A Review of Coumarins and Coumarin-Related Compounds for Their Potential Antidiabetic Effect

Abstract

Background and aims: Worldwide, type 2 diabetes mellitus accounts for a considerable burden of disease, with an estimated global cost of >800 billion USD annually. For this reason, the search for more effective and efficient therapeutic anti-diabetic agents is continuing. Coumarins are naturally derived and synthetic molecules with a wide variety of biological actions. The most common application of these molecules in medicine is for their thrombostatic activity. This study aims to give an overview of the current knowledge about the applicability of these chemical products in the therapeutic strategy against diabetes and its complications. Methods: For this purpose, we searched internet databases for publications and abstracts in English that investigated the effects of coumarins or coumarin-like agents with potential anti-diabetic activity. Results: The result is that a variety of these agents have proven in in vitro, in silico, and simple animal models to possess properties that may reduce the glucose absorption rate in the intestines, increase the level of insulin, increase the cellular uptake of glucose or reduce the gluconeogenesis. In addition, some of these agents also reduced the level of glycation of peptides in diabetic animal models and showed antioxidant properties. Conclusion: In conclusion, we can summarize that coumarins and their related derivatives may be potential antidiabetic agents. Useful formulations with appropriate pharmacokinetic and pharmacodynamic properties must be developed and tested for their efficacy and toxicity in comprehensive animal models before they can enter clinical trials.

Comparative Analysis of Qualitative and Quantitative Phytochemical Evaluation of Selected Leaves of Medicinal Plants in Jaffna, Sri Lanka

“…Coumarins are present in all selected plants. Coumarins have many biochemical and pharmacological properties which may be effective against diabetes and its complications, some of which are of potential therapeutic interest 30 . Tannins are thought to have various properties, including analgesic, anti-diabetic, and anti-inflammatory properties.…”

Cichorioside a biocoumarin modulates lipid and glucose storage on 3T3-L1 cell lines: In vitro and in silico approach

“…16,17 In addition, coumarins showed broad pharmacological activities. 18,19 Coumarins and their derivatives demonstrated various therapeutic properties including antioxidant, 20 antiinflammatory, 21 anticancer, 22 anti-diabetic 23 and anti-obesity. 24 These talented findings provoked us to evaluate the anti-obesity activity of the coumarin glucoside, namely Cichorioside (cichoriin).…”

Synthesis and Vasorelaxant Activity of Nitrate−Coumarin Derivatives

“…Due to their large number of pharmacological and biochemical properties, they constitute an important group of pharmacological agents with potential therapeutic application. Several studies, including those carried out by our group, have shown that a pharmacomodulation of the coumarin structure can give rise to different pharmacological activities: monoamine oxidase inhibition,[ 9 , 10 ] acetyl‐ and butyrylcholinesterase inhibition,[ 11 , 12 ] antioxidant,[ 13 , 14 ] anti‐inflammatory,[ 15 , 16 ] antithrombotic,[ 17 , 18 ] inhibition of β‐amyloid aggregation [19] and vasorelaxant. [ 20 , 21 , 22 , 23 , 24 ] The vasorelaxant effects begin to be observed at concentrations in the micromolar range, reaching the higher effects at concentrations in the millimolar range.…”