State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau.
School of Basic Medicine, Qingdao University, Qingdao, 266071, China.
Pharmacol Res. 2020 Oct;160:105193. doi: 10.1016/j.phrs.2020.105193. Epub 2020 Sep 8.
Dicoumarol is an oral anticoagulant agent prescribed in clinical for decades. It is a natural hydroxycoumarin discovered from the spoilage of Melilotus officinalis (L.) Pall and is originally discovered as a rodenticide. Due to its structural similarity to that of vitamin K, it significantly inhibits vitamin K epoxide reductase and acts as a vitamin K antagonist. Dicoumarol is mainly used as an anticoagulant to prevent thrombogenesis and to cure vascular thrombosis. Other biological activities besides anticoagulants such as anticancer, antimicrobial, antiviral, etc., have also been documented. The side effects of dicoumarol raise safety concerns for clinical application. In this review, the physicochemical property, the pharmacological activities, the side effects, and the pharmacokinetics of dicoumarol were summarized, aiming to provide a whole picture of the "old" anticoagulant.
双香豆素是一种临床应用数十年的口服抗凝剂。它是从草木樨（Melilotus officinalis（L.）Pall）变质中发现的天然羟基香豆素，最初被发现是一种灭鼠剂。由于其结构与维生素 K 相似，它能显著抑制维生素 K 环氧化物还原酶，并作为维生素 K 拮抗剂。双香豆素主要用作抗凝剂，以防止血栓形成和治疗血管血栓形成。除抗凝剂外，还有其他生物活性，如抗癌、抗菌、抗病毒等，也有记载。双香豆素的副作用引起了临床应用的安全问题。本综述总结了双香豆素的理化性质、药理学活性、副作用和药代动力学，旨在为这种“老”抗凝剂提供一个全面的了解。
