Back to Search
Start Over
Flavonolignans inhibit ADP induced blood platelets activation and aggregation in whole blood.
- Source :
-
International journal of biological macromolecules [Int J Biol Macromol] 2017 Feb; Vol. 95, pp. 682-688. Date of Electronic Publication: 2016 Dec 05. - Publication Year :
- 2017
-
Abstract
- Flavonolignans are a group of active chemical compounds presented in the silymarin - a standardized extract obtained from fruits and seeds of Milk thistle (Silybum marianum L. Gaernt.). Since the 70s of the last century, flavonolignans have been regarded to the official medicine as a substances having hepatoprotective properties. However many researches performed in recent years have demonstrated that flavonolignans posses many other healthy properties including modulation of variety cell-signaling pathways. The aim of our study was to examine the effects of three major flavonolignans (silybin, silychristin and silydianin) on ADP-induced blood platelet activation using the flow cytometry analysis as well as determine the mechanism of this interaction by bioinformatic ligand docking method. We observed that all tested flavonolignans in dose-dependent manner inhibit formation of blood platelet aggregates and microparticles as well as decrease expression of P-selectin and activation of integrin α <subscript>IIb</subscript> β <subscript>3</subscript> . Our computer-generated models confirm the flow cytometry analysis. We observed that all tested flavonolignans have conformations which are able to bind to the extracellular domain of P2Y12 receptor and probably block interaction with ADP. Our studies may help in the development of a new potential anti-platelet agent, which might be an alternative to the current using drugs.<br /> (Copyright © 2016 Elsevier B.V. All rights reserved.)
- Subjects :
- Dose-Response Relationship, Drug
Flavonolignans metabolism
Humans
Molecular Docking Simulation
Protein Conformation
Receptors, Purinergic P2Y12 chemistry
Receptors, Purinergic P2Y12 metabolism
Adenosine Diphosphate pharmacology
Blood Platelets drug effects
Blood Platelets physiology
Flavonolignans pharmacology
Platelet Aggregation drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1879-0003
- Volume :
- 95
- Database :
- MEDLINE
- Journal :
- International journal of biological macromolecules
- Publication Type :
- Academic Journal
- Accession number :
- 27923566
- Full Text :
- https://doi.org/10.1016/j.ijbiomac.2016.12.002