State Key Laboratory of Southwestern Chinese Medicine Resources, Pharmacy School, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, PR China.
Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, PR China.
Biomed Pharmacother. 2021 Jul;139:111561. doi: 10.1016/j.biopha.2021.111561. Epub 2021 Apr 10.
Heparin is the earliest and most widely used anticoagulant and antithrombotic drug that is still used in a variety of clinical indications. Since it was discovered in 1916, after more than a century of repeated exploration, heparin has not been replaced by other drugs, but a great progress has been made in its basic research and clinical application. Besides anticoagulant and antithrombotic effects, heparin also has antitumor, anti-inflammatory, antiviral, and other pharmacological activities. It is widely used clinically in cardiovascular and cerebrovascular diseases, lung diseases, kidney diseases, cancer, etc., as the first anticoagulant medicine in COVID-19 exerts anticoagulant, anti-inflammatory and antiviral effects. At the same time, however, it also leads to a lot of adverse reactions, such as bleeding, thrombocytopenia, elevated transaminase, allergic reactions, and others. This article comprehensively reviews the modern research progress of heparin compounds; discusses the structure, preparation, and adverse reactions of heparin; emphasizes the pharmacological activity and clinical application of heparin; reveals the possible mechanism of the therapeutic effect of heparin in related clinical applications; provides evidence support for the clinical application of heparin; and hints on the significance of exploring the wider application fields of heparin.
肝素是最早、应用最广泛的抗凝和抗血栓药物,至今仍广泛应用于多种临床适应证。自 1916 年发现以来,经过一个多世纪的反复探索,肝素在基础研究和临床应用方面都取得了很大进展。除了抗凝和抗血栓作用外,肝素还具有抗肿瘤、抗炎、抗病毒等药理作用。肝素在心血管和脑血管疾病、肺部疾病、肾脏疾病、癌症等方面得到了广泛的临床应用,作为 COVID-19 的首选用抗凝药物发挥抗凝、抗炎和抗病毒作用。然而,同时也导致了许多不良反应,如出血、血小板减少、转氨酶升高、过敏反应等。本文全面综述了肝素化合物的现代研究进展;讨论了肝素的结构、制备和不良反应;强调了肝素的药理学活性和临床应用;揭示了肝素在相关临床应用中的治疗效果的可能机制;为肝素的临床应用提供了证据支持;并提示了探索肝素更广泛应用领域的意义。