Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation
Coumarin was first discovered in Tonka bean and then widely in other plants. Coumarin has an anticoagulant effect, and its derivative, warfarin, is a vitamin K analogue that inhibits the synthesis of clotting factors and is more widely used in the clinical treatment of endovascular embolism. At pres...
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MDPI AG
2022-06-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/27/13/4054 |
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| author | Ping-Hsun Lu Tzu-Hsien Liao Yau-Hung Chen Yeng-Ling Hsu Chan-Yen Kuo Chuan-Chi Chan Lu-Kai Wang Ching-Yuh Chern Fu-Ming Tsai |
| author_facet | Ping-Hsun Lu Tzu-Hsien Liao Yau-Hung Chen Yeng-Ling Hsu Chan-Yen Kuo Chuan-Chi Chan Lu-Kai Wang Ching-Yuh Chern Fu-Ming Tsai |
| author_sort | Ping-Hsun Lu |
| collection | DOAJ |
| description | Coumarin was first discovered in Tonka bean and then widely in other plants. Coumarin has an anticoagulant effect, and its derivative, warfarin, is a vitamin K analogue that inhibits the synthesis of clotting factors and is more widely used in the clinical treatment of endovascular embolism. At present, many artificial chemical synthesis methods can be used to modify the structure of coumarin to develop many effective drugs with low toxicity. In this study, we investigated the effects of six coumarin derivatives on the platelet aggregation induced by adenosine diphosphate (ADP). We found that the six coumarin derivatives inhibited the active form of GPIIb/IIIa on platelets and hence inhibit platelet aggregation. We found that 7-hydroxy-3-phenyl 4H-chromen-4-one (7-hydroxyflavone) had the most severe effect. In addition, we further analyzed the downstream signal transduction of the ADP receptor, including the release of calcium ions and the regulation of cAMP, which were inhibited by the six coumarin derivatives selected in this study. These results suggest that coumarin derivatives inhibit coagulation by inhibiting the synthesis of coagulation factors and they may also inhibit platelet aggregation. |
| first_indexed | 2024-03-09T12:45:13Z |
| format | Article |
| id | doaj.art-c1044cd3723c4af0ac96e9544d203bf5 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-09T12:45:13Z |
| publishDate | 2022-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-c1044cd3723c4af0ac96e9544d203bf52023-11-30T22:13:32ZengMDPI AGMolecules1420-30492022-06-012713405410.3390/molecules27134054Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and AggregationPing-Hsun Lu0Tzu-Hsien Liao1Yau-Hung Chen2Yeng-Ling Hsu3Chan-Yen Kuo4Chuan-Chi Chan5Lu-Kai Wang6Ching-Yuh Chern7Fu-Ming Tsai8Department of Chinese Medicine, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City 231, TaiwanDepartment of Chinese Medicine, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City 231, TaiwanDepartment of Chemistry, Tamkang University, New Taipei City 251, TaiwanDepartment of Applied Chemistry, National Chia-Yi University, Chiayi City 600, TaiwanDepartment of Research, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City 231, TaiwanDepartment of Laboratory Medicine, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City 231, TaiwanDepartment of Life Sciences, Ministry of Science and Technology, Taipei 106, TaiwanDepartment of Applied Chemistry, National Chia-Yi University, Chiayi City 600, TaiwanDepartment of Research, Taipei Tzu Chi Hospital, Buddhist Tzu Chi Medical Foundation, New Taipei City 231, TaiwanCoumarin was first discovered in Tonka bean and then widely in other plants. Coumarin has an anticoagulant effect, and its derivative, warfarin, is a vitamin K analogue that inhibits the synthesis of clotting factors and is more widely used in the clinical treatment of endovascular embolism. At present, many artificial chemical synthesis methods can be used to modify the structure of coumarin to develop many effective drugs with low toxicity. In this study, we investigated the effects of six coumarin derivatives on the platelet aggregation induced by adenosine diphosphate (ADP). We found that the six coumarin derivatives inhibited the active form of GPIIb/IIIa on platelets and hence inhibit platelet aggregation. We found that 7-hydroxy-3-phenyl 4H-chromen-4-one (7-hydroxyflavone) had the most severe effect. In addition, we further analyzed the downstream signal transduction of the ADP receptor, including the release of calcium ions and the regulation of cAMP, which were inhibited by the six coumarin derivatives selected in this study. These results suggest that coumarin derivatives inhibit coagulation by inhibiting the synthesis of coagulation factors and they may also inhibit platelet aggregation.https://www.mdpi.com/1420-3049/27/13/4054coumarinplateletsADPaggregation7-hydroxyflavoneflavonoids |
| spellingShingle | Ping-Hsun Lu Tzu-Hsien Liao Yau-Hung Chen Yeng-Ling Hsu Chan-Yen Kuo Chuan-Chi Chan Lu-Kai Wang Ching-Yuh Chern Fu-Ming Tsai Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation Molecules coumarin platelets ADP aggregation 7-hydroxyflavone flavonoids |
| title | Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation |
| title_full | Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation |
| title_fullStr | Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation |
| title_full_unstemmed | Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation |
| title_short | Coumarin Derivatives Inhibit ADP-Induced Platelet Activation and Aggregation |
| title_sort | coumarin derivatives inhibit adp induced platelet activation and aggregation |
| topic | coumarin platelets ADP aggregation 7-hydroxyflavone flavonoids |
| url | https://www.mdpi.com/1420-3049/27/13/4054 |
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