An insight into the therapeutic applications of coumarin compounds and their mechanisms of action

Abstract

The coumarins are heterocyclic compounds belonging to the class of benzopyrone enriched in various plants like tonka beans. Coumarins and their derivatives exert a vast array of bioactive properties such as anticoagulant, antibacterial, anti-inflammatory, antioxidant, antitumor, antiviral, and enzyme inhibition. Higher doses of coumarin are found to be hepatotoxic however they exhibit beneficial effects by reducing the risk of cancer and other neuronal and cardiovascular ailments. Most of these effects can be attributed to their free radical scavenging effects. Coumarins such as umbelliferone, esculetin and quercetin show antioxidant properties and protect the cellular DNA from oxidative damage. The dicumarol shows anticoagulant properties by inhibiting the action of vitamin K, whereas angelmarin has been reported to be cytotoxic in pancreatic cancer. Coumarins also reduce edema and inflammation by inhibiting the prostaglandins biosynthesis. Hydroxyl aromatic substituted derivatives such as 5-hydroxycoumarin or vicinal dihydroxy coumarins have also been found to be potent anti-inflammatory agents. Some coumarins are approved by the FDA as drugs, and warfarin is one such example. It blocks the Vitamin K reductase enzyme thus disrupting the clotting mechanism. In conclusion, the coumarin class of phytomolecules has a lot of potential to be used as drugs for various diseases. Much work is needed to bring them at the stage of clinical trials for further approval. There is a lot of hope for this unexplored area of translational research.

Keywords: Anti-inflammatory; Anticoagulant; Coumarin derivatives; Coumarins; Esculetin; Warfarin.