Chemistry, Toxicity, Synthesis, Biological and Pharmacological Activities of Coumarins and their Derivatives: Recent Advances and Future Perspectives

Coumarins are compounds found in plants, in bond form as esters or glycosides and also in free form. They are also found in fungi and exert many therapeutic effects. The name ‘coumarin’ is obtained from Dipteryx odorata (Coumarouna odorata Aube), a plant from which it was first isolated. These secondary metabolites are broadly found in many families of plants, and in their essential oil. They have been utilised as an aroma in pharmaceuticals, cosmetics, foods, and dyes production. Coumarins are lactones of 2-coumaric acid and are synthesized through a benzene ring fused to an α-pyrone ring. With respect to their structural and chemical complexity and diversity, coumarins from natural sources are grouped into various classes, including simple coumarins, furanocoumarins and pyranocuomarins. These compounds can also be designed and synthesized in the laboratory via various standard procedures. This gives rise to several derivatives of coumarins with synthetic origin and thus leads to remarkable increase in the number of the compound structures. Moreover, coumarin derivatives have increasingly appealed to ethnopharmacologist, ethnobotanists, and medicinal chemists due to their potential efficacy in preventing and managing metabolic and non-metabolic diseases. Thus, they are versatile compounds and can be transformed into different active analogues to address wide range of biological properties, including anticancer, antioxidant, anticoagulant, anti-inflammatory, antimicrobial, antidiabetic and other activities.

Despite the global advances made in the use of medicinal plants, the evaluation of their secondary metabolites in terms of synthesis, biological, and pharmacological activities as well as their toxicity profile are still elusive. Coumarins and their derivatives, which are polyphenolic compounds found in plants, have wide pharmacological actions due to their structural versatility. However, toxicity associated with many of these compounds are still scanty and this needs to be addressed as related to their therapeutic importance. In addition, coumarin derivatives can be designed, synthesized and investigated to ascertain their new biological activities via structure-activity relationships of their versatile structure. The aim of this Research Topic is to invite researchers and scientists to submit original research articles and review articles with focus on the biological and pharmacological activities of coumarins and their derivatives through preclinical and clinical studies.

We welcome manuscripts that explore the following:

• Critical overview of coumarins and their classes.

• A look into the various classes and subclass of coumarins, and their derivatives. Discussions on their biological and pharmacological relevance, recent advances and future prospects.

• Sources of coumarins and their derivatives from natural sources, with relevance to health-promoting properties.

• Metabolic cascades involved in the synthesis of various class of coumarins and their derivatives.

• Metabolic pathways for coumarins, their derivatives, biosynthesis and synthetic analogues.

• Detailed and comprehensive discussions of biological and pharmacological relevance of coumarins, their derivatives. Roles in treatments and managements of diseases.

• Toxicity and safety profile of coumarins and their derivatives.
Detailed description of coumarin toxicity, and safety in deference experimental studies.

• Structure activity relationship (SAR) of coumarins and their derivatives, with details for understanding of their biological activities and significance.

Importantly, the ethnopharmacological foundation or context of a study must be clearly laid out in the introduction to the manuscript. All the manuscripts submitted to the collection will need to fully comply with the Four Pillars of Best Practice in Ethnopharmacology (you can freely download the full version here)..