A Systematic Review on Anti-diabetic Properties of Chalcones

(E-pub Ahead of Print)

Author(s): Sonia Rocha, Daniela Ribeiro, Eduarda Fernandes*, Marisa Freitas*.

Journal Name: Current Medicinal Chemistry

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Abstract:

The use of anti-diabetic drugs has been increasing worldwide and the evolution of therapeutics has been enormous. Still, the currently available anti-diabetic drugs do not present the desired efficacy and are generally associated with serious adverse effects. Thus, entirely new interventions, addressing the underlying etiopathogenesis of type 2 diabetes mellitus, are required. Chalcones, secondary metabolites of terrestrial plants and precursors of the flavonoids biosynthesis, have been used for a long time in traditional medicine due to their wide-range of biological activities, from which the anti-diabetic activity stands out. This review systematizes the information found in literature about the anti-diabetic properties of chalcones, in vitro and in vivo. Chalcones are able to exert these properties by acting in different therapeutic targets: dipeptidyl peptidase 4 (DPP-4); glucose transporter type 4 (GLUT4), sodium glucose cotransporter 2 (SGLT2), α-amylase, α-glucosidase, aldose reductase (ALR), protein tyrosine phosphatase 1B (PTP1B), peroxisome proliferator-activated receptor-gamma (PPARγ) and adenosine monophosphate (AMP)-activated protein kinase (AMPK). Chalcones are, undoubtedly, promising anti-diabetic agents, and some crucial structural features have already been established. From the structure-activity relationships analysis, it can generally be stated that the presence of hydroxyl, prenyl and geranyl groups in their skeleton improves their activity for the evaluated antidiabetic targets.

Keywords: Antidiabetic drugs, chalcones, dipeptidyl peptidase 4 (DPP-4), glucose transporter type 4 (GLUT4), sodium glucose cotransporter 2 (SGLT2), α-amylase, α-glucosidase, aldose reductase (ALR), protein tyrosine phosphatase 1B (PTP1B), peroxisome proliferator-activated receptor-gamma (PPARγ), adenosine monophosphate (AMP)-activated protein kinase (AMPK), structure-activity relationship.

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Article Details

(E-pub Ahead of Print)
DOI: 10.2174/0929867325666181001112226
Price: $95

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