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Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review
Hirudin, an acidic polypeptide secreted by the salivary glands of Hirudo medicinalis (also known as “Shuizhi” in traditional Chinese medicine), is the strongest natural specific inhibitor of thrombin found so far. Hirudin has been demonstrated to possess potent anti-thrombotic effect in previous stu...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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Frontiers Media S.A.
2021
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8085555/ https://www.ncbi.nlm.nih.gov/pubmed/33935784 http://dx.doi.org/10.3389/fphar.2021.660757 |
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author | Junren, Chen Xiaofang, Xie Huiqiong, Zhang Gangmin, Li Yanpeng, Yin Xiaoyu, Cao Yuqing, Gao Yanan, Li Yue, Zhang Fu, Peng Cheng, Peng |
author_facet | Junren, Chen Xiaofang, Xie Huiqiong, Zhang Gangmin, Li Yanpeng, Yin Xiaoyu, Cao Yuqing, Gao Yanan, Li Yue, Zhang Fu, Peng Cheng, Peng |
author_sort | Junren, Chen |
collection | PubMed |
description | Hirudin, an acidic polypeptide secreted by the salivary glands of Hirudo medicinalis (also known as “Shuizhi” in traditional Chinese medicine), is the strongest natural specific inhibitor of thrombin found so far. Hirudin has been demonstrated to possess potent anti-thrombotic effect in previous studies. Recently, increasing researches have focused on the anti-thrombotic activity of the derivatives of hirudin, mainly because these derivatives have stronger antithrombotic activity and lower bleeding risk. Additionally, various bioactivities of hirudin have been reported as well, including wound repair effect, anti-fibrosis effect, effect on diabetic complications, anti-tumor effect, anti-hyperuricemia effect, effect on cerebral hemorrhage, and others. Therefore, by collecting and summarizing publications from the recent two decades, the pharmacological activities, pharmacokinetics, novel preparations and derivatives, as well as toxicity of hirudin were systematically reviewed in this paper. In addition, the clinical application, the underlying mechanisms of pharmacological effects, the dose-effect relationship, and the development potential in new drug research of hirudin were discussed on the purpose of providing new ideas for application of hirudin in treating related diseases. |
format | Online Article Text |
id | pubmed-8085555 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | Frontiers Media S.A. |
record_format | MEDLINE/PubMed |
spelling | pubmed-80855552021-05-01 Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review Junren, Chen Xiaofang, Xie Huiqiong, Zhang Gangmin, Li Yanpeng, Yin Xiaoyu, Cao Yuqing, Gao Yanan, Li Yue, Zhang Fu, Peng Cheng, Peng Front Pharmacol Pharmacology Hirudin, an acidic polypeptide secreted by the salivary glands of Hirudo medicinalis (also known as “Shuizhi” in traditional Chinese medicine), is the strongest natural specific inhibitor of thrombin found so far. Hirudin has been demonstrated to possess potent anti-thrombotic effect in previous studies. Recently, increasing researches have focused on the anti-thrombotic activity of the derivatives of hirudin, mainly because these derivatives have stronger antithrombotic activity and lower bleeding risk. Additionally, various bioactivities of hirudin have been reported as well, including wound repair effect, anti-fibrosis effect, effect on diabetic complications, anti-tumor effect, anti-hyperuricemia effect, effect on cerebral hemorrhage, and others. Therefore, by collecting and summarizing publications from the recent two decades, the pharmacological activities, pharmacokinetics, novel preparations and derivatives, as well as toxicity of hirudin were systematically reviewed in this paper. In addition, the clinical application, the underlying mechanisms of pharmacological effects, the dose-effect relationship, and the development potential in new drug research of hirudin were discussed on the purpose of providing new ideas for application of hirudin in treating related diseases. Frontiers Media S.A. 2021-04-16 /pmc/articles/PMC8085555/ /pubmed/33935784 http://dx.doi.org/10.3389/fphar.2021.660757 Text en Copyright © 2021 Junren, Xiaofang, Huiqiong, Gangmin, Yanpeng, Xiaoyu, Yuqing, Yanan, Yue, Fu and Cheng. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
spellingShingle | Pharmacology Junren, Chen Xiaofang, Xie Huiqiong, Zhang Gangmin, Li Yanpeng, Yin Xiaoyu, Cao Yuqing, Gao Yanan, Li Yue, Zhang Fu, Peng Cheng, Peng Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title | Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title_full | Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title_fullStr | Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title_full_unstemmed | Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title_short | Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review |
title_sort | pharmacological activities and mechanisms of hirudin and its derivatives - a review |
topic | Pharmacology |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8085555/ https://www.ncbi.nlm.nih.gov/pubmed/33935784 http://dx.doi.org/10.3389/fphar.2021.660757 |
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