Natural Coumarins: Exploring the Pharmacological Complexity and Underlying Molecular Mechanisms

Abstract

Coumarins belong to the benzopyrone family commonly found in many medicinal plants. Natural coumarins demonstrated a wide spectrum of pharmacological activities, including anti-inflammatory, anticoagulant, anticancer, antibacterial, antimalarial, casein kinase-2 (CK2) inhibitory, antifungal, antiviral, Alzheimer's disease inhibition, neuroprotective, anticonvulsant, phytoalexins, ulcerogenic, and antihypertensive. There are very few studies on the bioavailability of coumarins; therefore, further investigations are necessitated to study the bioavailability of different coumarins which already showed good biological activities in previous studies. On the evidence of varied pharmacological properties, the present work presents an overall review of the derivation, availability, and biological capacities of coumarins with further consideration of the essential mode of their therapeutic actions. In conclusion, a wide variety of coumarins are available, and their pharmacological activities are of current interest thanks to their synthetic accessibility and riches in medicinal plants. Coumarins perform the valuable function as therapeutic agents in a range of medical fields.

Figure 1

Diagram with the most relevant pharmacological properties related to chemical structures of natural coumarins and their derivatives.

Figure 2

Schematic representation of molecular mechanisms and signaling pathways of the most representative coumarins and their derivatives. Abbreviations: COX-2: cyclooxygenase 2; iNOS: inducible nitric oxide synthase, PTP-1B: protein tyrosine phosphatase; MAO: monoamine oxidase.