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  2. Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review

Pharmacological Activities and Mechanisms of Hirudin and Its Derivatives - A Review

  • Front Pharmacol. 2021 Apr 16;12:660757. doi: 10.3389/fphar.2021.660757.
Chen Junren 1 2 Xie Xiaofang 1 2 Zhang Huiqiong 1 2 Li Gangmin 1 2 Yin Yanpeng 1 2 Cao Xiaoyu 1 2 Gao Yuqing 1 2 Li Yanan 1 2 Zhang Yue 1 2 Peng Fu 1 2 3 Peng Cheng 1 2
Affiliations

Affiliations

  • 1 State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu, China.
  • 2 Chengdu University of Traditional Chinese Medicine, Chengdu, China.
  • 3 West China School of Pharmacy, Sichuan University, Chengdu, China.
Abstract

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.

Keywords

anti-fibrosis; anti-thrombosis; mechanisms; natural hirudin; recombinant hirudin; wound repair.

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