Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1
Atherosclerotic cardiovascular disease is the leading cause of death in developed countries. Therefore, there is an increasing interest in developing new potent and safe antiplatelet agents. Coumarins are a family of polyphenolic compounds with several pharmacological activities, including platelet...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-05-01
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| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/26/10/3036 |
| _version_ | 1827692039912816640 |
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| author | Cristina Zaragozá Francisco Zaragozá Irene Gayo-Abeleira Lucinda Villaescusa |
| author_facet | Cristina Zaragozá Francisco Zaragozá Irene Gayo-Abeleira Lucinda Villaescusa |
| author_sort | Cristina Zaragozá |
| collection | DOAJ |
| description | Atherosclerotic cardiovascular disease is the leading cause of death in developed countries. Therefore, there is an increasing interest in developing new potent and safe antiplatelet agents. Coumarins are a family of polyphenolic compounds with several pharmacological activities, including platelet aggregation inhibition. However, their antiplatelet mechanism of action needs to be further elucidated. The aim of this study is to provide insight into the biochemical mechanisms involved in this activity, as well as to establish a structure–activity relationship for these compounds. With this purpose, the antiplatelet aggregation activities of coumarin, esculetin and esculin were determined in vitro in human whole blood and platelet-rich plasma, to set the potential interference with the arachidonic acid cascade. Here, the platelet COX activity was evaluated from 0.75 mM to 6.5 mM concentration by measuring the levels of metabolites derived from its activity (MDA and TXB<sub>2</sub>), together with colorimetric assays performed with the pure recombinant enzyme. Our results evidenced that the coumarin aglycones present the greatest antiplatelet activity at 5 mM and 6.5 mM on aggregometry experiments and inhibiting MDA levels. |
| first_indexed | 2024-03-10T11:14:51Z |
| format | Article |
| id | doaj.art-1a975e0a36cd4368a7bd28d130b5b574 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T11:14:51Z |
| publishDate | 2021-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-1a975e0a36cd4368a7bd28d130b5b5742023-11-21T20:27:54ZengMDPI AGMolecules1420-30492021-05-012610303610.3390/molecules26103036Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1Cristina Zaragozá0Francisco Zaragozá1Irene Gayo-Abeleira2Lucinda Villaescusa3Pharmacology Unit, Biomedical Sciences Department, University of Alcalá, Alcalá de Henares, 28871 Madrid, SpainPharmacology Unit, Biomedical Sciences Department, University of Alcalá, Alcalá de Henares, 28871 Madrid, SpainPharmacology Unit, Biomedical Sciences Department, University of Alcalá, Alcalá de Henares, 28871 Madrid, SpainPharmacology Unit, Biomedical Sciences Department, University of Alcalá, Alcalá de Henares, 28871 Madrid, SpainAtherosclerotic cardiovascular disease is the leading cause of death in developed countries. Therefore, there is an increasing interest in developing new potent and safe antiplatelet agents. Coumarins are a family of polyphenolic compounds with several pharmacological activities, including platelet aggregation inhibition. However, their antiplatelet mechanism of action needs to be further elucidated. The aim of this study is to provide insight into the biochemical mechanisms involved in this activity, as well as to establish a structure–activity relationship for these compounds. With this purpose, the antiplatelet aggregation activities of coumarin, esculetin and esculin were determined in vitro in human whole blood and platelet-rich plasma, to set the potential interference with the arachidonic acid cascade. Here, the platelet COX activity was evaluated from 0.75 mM to 6.5 mM concentration by measuring the levels of metabolites derived from its activity (MDA and TXB<sub>2</sub>), together with colorimetric assays performed with the pure recombinant enzyme. Our results evidenced that the coumarin aglycones present the greatest antiplatelet activity at 5 mM and 6.5 mM on aggregometry experiments and inhibiting MDA levels.https://www.mdpi.com/1420-3049/26/10/3036coumarinesculinesculetinantiplatelet activityimpedance aggregometryCOX |
| spellingShingle | Cristina Zaragozá Francisco Zaragozá Irene Gayo-Abeleira Lucinda Villaescusa Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 Molecules coumarin esculin esculetin antiplatelet activity impedance aggregometry COX |
| title | Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 |
| title_full | Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 |
| title_fullStr | Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 |
| title_full_unstemmed | Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 |
| title_short | Antiplatelet Activity of Coumarins: In Vitro Assays on COX-1 |
| title_sort | antiplatelet activity of coumarins in vitro assays on cox 1 |
| topic | coumarin esculin esculetin antiplatelet activity impedance aggregometry COX |
| url | https://www.mdpi.com/1420-3049/26/10/3036 |
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