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

0518345 - MBÚ 2020 RIV CH eng J - Journal Article
Pourová, J. - Applová, L. - Macáková, K. - Vopršalová, M. - Migkos, T. - Bentanachs, R. - Biedermann, David - Petrásková, Lucie - Tvrdý, V. - Hrubša, M. - Karlíčková, J. - Křen, Vladimír - Valentová, Kateřina - Mladěnka, P.
The effect of silymarin flavonolignans and their sulfated conjugates on platelet aggregation and blood vessels ex vivo.
Nutrients. Roč. 11, č. 10 (2019), č. článku 2286. E-ISSN 2072-6643
R&D Projects: GA ČR(CZ) GA18-00121S; GA MŠMT(CZ) LTC18003; GA MŠMT(CZ) LTC18071
Institutional support: RVO:61388971
Keywords : Silymarin * Milk Thiste * Flavonolignans
OECD category: Cardiac and Cardiovascular systems
Impact factor: 4.546, year: 2019
Method of publishing: Open access
https://www.mdpi.com/2072-6643/11/10/2286

Silymarin 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.
Permanent Link: http://hdl.handle.net/11104/0303506