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Anticoagulant Activities of Indobufen, an Antiplatelet Drug

Indobufen is a new generation of anti-platelet aggregation drug, but studies were not sufficient on its anticoagulant effects. In the present study, the anticoagulant activity of indobufen was determined by monitoring the activated partial thromboplastin time (APTT), prothrombin time (PT), and throm...

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Detalles Bibliográficos
Autores principales: Liu, Jia, Xu, Dan, Xia, Nian, Hou, Kai, Chen, Shijie, Wang, Yu, Li, Yunman
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099839/
https://www.ncbi.nlm.nih.gov/pubmed/29914049
http://dx.doi.org/10.3390/molecules23061452
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author Liu, Jia
Xu, Dan
Xia, Nian
Hou, Kai
Chen, Shijie
Wang, Yu
Li, Yunman
author_facet Liu, Jia
Xu, Dan
Xia, Nian
Hou, Kai
Chen, Shijie
Wang, Yu
Li, Yunman
author_sort Liu, Jia
collection PubMed
description Indobufen is a new generation of anti-platelet aggregation drug, but studies were not sufficient on its anticoagulant effects. In the present study, the anticoagulant activity of indobufen was determined by monitoring the activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT) in rabbit plasma. We evaluated the anticoagulant mechanisms on the content of the platelet factor 3,4 (PF3,4), and the coagulation factor 1, 2, 5, 8, 10 (FI, II, V, VIII, X) in rabbits, as well as the in vivo bleeding time and clotting time in mice. The pharmacodynamic differences between indobufen and warfarin sodium, rivaroxaban, and dabigatran were further studied on thrombus formation and the content of FII and FX in rats. Animal experiments showed that intragastric-administrated indobufen can significantly reduce the APTT, PT, TT, PF3, FI, II, V, VIII, and X plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban. These results suggest that indobufen has some anticoagulant effects as strong as some conventional anticoagulants. The mechanism may be related to both exogenous and endogenous coagulation system.
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spelling pubmed-60998392018-11-13 Anticoagulant Activities of Indobufen, an Antiplatelet Drug Liu, Jia Xu, Dan Xia, Nian Hou, Kai Chen, Shijie Wang, Yu Li, Yunman Molecules Article Indobufen is a new generation of anti-platelet aggregation drug, but studies were not sufficient on its anticoagulant effects. In the present study, the anticoagulant activity of indobufen was determined by monitoring the activated partial thromboplastin time (APTT), prothrombin time (PT), and thrombin time (TT) in rabbit plasma. We evaluated the anticoagulant mechanisms on the content of the platelet factor 3,4 (PF3,4), and the coagulation factor 1, 2, 5, 8, 10 (FI, II, V, VIII, X) in rabbits, as well as the in vivo bleeding time and clotting time in mice. The pharmacodynamic differences between indobufen and warfarin sodium, rivaroxaban, and dabigatran were further studied on thrombus formation and the content of FII and FX in rats. Animal experiments showed that intragastric-administrated indobufen can significantly reduce the APTT, PT, TT, PF3, FI, II, V, VIII, and X plasma contents. Its inhibitory effect on plasma FII was better than thrombin inhibitor dabigatran with effect on FX better than FXa inhibitor rivaroxaban. These results suggest that indobufen has some anticoagulant effects as strong as some conventional anticoagulants. The mechanism may be related to both exogenous and endogenous coagulation system. MDPI 2018-06-15 /pmc/articles/PMC6099839/ /pubmed/29914049 http://dx.doi.org/10.3390/molecules23061452 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Liu, Jia
Xu, Dan
Xia, Nian
Hou, Kai
Chen, Shijie
Wang, Yu
Li, Yunman
Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title_full Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title_fullStr Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title_full_unstemmed Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title_short Anticoagulant Activities of Indobufen, an Antiplatelet Drug
title_sort anticoagulant activities of indobufen, an antiplatelet drug
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6099839/
https://www.ncbi.nlm.nih.gov/pubmed/29914049
http://dx.doi.org/10.3390/molecules23061452
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