Affiliation:
1. LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Rua de Jorge Viterbo Ferreira No. 228, 4050-313 Porto, Portugal
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 anti-diabetic targets.
Funder
European Regional Development Fund
Programa Operacional Competitividade e Internacionalização
Fundação para a Ciência e a Tecnologia
Publisher
Bentham Science Publishers Ltd.
Subject
Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry
Reference105 articles.
1. Zhuang C.; Zhang W.; Sheng C.; Zhang W.; Xing C.; Miao Z.; Chalcone: a privileged structure in medicinal chemistry. Chem Rev 2017,117(12),7762-7810
2. Cazarolli L.H.; Kappel, V.D.; Zanatta, A.P.; Suzuki,
D.O.H.; Yunes, R.A.; Nunes, R.J.; Pizzolatti, M.G.; Silva,
F.R.M.B. In Studies In Natural Products Chemistry 2013,39,47-89
3. Chopra G.; Chalcones: a brief review. Int J Res Eng Appl Sci 2016,6(5),173-185
4. Evranos Aksöz B.; Ertan R.; Chemical and structural properties of chalcones I. Fabad J Pharm Sci 2011,36(4),223-242
5. Gaonkar S.L.; Vignesh U.N.; Synthesis and pharmacological properties of chalcones: a review. Res Chem Intermed 2017,43(11),6043-6077
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