karlíčková, J. (CZ)
    Křen, Vladimír (MBU-M) RID, ORCID
    Valentová, Kateřina (MBU-M) RID, ORCID
    Mladěnka, P. (CZ)
    Article number2286
    Source TitleNutrients. - : MDPI
    Roč. 11, č. 10 (2019)
    Number of pages16 s.
    Languageeng - English
    CountryCH - Switzerland
    KeywordsSilymarin ; Milk Thiste ; Flavonolignans
    Subject RIVFA - Cardiovascular Diseases incl. Cardiotharic Surgery
    OECD categoryCardiac and Cardiovascular systems
    R&D ProjectsGA18-00121S GA ČR - Czech Science Foundation (CSF)
    LTC18003 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
    LTC18071 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
    Method of publishingOpen access
    Institutional supportMBU-M - RVO:61388971
    UT WOS000498227300027
    EID SCOPUS85072847662
    DOI10.3390/nu11102286
    AnnotationSilymarin is a traditional drug and food supplement employed for numerous liver disorders. The available studies indicate that its activities may be broader, in particular due to claimed benefits in some cardiovascular diseases, but the contributions of individual silymarin components are unclear. Therefore, we tested silymarin flavonolignans as pure diastereomers as well as their sulfated metabolites for potential vasorelaxant and antiplatelet effects in isolated rat aorta and in human blood, respectively. Eleven compounds from a panel of 17 tested exhibited a vasorelaxant effect, with half maximal effective concentrations (EC50) ranging from 20 to 100 µM, and some substances retained certain activity even in the range of hundreds of nM. Stereomers A were generally more potent as vasorelaxants than stereomers B. Interestingly, the most active compound was a metabolite-silychristin-19-O-sulfate. Although initial experiments showed that silybin, 2,3-dehydrosilybin, and 2,3-dehydrosilychristin were able to substantially block platelet aggregation, their effects were rapidly abolished with decreasing concentration, and were negligible at concentrations ≤100 µM. In conclusion, metabolites of silymarin flavonolignans seem to have biologically relevant vasodilatory properties, but the effect of silymarin components on platelets is low or negligible.
    WorkplaceInstitute of Microbiology
    ContactEliška Spurná, eliska.spurna@biomed.cas.cz, Tel.: 241 062 231
    Year of Publishing2020
    Electronic addresshttps://www.mdpi.com/2072-6643/11/10/2286
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