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Can Isoquinoline Alkaloids Affect Platelet Aggregation in Whole Human Blood?

Authors :
Mst Shamima Parvin
Marcel Hrubša
Jaka Fadraersada
Alejandro Carazo
Jana Karlíčková
Lucie Cahlíková
Jakub Chlebek
Kateřina Macáková
Přemysl Mladěnka
Source :
Toxins, Vol 14, Iss 7, p 491 (2022)
Publication Year :
2022
Publisher :
MDPI AG, 2022.

Abstract

Isoquinoline alkaloids have multiple biological activities, which might be associated with positive pharmacological effects as well as negative adverse reactions. As bleeding was suggested to be a side effect of the isoquinoline alkaloid berberine, we decided to ascertain if different isoquinoline alkaloids could influence hemocoagulation through the inhibition of either platelet aggregation or blood coagulation. Initially, a total of 14 compounds were screened for antiplatelet activity in whole human blood by impedance aggregometry. Eight of them demonstrated an antiplatelet effect against arachidonic acid-induced aggregation. Papaverine and bulbocapnine were the most potent compounds with biologically relevant IC50 values of 26.9 ± 12.2 μM and 30.7 ± 5.4 μM, respectively. Further testing with the same approach confirmed their antiplatelet effects by employing the most physiologically relevant inducer of platelet aggregation, collagen, and demonstrated that bulbocapnine acted at the level of thromboxane receptors. None of the alkaloids tested had an effect on blood coagulation measured by a mechanical coagulometer. In conclusion, the observed antiplatelet effects of isoquinoline alkaloids were found mostly at quite high concentrations, which means that their clinical impact is most likely low. Bulbocapnine was an exception. It proved to be a promising antiplatelet molecule, which may have biologically relevant effects.

Details

Language :
English
ISSN :
20726651
Volume :
14
Issue :
7
Database :
Directory of Open Access Journals
Journal :
Toxins
Publication Type :
Academic Journal
Accession number :
edsdoj.3005161ac514ba2b27ae769110251cd
Document Type :
article
Full Text :
https://doi.org/10.3390/toxins14070491