This chapter gives an overview of medical applications of coumarins, in particular the history and evolution of warfarin and related compounds as important anticoagulant agents. Anticoagulants reduce the risks of undesirable blood clots leading to myocardial infarction, pulmonary embolism, and ischemic stroke among others. Due to this action, these coumarins are a major group of oral drugs with anticoagulant activity. The mechanism of action of these anticoagulants lies in the competitive antagonism of vitamin K, through which they inhibit coagulation of blood in the body by preventing the production of prothrombin and several other coagulation factors. Despite the wide availability of coumarins and their lead compounds and metabolites in natural products, their application up till now has been mostly limited to the anticoagulant activity of warfarin derived from dicoumarol and its analogues. The clinical application of these actions has yet to be demonstrated.Ĭoumarins are members of the benzopyrone class of organic compounds that are found in many plants and possess a variety of pharmacological properties such as antimicrobial, anti-inflammatory, antidiabetic, and antioxidant activity, as well as a significant influence on physiological processes like enzyme inhibitory activity. Recent findings propose additional uses like anti-tumor and antibiotic actions for coumarins. In addition, there is a significant augmentation of the anticoagulant activity when used in combination with non-steroidal anti-inflammatory agents and agents interfering with the metabolism of the coumarins. Extreme caution is warranted when given to menstruating women, patients suffering from disorders prone to bleeding like gastric ulcer and rheumatoid arthritis, and to persons with a high likelihood of blunt and sharp trauma. The anticoagulant activity can also lead to undesired bleeding. Due to this action, these coumarins are a major group of drugs with anticoagulant activity. Their mechanism of action lies in the competitive antagonism of vitamin K, through which they inhibit coagulation in the body by preventing the production of prothrombin. Warfarin and its derivatives are coumarins used today in medical practice.
Current research suggests that at least some of the actions described may be attributable to the action of these coumarins. Historical reports mention the application of medicinal plants containing coumarins against various ailments.
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